Platform Technology

ENGLISH VERSION

NanoActive Alavelle™Aminolevulinic Acid Nanoliposomes

Product overview

NanoActive Alavelle™

Aminolevulinic Acid Nanoliposomes · Advanced ALA Delivery for Skin and Scalp Innovation

Powered by PURISOME® FlexVes™ Liposome Technology

Purui Biomedical Technology Co., Ltd. · Innovation for Health and Beauty

Product identity

One active ingredient, engineered for delivery

Product name

NanoActive Alavelle™ Aminolevulinic Acid Nanoliposomes

Active ingredient INCI name

AMINOLEVULINIC ACID

Scientific identity

5-Aminolevulinic acid (5-ALA)

Delivery platform

PURISOME® FlexVes™ Liposome Technology

AMINOLEVULINIC ACID identifies the active component. The complete raw material is a multicomponent liposomal composition; see the technical documentation for the full INCI list.

5-ALA is a natural biochemical precursor of protoporphyrin IX (PpIX) in the heme pathway.

Application development landscape

■ Sprays for facial and scalp coverage

■ Topical aqueous gels

■ Scalp serums and tonics

■ Professional photoactivated treatments

■ Daylight photodynamic applications

■ Oral formulation development

Why this ingredient, why now

Development opportunities

5-ALA is one of the most extensively studied actives in photodynamic dermatology—and one of the most challenging to formulate.

4 Interconnected opportunities, one delivery platform

01 Stabilize the active. Protect a pH-sensitive hydrophilic molecule within engineered vesicles, turning aqueous stability measured in days into a usable shelf life.

02 Deliver where it matters. Improve transport to target skin compartments and sebum-rich follicles, rather than leaving the active on the surface.

One platform, multiple formats. Sprays, gels, scalp care, professional photoactivation and daylight photodynamic applications, with a separate oral development pathway.

Design for comfort. Build dose, incubation and light exposure into the protocol so efficacy and tolerability are developed together.

 

Mechanism of action

ALA in cell biology: the heme pathway

What happens when ALA is supplied externally?

Exogenous ALA bypasses the rate-limiting ALA synthase step and heme feedback control. In metabolically active cells, including sebaceous glands and proliferative epidermis, limited ferrochelatase capacity favors PpIX accumulation in target tissue.

Schematic of heme biosynthesis. 5-ALA is a metabolic precursor of PpIX; it is not itself a photoactivated photosensitizer.

Innovation pathways

Two routes to application innovation

Route A—photoactivated chemistry

Vesicular delivery → intracellular PpIX → controlled illumination → photodynamic response

Skin renewal and photorejuvenation: 0.5% liposomal ALA spray + IPL has been studied for wrinkles and photodamage.

Pilosebaceous care: follicular delivery combined with IPL has been studied in inflammatory acne.

Daylight protocols: continuous low-dose activation has clinical validation in actinic keratosis studies.

Piccioni et al. | J Dermatolog Treat | 2011 · Yeung et al. | Dermatol Surg | 2011 · Dirschka et al. | JEADV | 2019

Route B—non-photodynamic combinations

ALA + iron/peptide cofactors → dermal papilla signaling → follicle research

No light required. ALA combined with ferric ammonium citrate activates ERK/AKT signaling in dermal papilla cells and supports hair-shaft elongation in ex vivo human follicles.

Combination logic. Peptide (GHK) and iron partners define the studied systems; results belong to the combination, not to ALA alone.

Ryu et al. | FEBS Open Bio | 2026 · Lee et al. | Ann Dermatol | 2016 · Morokuma et al. | Int J Dermatol | 2008

Formulation science

Why formulation matters: ALA is highly formulation-sensitive

1 · A hydrophilic zwitterion facing a lipid barrier

At physiological pH, ALA carries both positive and negative groups and partitions poorly into the lipid-rich stratum corneum. Unformulated aqueous ALA largely remains on the surface.

2 · pH-triggered dimerization, followed by oxidation

Above approximately pH 5, the deprotonated amino group of one ALA molecule attacks another molecule’s ketone group. The resulting dihydropyrazine (DHPY) oxidizes in air to inactive pyrazine (PY), with loss of PpIX-forming activity.

3 · Second-order decay that antioxidants cannot stop

Degradation accelerates with the square of the free ALA concentration. Chelators and antioxidants cannot stop the primary pathway; effective controls are pH, temperature and oxygen exclusion.

Measured half-life of 1% aqueous ALA (50 °C)

3 h

pH 7.42—near physiological pH

257 h

pH 4.81—mild acidification

37 d

Stable at pH 2.35—fully protonated amino group

The active’s microenvironment—pH, oxygen and molecular mobility—determines shelf life. Formulation creates the challenge and provides the solution.

Bunke et al. | J Pharm Sci | 2000 | PMID: 10980508 · Elfsson et al. | Eur J Pharm Sci | 1999 | PMID: 9845784

Delivery platform

PURISOME® FlexVes™: an architecture for hydrophilic actives

Phospholipid bilayer membrane

Aqueous core—hydrophilic ALA payload

Flexible, skin-compatible vesicle design

What this architecture does

Accommodates the payload correctly. ALA resides in aqueous and interfacial regions, associating with phospholipid headgroups rather than dissolving in oil.

Stabilizes the chemistry. Restricted molecular mobility and controlled local pH slow the dimerization that degrades aqueous ALA.

Prepares for delivery. A deformable lipid membrane supports partitioning into the stratum corneum and sebum-rich follicles.

Published studies of liposomal ALA delivery and treatment protocols are cited as technical background for this platform class.

PURISOME® FlexVes™ Liposome Technology

Formulation science

Stability through formulation design

01 Interfacial association. ALA associates with phospholipid headgroups, reducing free-molecule collisions that drive second-order dimerization.

02 Microenvironmental pH. A mildly acidic interface keeps amino groups protonated and unable to attack neighboring ketone groups.

03 Compartmentalization. Interfacial membranes restrict orientation and contact, turning one bulk phase into many isolated microenvironments.

04 Locally reduced oxygen. The lipid environment limits oxygen access to DHPY intermediates, slowing irreversible oxidation to inactive PY.

Published precedent. In a phospholipid nanovesicular gel containing 7.8% ALA, reported association with phosphatidylcholine polar headgroups extended stability from days in water to a shelf life of 24–36 months. PURISOME® vesicles apply the same physical rationale.

Days Aqueous solution → 24–36 months

Reported shelf life of a 7.8% ALA nanovesicular gel

Quality note: measure chemical stability (ALA content and pyrazine impurities) separately from vesicle size and appearance. Colloidal stability alone does not prove chemical stability. Antioxidants have little effect on the main condensation pathway; effective measures include pH below approximately 5 and oxygen exclusion.

Reinhold | Future Oncol | 2017 | PMID: 28805092 · Bunke et al. | J Pharm Sci | 2000 | PMID: 10980508

Formulation science

Aqueous vs nanovesicular systems: what changes for ALA?

Table expanded in original row order; all column labels and data are retained.

Read the shelf-life row correctly: 24–36 months refers to that specific proprietary nanovesicular gel. It is neither a general emulsion claim nor a NanoActive Alavelle™ specification. Every formulation needs its own stability program with ALA content and pyrazine impurities as endpoints; size and appearance alone cannot prove chemical stability.

Bunke et al. | J Pharm Sci | 2000 | PMID: 10980508 · Reinhold | Future Oncol | 2017 | PMID: 28805092 · Elfsson et al. | Eur J Pharm Sci | 1999

Delivery evidence

Delivery into skin and follicular compartments

Schematic: smaller vesicles can pass between corneocytes

Confocal cross-sections: as particle size decreases (a → c), fluorescent material reaches deeper skin layers

Particle size defines the depth budget

Vesicle size and membrane deformability determine how far the carrier delivers its payload. Comparative studies show that deformable liposomes can substantially improve ALA delivery into skin.

Follicles provide a fast route

Hair follicles and sebaceous glands bypass the stratum corneum and extend into the dermis. Lipid vesicles readily partition into this sebum-rich environment.

Local retention rather than systemic absorption

The goal is retention in skin compartments where PpIX forms. After topical ALA application, plasma levels remained within normal reference ranges; delivery is intended to be local.

Oh et al. | Eur J Pharm Sci | 2011 | PMID: 21782942 · Schmitz et al. | Photodiagn Photodyn Ther | 2016 · Rick et al. | J Photochem Photobiol B | 1997

Evidence—delivery

Low-concentration liposomal ALA: rapid, self-limiting PpIX formation

A 0.5% liposomal ALA spray saturates skin fluorescence in approximately 2 hours, with clearance within 8 hours.

Mean peak skin PpIX fluorescence, expressed as a percentage of maximum (healthy volunteers, n = 10). The source describes the protocols as statistically equivalent (P = 0.47).

Plateau at about 2 h. Non-occluded 0.5% liposomal ALA reaches a fluorescence plateau after approximately two hours.

Return to baseline within 8 h. The signal declines within minutes after removal and clears fully within eight hours, giving a short photosensitivity window.

Comparison with 20% cream. Fluorescence continues rising for approximately eight hours after removal of the high-concentration cream, producing a longer, less controllable exposure tail.

Concentrations here describe dose and kinetics, not a fold-increase in bioavailability.

Christiansen et al. | Lasers Surg Med | 2007 | PMID: 17457834

Mechanism—light

Photoactivation: PpIX photochemistry needs photons and oxygen

PpIX absorption profile: Soret band (approximately 405 nm) and Q bands (approximately 510–635 nm). Schematic, not to scale.

Blue light, 405–417 nm

Red light, 630–635 nm

Daylight and IPL cover the full activation spectrum

1 · Excitation. PpIX absorbs a photon and enters a long-lived triplet state.

2 · Energy transfer. Triplet PpIX transfers energy to dissolved molecular oxygen (Type II photochemistry), producing singlet oxygen and ROS.

3 · Local response. ROS act within micrometers of PpIX, mapping the response to the tissue reached by delivery.

4 · Dose rate is a design variable. Spectrum, irradiance and duration shape efficacy and comfort. Continuous low-rate daylight activation can deliver a comparable cumulative dose with much less pain than high-intensity lamps.

For photochemistry and PpIX photophysics, see Bunke et al. | J Pharm Sci | 2000 and Christiansen et al. | Lasers Surg Med | 2007.

Evidence—skin renewal

Photodynamic photorejuvenation: a measurable light dose guided by the skin

The liposomal ALA concept was developed for photodamaged skin: deliver a low-dose precursor, use skin fluorescence to indicate PpIX formation, then activate it with light.

1.7 vs 1.1

Mean participant-rated improvement in skin quality in a fluorescence-guided photodynamic rejuvenation study (0–4 scale)

2007

Mapping the fluorescence kinetics of 0.5% liposomal ALA in normal skin

2009

Fluorescence-controlled photorejuvenation: skin signals determine the light dose

2011

Wrinkle study: 30 participants, three liposomal ALA + IPL sessions

2011

A pilot study in inflammatory facial acne using the same spray + IPL approach

Implication for development: spray format, a 0.5% dose and IPL use have been published together, providing a literature template for professional photoactivated skin care.

Christiansen et al. | Lasers Surg Med | 2007 · Bjerring et al. | Lasers Surg Med | 2009; 41:327–336 · Piccioni et al. | 2011 · Yeung et al. | 2011

Clinical evidence—photorejuvenation

Wrinkle scores fall after three 0.5% liposomal ALA + IPL sessions

Mean modified Fitzpatrick wrinkle scores (lower is milder). These are means on an ordinal scale, not direct percentage measurements of wrinkle depth.

Study design

30 participants with facial photodamage

Three sessions of 0.5% liposomal ALA spray + IPL

Three-week intervals

Follow-up three months after the final session

Scores improved further between the last session and follow-up, consistent with ongoing post-treatment remodeling.

Piccioni et al. | J Dermatolog Treat | 2011 | DOI: 10.3109/09546634.2011.590791 | PMID: 21801099

Clinical evidence—dermal remodeling

Beyond wrinkle scores: the procollagen response after ALA-PDT

Mean target-antigen staining (%), paired biopsies before and one month after two ALA-PDT sessions. Values are approximate readings from Figure 2C. This is a photoactivation protocol, not evidence for unilluminated ALA.

Original histology (Figure 2B): Masson’s trichrome staining of dermal collagen

Study protocol

Two ALA-PDT sessions one month apart; 14 patients with facial actinic keratoses; 25 paired biopsies before treatment and one month afterward.

Histological findings

↑ Total dermal collagen; ↑ type I/III procollagen

↑ Epidermal TGF-β and TGF-β receptor II

↓ MMP-1, MMP-3 and MMP-12 (collagen-degrading enzymes)

↓ Solar elastosis; ↓ inflammatory infiltrates

ALA-PDT → ↑ TGF-β → ↑ procollagen I/III → ↓ MMP-1/3/12 → ↓ elastosis

Park MY, Sohn S, Lee ES, Kim YC | J Am Acad Dermatol | 2010;62:85–95 | DOI: 10.1016/j.jaad.2009.06.025 | PMID: 19926165

Clinical evidence—acne

Follicular delivery supports improvement in inflammatory acne

Pilosebaceous unit: the hair follicle and sebaceous gland as delivery targets

Why follicles matter. Inflammatory acne is a disease of the pilosebaceous unit, a structure preferentially accessed by lipid vesicles.

Delivery rationale. The lipophilic vesicle surface mixes with sebum, carrying the hydrophilic precursor down the follicular canal.

Activation rationale. PpIX forms in sebaceous tissue; IPL then drives a local photodynamic response.

Mean reduction in inflammatory lesion counts (%) after 0.5% liposomal ALA spray + IPL; pilot study in 12 participants.

Yeung et al. | Dermatol Surg | 2011 | DOI: 10.1111/j.1524-4725.2011.01929.x | PMID: 21414073

Evidence—tissue level

Tissue evidence: PpIX forms where the carrier delivers ALA

Full-thickness ex vivo skin—Maisch 2010

An ALA nanoemulsion induced measurable PpIX fluorescence in a full-thickness skin model: the delivered precursor reached viable epidermis and was metabolized there.

Ex vivo human skin comparison—Schmitz 2016

Formulation choice changed both epidermal ALA delivery and PpIX formation. The carrier, as well as the active, determines the tissue dose.

PpIX in tissue lysates (nmol/L, median), ex vivo human eyelid skin from 10 donors; redrawn from the reported data (Schmitz et al., 2016).

Maisch et al. | Exp Dermatol | 2010 | DOI: 10.1111/j.1600-0625.2009.01001.x · Schmitz et al. | Photodiagn Photodyn Ther | 2016 | DOI: 10.1016/j.pdpdt.2015.11.004

Evidence—imaging

Imaging evidence: fluorescence follows the carrier, not just the active

Schmitz 2016, Figure 2—original image

Placebo

Nanoemulsion gel

20% cream

Image labels: 3 h, 6 h and 12 h; hematoxylin & eosin; PpIX fluorescence. Columns: placebo, nanoemulsion gel, 20% cream.

H&E and PpIX fluorescence cryosections; ex vivo human eyelid skin from 10 donors.

Christiansen 2007, Figure 6—original image

Follicle/lesion-selective signal (A) vs uniform signal (B)

Measured skin-surface PpIX fluorescence: 0.5% liposomal ALA spray for 3 h without occlusion (A) vs occluded 20% ALA cream (B). The lipid carrier concentrates the signal in follicles and lesions.

de Leeuw 2010, Figure 3—original image

Split-face comparison, one day after identical IPL settings

Image labels: 0.5% 5-ALA liposomes; 20% 5-ALA cream; after IPL treatment.

Non-occluded 0.5% liposomal ALA spray (left circled area) vs occluded 20% ALA cream (right). Tolerability differs with delivery and protocol, rather than with the active alone.

Original images reproduced from the cited publications for scientific reference. Third-party trademarks appearing in the source images were neutralized in the supplied PPT. Microscopy supports localization, not quantitative depth measurement.

Schmitz et al. | Photodiagn Photodyn Ther | 2016 | DOI: 10.1016/j.pdpdt.2015.11.004 · Christiansen et al. | Lasers Surg Med | 2007 | PMID: 17457834 · de Leeuw et al. | JEADV | 2010 | DOI: 10.1111/j.1468-3083.2009.03447.x

 

Protocol design

Designing for efficacy and comfort together

Table expanded in original row order; all column labels and data are retained.

Comfort is a property of the whole protocol—formulation, incubation and illumination—not encapsulation alone.

Christiansen et al. | Lasers Surg Med | 2007 | PMID: 17457834 · Dirschka et al. | JEADV | 2019 | PMID: 30022544

Daylight photodynamic applications

Daylight as the light source: a simple, continuous protocol

Why continuous low-intensity light can remain comfortable

During two hours of daylight, PpIX is activated and photobleached almost as soon as cells synthesize it. Tissue PpIX stays at a low steady state, delivering cumulative photochemical exposure without the concentration spikes associated with treatment pain.

Protocol flexibility: seasonal natural daylight or simulated-daylight lamps that avoid weather and latitude constraints, both evaluated clinically.

Image label: assessment after 12 weeks.

Original daylight PDT treatment schematic (Wiegell et al., 2008, Figure 1). A professional clinical protocol, not consumer sun-exposure guidance.

Schematic: Wiegell et al. | Br J Dermatol | 2008 | PMID: 18294318 · Protocol: Dirschka et al. | JEADV | 2019 | PMID: 30022544 · Simulated daylight: Bai-Habelski et al. | 2021

 

Clinical evidence—daylight

Daylight PDT: comparable clearance, lower recurrence and very little pain

Values are percentages. Single-session daylight PDT; randomized intraindividual controlled phase III study in 52 patients with actinic keratoses. Non-inferiority P < 0.0001; recurrence difference P = 0.01.

1.2 vs >4

Mean maximum pain during daylight exposure (VAS 0–10), compared with reported mean values above 4 for conventional lamp-based PDT

Reading the evidence correctly

Indication: actinic keratosis, a clinical endpoint shown here as delivery-platform evidence, not cosmetic efficacy.

Carrier: a phospholipid nanoemulsion gel, related to liposomal technology, clinically demonstrating daylight-compatible ALA delivery.

Design: randomized split-face non-inferiority study; 52 randomized, 49 per protocol; gel = 10% ALA hydrochloride (approximately 7.8% free acid), versus 16% methyl aminolevulinate cream.

Dirschka et al. | J Eur Acad Dermatol Venereol | 2019 | DOI: 10.1111/jdv.15185 | PMID: 30022544

Scalp science

Follicle biology: a second home for vesicular delivery

Image labels: nanoparticle, drug; SC = stratum corneum, E = epidermis, D = dermis; dermal–epidermal junction; blood vessel.

Particle-delivery pathways at the follicle: surface film, follicular canal and deeper follicular penetration

The follicle is a living, cycling mini-organ

Dermal papilla cells at its base drive the anagen–catagen–telogen cycle. Their metabolic activity makes them a relevant target for active combinations.

Follicles bypass the barrier

The follicular canal extends into the dermis, with no mature stratum corneum in deeper regions—a natural bypass available to vesicles.

Sebum supports lipid vesicles

The sebum-rich canal is chemically compatible with phospholipid vesicles, supporting retention and release near the papilla.

This development route requires no photoactivation: the non-photodynamic track for NanoActive Alavelle™.

Scalp science

Inside the papilla: ERK/AKT signaling triggered by ALA + iron

HMOX1 (HO-1) remained unchanged. Signaling involved ERK/AKT, rather than the sometimes-assumed ALA + iron heme oxygenase pathway.

Reading the evidence correctly

A combination, not ALA alone. Cellular and follicular responses were observed with joint 5-ALA and iron exposure and cannot be attributed to ALA itself.

Models, not patients. Immortalized dermal papilla cells and ex vivo follicle organ culture are mechanistic models. Clinical endpoints require clinical studies.

Ryu et al. | FEBS Open Bio | 2026 | DOI: 10.1002/2211-5463.70230 | PMID: 41873782

Scalp science

Original data from follicle models (open access)

Phospho-kinase array—Figure 3A (original)

Image labels: Control_spot_1/2 and 5-ALA/FAC_spot_1/2. The supplied PPT image has no visible x-axis item names; none have been inferred.

Relative phosphorylation in dermal papilla cells, 1 µM 5-ALA/FAC vs control: increased kinases along the ERK/AKT axis.

Follicle organ culture—Figure 4B (original)

Image labels: D0/D5 = days 0/5; control; 5-ALA/FAC combination; increased hair length (mm). The asterisk is the original significance marker; P < 0.05 is specified in the text.

Hair-shaft elongation after five days of ex vivo human follicle organ culture, combination vs control, n = 20, P < 0.05.

Original images reproduced under CC BY 4.0 (© 2026 the authors; FEBS Open Bio / John Wiley & Sons). Results belong to the 5-ALA + FAC combination, not ALA alone, and to model systems rather than human clinical outcomes.

Ryu et al. | FEBS Open Bio | 2026;16:1527–1536 | DOI: 10.1002/2211-5463.70230 | PMID: 41873782 | Open access CC BY 4.0

Scalp science

Three levels of hair evidence: cells, follicles and humans

Table expanded in original row order; all column labels and data are retained.

What the three studies have in common

Every positive hair-related result combined ALA with an iron source or peptide partner: the combination is the active principle. None used photoactivation; this is a chemistry-and-delivery pathway, not PDT.

Ryu et al. | FEBS Open Bio | 2026 | PMID: 41873782 · Lee et al. | Ann Dermatol | 2016 | PMID: 27489425 · Morokuma et al. | Int J Dermatol | 2008 | PMID: 19126021

Product formats

Sprays and aqueous gels: built around vesicles

Leave-on spray

Forms a thin, even film without rubbing, treating the application site gently. Covers large areas and reaches the scalp through hair. Low viscosity naturally suits aqueous vesicle dispersions.

Precedent: the published liposomal ALA skin studies used spray formulations.

Aqueous gel

Provides longer residence at precisely targeted sites, with accurate, repeatable dosing.

A water-based gel keeps hydrophilic ALA in a compatible environment while vesicles handle delivery.

Formulation guardrails from the stability literature

pH approximately 5–6. Balance ALA chemical stability with skin compatibility.

Protect from oxygen and light. Packaging is part of the stability strategy.

Test chemistry, not just colloids. Track ALA content and pyrazine condensation impurities; size and PDI alone cannot establish active integrity.

Watch cosolvent levels. Published ALA nanoemulsion data associate excess polyols with impurity formation.

Bunke et al. | J Pharm Sci | 2000 | PMID: 10980508 · Christiansen et al. | Lasers Surg Med | 2007 | PMID: 17457834

Scalp science

Scalp-care concepts: the non-photodynamic route

Leave-on scalp serum

A vesicle dispersion targeting the follicular canal, designed for overnight residence near the papilla’s “doorway.”

Daily nourishing mist

A lightweight aqueous formula provides broad, even coverage through hair, using a format with published precedent in ALA scalp applications.

Pretreatment gel

Controlled, timed contact before rinsing, for consumers who prefer a defined exposure window.

Combination-first design

Published hair-study results belong to ALA combined with iron or peptide partners. Formulate the concept around the combination, not ALA alone.

Concepts, not specifications. These are development directions for brand partners. Concentration, packaging and shelf life depend on each partner’s formulation and stability studies. None of these concepts involves photoactivation.

Basis: Ryu et al. | FEBS Open Bio | 2026 | PMID: 41873782 · Lee et al. | Ann Dermatol | 2016 | PMID: 27489425 · Morokuma et al. | Int J Dermatol | 2008 | PMID: 19126021

Professional applications

Photoactivated formats: formulation, light and evidence

Table expanded in original row order; all column labels and data are retained.

How Purui Biomedical positions this evidence

These are professional protocols studied in clinical settings. For NanoActive Alavelle™, they provide platform evidence that low-concentration ALA in engineered carriers works under real illumination, rather than cosmetic product claims.

Piccioni et al. | J Dermatolog Treat | 2011 | PMID: 21801099 · Yeung et al. | Dermatol Surg | 2011 | PMID: 21414073 · Dirschka et al. | JEADV | 2019 | PMID: 30022544 · Bai-Habelski et al. | Photodiagn Photodyn Ther | 2021 | DOI: 10.1016/j.pdpdt.2021.102692

Route-specific science

Another route: lessons from oral ALA pharmacokinetics

≈60%

Oral 5-ALA bioavailability in healthy volunteers

≈45 min

Elimination half-life—rapid systemic clearance

Rapid absorption, onset and clearance: kinetics fundamentally different from a topical leave-on product.

Route-specific data cannot be transferred across routes

No cross-route extrapolation. Oral bioavailability and clearance do not establish topical penetration, and vesicular skin-delivery data do not establish oral exposure.

A separate development program is required. Any oral concept based on ALA chemistry needs its own regulatory and clinical pathway. The PURISOME® platform discussed here targets topical delivery.

Dalton et al. | J Pharmacol Exp Ther | 2002 | DOI: 10.1124/jpet.301.2.507 | PMID: 11961050

Formulator’s checklist

Six decisions that determine whether ALA survives and performs

Table expanded in original row order; all column labels and data are retained.

Elfsson et al. | Eur J Pharm Sci | 1999 | PMID: 9845784 · Bunke et al. | J Pharm Sci | 2000 | PMID: 10980508 · Dalton et al. | J Pharmacol Exp Ther | 2002 | PMID: 11961050

Platform overview

One platform, four evidence-informed directions

Table expanded in original row order; all column labels and data are retained.

Each evidence label corresponds to a full citation in the reference section. NanoActive Alavelle™ product specifications are provided by Purui Biomedical under project-specific agreements.

Closing perspective

One molecule, one platform, multiple thoughtfully designed formats.

01 Stabilize the chemistry

Control pH and oxygen; demonstrate integrity by testing ALA and its condensation impurities.

02 Deliver where it matters

Flexible phospholipid vesicles carry hydrophilic ALA across the barrier and along the follicular bypass.

03 Design for comfort

Low loading, short contact and gentle illumination: comfort is a protocol property.

Purui Biomedical Technology Co., Ltd.

NanoActive Alavelle™ Aminolevulinic Acid Nanoliposomes—powered by PURISOME® Liposome Technology

Innovation for Health and Beauty

Regulatory statement: finished products containing NanoActive Alavelle™ must comply with the laws and regulations of the countries or regions where they are manufactured and sold. The brand is responsible for final-product regulatory compliance.

References

References (Part 1 of 2)

01 · Rick K, Sroka R, Stepp H, Kriegmair M, Huber RM, Jacob K, Baumgartner R. Pharmacokinetics of 5-aminolevulinic acid-induced protoporphyrin IX in skin and blood. J Photochem Photobiol B. 1997;40(3):313–319. DOI: 10.1016/S1011-1344(97)00076-6 · PMID: 9372622

02 · Elfsson B, Wallin I, Eksborg S, Rudaeus K, Ros AM, Ehrsson H. Stability of 5-aminolevulinic acid in aqueous solution. Eur J Pharm Sci. 1999;7(2):87–91. DOI: 10.1016/S0928-0987(98)00098-8 · PMID: 9845784

03 · Bunke A, Zerbe O, Schmid H, Burmeister G, Merkle HP, Gander B. Degradation mechanism and stability of 5-aminolevulinic acid. J Pharm Sci. 2000;89(10):1335–1341. PMID: 10980508

04 · Dalton JT, Yates CR, Yin D, Straughn A, Marcus SL, Golub AL, Meyer MC. Clinical pharmacokinetics of 5-aminolevulinic acid in healthy volunteers and patients at high risk for recurrent bladder cancer. J Pharmacol Exp Ther. 2002;301(2):507–512. DOI: 10.1124/jpet.301.2.507 · PMID: 11961050

05 · Christiansen K, Bjerring P, Troilius A. 5-ALA for photodynamic photorejuvenation — optimization of treatment regime based on normal-skin fluorescence measurements. Lasers Surg Med. 2007;39(4):302–310. PMID: 17457834

06 · Morokuma Y, Yamazaki M, Maeda T, Yoshino I, Ishizuka M, Tanaka T, Ito Y, Tsuboi R. Hair growth stimulatory effect by a combination of 5-aminolevulinic acid and iron ion. Int J Dermatol. 2008;47(12):1298–1303. PMID: 19126021

07 · Bjerring P, Christiansen K, Troilius A, Bekhor P, de Leeuw J. Skin fluorescence controlled photodynamic photorejuvenation (wrinkle reduction). Lasers Surg Med. 2009;41(5):327–336.

08 · Maisch T, Santarelli F, Schreml S, Babilas P, Szeimies RM. Fluorescence induction of protoporphyrin IX by a new 5-aminolevulinic acid nanoemulsion used for photodynamic therapy in a full-thickness ex vivo skin model. Exp Dermatol. 2010;19(8):e302–e305. DOI: 10.1111/j.1600-0625.2009.01001.x · PMID: 19845760

09 · Oh EK, Jin SE, Kim JK, Park JS, Park Y, Kim CK. Retained topical delivery of 5-aminolevulinic acid using cationic ultradeformable liposomes for photodynamic therapy. Eur J Pharm Sci. 2011;44(1–2):149–157. DOI: 10.1016/j.ejps.2011.07.003 · PMID: 21782942

10 · Piccioni A, Fargnoli MC, Schoinas S, Suppa M, Frascione P, Ginebri A, Chimenti S, Peris K. Efficacy and tolerability of 5-aminolevulinic acid 0.5% liposomal spray and intense pulsed light in wrinkle reduction of photodamaged skin. J Dermatolog Treat. 2011;22(5):247–253. DOI: 10.3109/09546634.2011.590791 · PMID: 21801099

References

References (Part 2 of 2)

11 · Yeung CK, Shek SY, Yu CS, Kono T, Chan HH. Liposome-encapsulated 0.5% 5-aminolevulinic acid with intense pulsed light for the treatment of inflammatory facial acne: a pilot study. Dermatol Surg. 2011;37(4):450–459. DOI: 10.1111/j.1524-4725.2011.01929.x · PMID: 21414073

12 · Lee WJ, et al. Efficacy of a complex of 5-aminolevulinic acid and glycyl-histidyl-lysine peptide on hair growth. Ann Dermatol. 2016;28(4). PMID: 27489425

13 · Schmitz L, Novak B, Hoeh AK, Luebbert H, Dirschka T. Epidermal penetration and protoporphyrin IX formation of two different 5-aminolevulinic acid formulations in ex vivo human skin. Photodiagnosis Photodyn Ther. 2016;14:40–46. DOI: 10.1016/j.pdpdt.2015.11.004 · PMID: 26607556

14 · Ryu et al. Combined 5-aminolevulinic acid and ferric ammonium citrate treatment promotes hair follicle growth by activating dermal papilla cells. FEBS Open Bio. 2026. DOI: 10.1002/2211-5463.70230 · PMID: 41873782

15*Reinhold U. Review of a 7.8% ALA nanoemulsion gel for the photodynamic treatment of mild-to-moderate actinic keratosis. Future Oncol. 2017;13(27):2413–2428. DOI: 10.2217/fon-2017-0247 · PMID: 28805092

16*Dirschka T, Ekanayake-Bohlig S, Dominicus R, et al. Randomized, intraindividual, non-inferiority phase III study of daylight photodynamic therapy comparing a 7.8% ALA nanoemulsion gel with MAL cream in actinic keratosis. J Eur Acad Dermatol Venereol. 2019;33(2):288–297. DOI: 10.1111/jdv.15185 · PMID: 30022544

17*Bai-Habelski JC, Medrano K, Palacio A, Reinhold U. Prospective study of simulated daylight photodynamic therapy with an indoor daylight-reproducing system and a 7.8% ALA nanoemulsion gel in actinic keratosis. Photodiagnosis Photodyn Ther. 2021;37:102692. DOI: 10.1016/j.pdpdt.2021.102692

18 · Park MY, Sohn S, Lee ES, Kim YC. Photorejuvenation induced by 5-aminolevulinic acid photodynamic therapy in patients with actinic keratosis: a histologic analysis. J Am Acad Dermatol. 2010;62(1):85–95. DOI: 10.1016/j.jaad.2009.06.025 · PMID: 19926165

19de Leeuw J, van der Beek N, Bjerring P, Neumann HA. Photodynamic therapy of acne vulgaris using 5-aminolevulinic acid 0.5% liposomal spray and intense pulsed light in combination with topical keratolytic agents. J Eur Acad Dermatol Venereol. 2010;24(4):460–469. DOI: 10.1111/j.1468-3083.2009.03447.x

20 · Wiegell SR, Haedersdal M, Philipsen PA, Eriksen P, Enk CD, Wulf HC. Continuous activation of PpIX by daylight is as effective as and less painful than conventional photodynamic therapy for actinic keratoses; a randomized, controlled, single-blinded study. Br J Dermatol. 2008;158(4):740–746. DOI: 10.1111/j.1365-2133.2008.08450.x · PMID: 18294318

*Descriptive titles are used to avoid third-party trademarks in this document. Each publication can be identified uniquely by its DOI/PMID.

PuriActives® TocoPhos™ 生育酚磷酸酯钠

PuriActives® TocoPhos™Sodium Tocopheryl Phosphate

PRODUCT & BRAND

PuriActives® TocoPhos™ Sodium Tocopheryl Phosphate

PuriPharm Co., Ltd.

Vitamin E, reimagined for skin and scalp.

INCI: SODIUM TOCOPHERYL PHOSPHATE

A phosphorylated vitamin E active with aqueous compatibility and biological activation in skin, supported by peer-reviewed studies on oxidative-stress protection and moisturization.

INGREDIENT OPPORTUNITY

One molecule, four formulation-relevant advantages

DESIGNED FOR AQUEOUS COMPATIBILITY

A 6-O-phosphate group masks the oxidation-sensitive phenolic hydroxyl, with sodium counterions converting an oily antioxidant into a water-dispersible powder for serums, essences and gels. Kato et al. 2011; Zingg 2018.

ACTIVATION AT THE SITE OF ACTION

After uptake, cellular phosphatases hydrolyze the phosphate to release active α-tocopherol within cells. Hydrolysis was not observed in the culture medium itself. Nishio et al. 2011; Saleh et al. 2021.

DUAL STRESS PROTECTION

In human keratinocytes, the sodium salt suppressed UVB-induced reactive nitrogen species (RNS) and reduced prostaglandin E2 (PGE2) responses to UVB, IL-1β and peroxide challenges. Nakama et al. 2009; Kato et al. 2011.

MOISTURE AND BARRIER SUPPORT

Topical treatment increased stratum corneum ceramides through serine palmitoyltransferase (SPT) and keratinocyte-differentiation pathways, improving moisture retention in hairless mouse skin. Kato & Takahashi 2012.

Phosphorylated vitamin E connects skin-defense research, moisturization mechanisms and contemporary formulation opportunities.

FORMULATION CHALLENGES

Why rethink vitamin E?

THE CLASSIC MOLECULE AND ITS FORMULATION CHALLENGES

OXIDATION SENSITIVITY

The phenolic hydroxyl is α-tocopherol’s antioxidant site and a key site of oxidation. Oxidation can deplete its activity.

AN OIL IN AN AQUEOUS WORLD

A viscous, hydrophobic liquid requires solubilization or emulsification for aqueous serums, essences and scalp formats.

ESTERS SOLVE ONLY PART OF THE PROBLEM

Tocopheryl acetate is stable but remains oily and depends on skin esterases. It produced much less tocopherol than the phosphate salt after 24 hours in a reconstructed human skin model. Kato et al. 2011, Figure 2A.

WHAT PHOSPHATE CHEMISTRY CHANGES

PROTECTED PHENOLIC HYDROXYL

The 6-O-phosphate masks the oxidizable hydroxyl until enzymatic hydrolysis. Kato et al. 2011.

A WATER-COMPATIBLE SALT

Sodium counterions yield a powder suitable for incorporation into the aqueous phase.

ACTIVATION AFTER UPTAKE

Cellular phosphatases release α-tocopherol after uptake, rather than in the culture medium. Nishio et al. 2011.

This chemistry supports development of water-based serums, essences, gels and leave-on scalp products.

MOLECULAR IDENTITY

A chromanol core with distinct functional regions

VITAMIN E FAMILY STRUCTURES

Adapted from Kato et al. 2011, Figure 1. Compound 1 is disodium tocopheryl phosphate, the TocoPhos™ active, shown with α-tocopherol and tocopheryl acetate.

IONIZATION OF THE PHOSPHATE GROUP

Adapted from Saleh et al. 2020, Figure 1. The phosphate undergoes two ionization steps, with pKa values of approximately 1.8 and 6.7. A predominantly dianionic state is described near pH 7.4.

CHROMANOL HEAD: ANTIOXIDANT CORE

The 6-position phenolic hydroxyl captures radicals in vitamin E; phosphorylation protects this site.

6-O-PHOSPHATE: AN IONIZABLE HANDLE

Ionization depends on pH. Near pH 7.4, the predominantly dianionic form supports water affinity while the phosphate protects the phenolic hydroxyl until hydrolysis.

SODIUM SALT: THE INCI-DEFINED FORM

Supplied as Sodium Tocopheryl Phosphate, a water-dispersible powder. The free acid has formula C29H51O5P, PubChem CID 94493.

PHYTYL TAIL: LIPID ANCHOR

After hydrolysis, the hydrophobic tail anchors released α-tocopherol in membranes, where it intercepts lipid peroxyl radicals.

Near pH 7.4, this anionic amphiphile self-associates into approximately 9 nm aggregates, with a critical aggregation concentration (CAC) of approximately 4.2 mM. At pH 9 it is monomeric, providing a formulation variable. Saleh et al. 2020.

VITAMIN E OPTIONS

Choosing the appropriate vitamin E form

Conventional forms and formulation comparison

Corresponding phosphate-salt properties

*Reconstructed human skin model: tocopherol accumulation after topical treatment, Kato et al. 2011, Figure 2A. General chemistry: Zingg 2018. Photostability of the phosphorylated form: Saleh et al. 2021.

Different systems call for different tools. The phosphate salt provides a route for aqueous and scalp-oriented formats.

UPTAKE · BIOCONVERSION · ANTIOXIDANT ACTION

Delivered as phosphate, activated as vitamin E

ACTIVATION PATHWAY

1 APPLICATION: an aqueous formulation deposits sodium tocopheryl phosphate at the skin surface.

2 UPTAKE: keratinocytes internalize the phosphorylated active.

3 BIOCONVERSION: cellular phosphatases hydrolyze the phosphate, releasing α-tocopherol.

4 ANTIOXIDANT ACTION: α-tocopherol associates with membranes and intercepts lipid peroxyl radicals.

• Deuterium tracing showed hydrolysis of α-TP to α-tocopherol in cells and mice, but not in culture medium, with lower plasma and liver lipid peroxidation. Nishio et al. 2011.

• In reconstructed human skin, tocopherol accumulation was approximately 190 nmol/g tissue at 24 hours with the phosphate salt; acetate remained near baseline. Kato et al. 2011, Figure 2A.

EVIDENCE: INTRACELLULAR BIOCONVERSION

HaCaT keratinocytes were incubated with 133 µg/mL α-TP. Intracellular α-TP increased, and α-tocopherol (α-T) appeared in cell lysates at 2–24 hours, supporting uptake and enzymatic hydrolysis. Adapted from Saleh et al. 2021, Figure 8.

Saleh et al. Scientific Reports. 2021. doi:10.1038/s41598-021-01299-y

STRESS BIOLOGY

Addressing oxidative and nitrosative stress

PUBLISHED EVIDENCE

UVB AND RNS IN HUMAN KERATINOCYTES

Real-time fluorescence imaging showed UVB-triggered RNS generation involving neuronal nitric oxide synthase (nNOS). Sodium dl-α-tocopheryl phosphate suppressed this response. Nakama et al. 2009.

SOOTHING-RELATED SIGNALS

In UVB-exposed NHEK, the sodium salt reduced Cox-2 mRNA by 33–51% at 0.5 µM, inhibited p38 MAPK phosphorylation and lowered PGE2. Kato et al. 2011.

MODEL CONTEXT MATTERS

Intact α-TP is a weak radical scavenger in cell-free DPPH / ORAC assays. Cellular protection follows bioconversion to α-tocopherol, making the experimental model essential to interpretation. Saleh et al. 2021, Figure 7.

KEY TERMS

ROS: reactive oxygen species. RNS: reactive nitrogen species. nNOS: neuronal nitric oxide synthase. PGE2: prostaglandin E2. NHEK: normal human epidermal keratinocytes.

EVIDENCE FOCUS: UV STRESS

Pretreated keratinocytes withstand high-dose UVA1 stress

HaCaT keratinocytes were pretreated for 24 hours before UVA1 exposure. Viability was measured by Alamar Blue 24 hours later. Mean ± SD; *p < 0.05 and **p < 0.01 versus irradiated control. From Saleh et al. 2021, Figure 5.

Saleh et al. Scientific Reports. 2021. doi:10.1038/s41598-021-01299-y

VIABILITY AFTER 226 J/cm² UVA1

88% versus 70% cell viability

80 µM α-TP pretreatment versus irradiated control. α-Tocopherol at the same concentration provided no significant protection in this model.

INTRACELLULAR ROS AFTER 57 J/cm²

24.1% lower ROS versus control

100 µM α-TP; H2DCFDA measurement within 2 hours after irradiation. α-Tocopherol reduced ROS by 23.9%.

Protection coincided with phosphatase-mediated conversion to α-tocopherol. Intact α-TP was weak in cell-free assays but protective in cells. The phosphorylated form also had a higher LD50 in this model: 1676 versus 1070 µM.

Additional UVB evidence: suppression of UVB-induced RNS in human keratinocytes. Nakama et al. 2009. J SCCJ 43(1):19. doi:10.5107/sccj.43.19.

MOISTURIZATION MECHANISM

Supporting the skin’s ceramide-production machinery

Ceramides are part of the lipid mortar of the stratum corneum. In keratinocytes, sodium tocopheryl phosphate acts on upstream processes involved in their synthesis.

In NHEK, the sodium salt increased intracellular ceramides to approximately 1.8-fold at 50 µM (*), SPTLC2 expression to approximately 2.2-fold (**), differentiation markers and intracellular Ca²⁺. Kato & Takahashi 2012.

WHY THIS MATTERS TO FORMULATORS

• Support for endogenous ceramide synthesis complements formulations that directly supply ceramides.

• Differentiation markers such as TG1, involucrin and loricrin inform barrier-care positioning.

• Supporting literature reports vitamin E upregulation of transglutaminase-1 and PPARγ in human keratinocytes. De Pascale et al. 2006.

Kato & Takahashi. Bioorg Med Chem. 2012;20(12):3837–3842. PMID 22579618. The schematic synthesizes the study pathway. Fold changes are approximate readings from the original figures. SPT: serine palmitoyltransferase. TG1: transglutaminase-1. CK10: cytokeratin 10. PPARγ: peroxisome proliferator-activated receptor γ.

EVIDENCE FOCUS: MOISTURIZATION

From keratinocyte signaling to a more hydrated barrier

IN VITRO: HUMAN KERATINOCYTES, NHEK

▲ Intracellular ceramides: approximately 1.8-fold versus control at 50 µM (*).

▲ SPT genes: SPTLC2 mRNA approximately 2.2-fold (**); SPTLC1 also increased (*).

▲ Differentiation markers TGM1, KRT10, IVL and LOR: approximately 2.2–3.3-fold (*/**).

▲ Intracellular Ca²⁺: significantly higher at 50–75 µM (*), consistent with differentiation signaling.

Original figure, panel 4A: intracellular NHEK ceramides increase with dose at 0 / 10 / 50 µM, measured as µg/mg protein.

IN VIVO: HAIRLESS MICE, TOPICAL 1% / 2% FOR 4 WEEKS

▲ Stratum corneum ceramides: approximately 4.8–5.0 µg/cm² in the 1% (*) and 2% (**) groups, versus approximately 3 µg/cm² in untreated and placebo groups.

▲ Hygroscopicity at 30 seconds: higher with both 1% (*) and 2% (**) versus untreated / placebo.

▲ Moisture retention at 60 seconds: significantly higher with both concentrations (*).

These findings link improved stratum corneum hydration with endogenous lipid processes.

Original figure, panel 2B: stratum corneum hygroscopicity at 30 seconds and moisture retention at 60 seconds; untreated / placebo / 1% / 2%.

Kato & Takahashi. Bioorg Med Chem. 2012;20(12):3837–3842. doi:10.1016/j.bmc.2012.04.029. PMID 22579618. Panels 2B and 4A are excerpts from the paper. Fold changes are approximate readings from original axes; * / ** reproduce the authors’ significance notation.

EVIDENCE FOCUS: SKIN COMFORT

Modulating inflammatory cascades in stressed keratinocytes

NHEK were pretreated with the sodium salt at 0.1–2 µM for 24 hours before UVB, IL-1β, tBHP or H2O2 challenge. PGE2 was measured in culture medium. Kato et al. 2011, Figure 3.

Kato et al. Bioorg Med Chem. 2011;19(21):6348–6355. doi:10.1016/j.bmc.2011.08.067

PGE2 REDUCTION VERSUS STIMULATED CONTROL

UVB: 44 / 65 / 69% at 0.1 / 0.5 / 2 µM.

tBHP: 74 / 87 / 90%; IL-1β: 41 / 58 / 57%.

H2O2: approximately 50%; UVB alone increased PGE2 approximately fivefold.

The acetate was weaker, and α-tocopherol had little effect at these concentrations.

CELL DEATH UNDER OXIDATIVE STRESS

Redrawn from US20090104258A1, Example 1. Keratinocytes, 1 mM H2O2 for 24 hours; flow cytometry. The y-axis is the percentage of apoptotic cells.

Example 2 of the same patent publication: α-TP at 1 µg/mL increased large stem-cell-derived colonies by 104% in a clonogenic assay under oxidative stress.

DELIVERY SCIENCE

The vehicle influences delivery to viable skin

α-TP FLUX ACROSS A SYNTHETIC MEMBRANE

Redrawn from Saleh et al. 2023: steady-state flux of 2% α-TP from four vehicles across a synthetic membrane.

In human skin, the emulsion outperformed the gel-like system:

3× viable-layer deposition at 3 hours and 5× at 24 hours.

Human-skin flux: 328.6 versus 175.2 µg/cm²/h. Cell-free DPPH activity of the delivered dose was higher: 73% versus 46%.

SKIN DEPOSITION: pH 7.4 VERSUS α-TOCOPHEROL

Porcine skin, 3 hours, infinite dose: α-TP at pH 7.4 reached approximately 506 ± 296 µg in the stratum corneum and 170 ± 29 µg in the epidermis. From Saleh et al. 2020, Figure 5. The source slide also describes approximately 8-fold / 4-fold differences; the comparison basis requires checking against the original paper.

At pH 7.4, α-TP forms approximately 9 nm aggregates that fuse with stratum corneum lipids in cryo-electron microscopy. At pH 9, monomer deposition is lower. Formulation pH therefore affects aggregation and skin interactions.

Saleh et al. Int J Pharm. 2023. doi:10.1016/j.ijpharm.2023.122781. PMID 36849039. Saleh et al. Int J Pharm. 2020. doi:10.1016/j.ijpharm.2020.120000.

SKINCARE APPLICATION PORTFOLIO

Five formats with a shared evidence base

Formats and rationale

Corresponding evidence anchors

SCALPIFICATION

The scalp is skin with additional challenges

The scalp shares keratinocytes, a ceramide barrier and UV / pollution exposure with facial skin, together with dense follicles and sebum.

SHARED STRESS BIOLOGY

UV reaches the scalp surface. ROS / RNS responses documented in keratinocytes inform this application rationale. Nakama 2009; Saleh 2021.

SHARED HYDRATION MACHINERY

The ceramide barrier also matters to scalp dryness and tightness. Kato & Takahashi 2012.

SHARED COMFORT-RELATED SIGNALS

PGE2-related stress pathways provide a basis for conceptual extension to scalp comfort. Kato et al. 2011.

The scalp is a development extension for TocoPhos™. PuriPharm technical and application teams support joint scalp-formulation projects.

SCALP PROTECTION AND COMFORT

Three scalp-care opportunities

FOLLICULAR-ENVIRONMENT PROTECTION

The scalp surface is UV-exposed skin. Keratinocyte findings on UVA1 survival and UVB-triggered RNS provide a rationale for leave-on antioxidant scalp care. Nakama et al. 2009; Saleh et al. 2021.

HYDRATION BALANCE AND BARRIER SUPPORT

SPT-related ceramide synthesis and improved stratum corneum moisture retention inform concepts for dry, tight-feeling scalps. Kato & Takahashi 2012.

COMFORT FOR STRESSED SCALPS

PGE2 / Cox-2 / p38 modulation and reduced stress-induced keratinocyte death provide a rationale for comfort-oriented products. Kato et al. 2011; US20090104258A1, Example 1.

All three are development opportunities extrapolated from published epidermal evidence. Work with PuriPharm Co., Ltd. to translate them into scalp-care products.

HAIRCARE FORMATS

TocoPhos™ in scalp and haircare formulations

PRACTICAL FORMULATION

Six practical principles for phosphate formulations

SOLUBILITY VERSUS pH

Adapted from Saleh et al. 2020, Figure 1. α-TP solubility rises with pH alongside changes in aggregation.

Contact PuriPharm technical and application teams for grade-specific use levels, processing-temperature limits, shelf life and full technical documentation.

Saleh et al. Int J Pharm. 2020. doi:10.1016/j.ijpharm.2020.120000. Saleh et al. Int J Pharm. 2023. doi:10.1016/j.ijpharm.2023.122781.

SKINCARE CONCEPT GALLERY

Three concepts to start development

FORMULATION CONCEPT

DAILY DEFENSE ANTIOXIDANT SERUM

Aqueous gel serum · Daily leave-on use

Suggested ingredients: Niacinamide · Panthenol · Glycerin

Aqueous delivery of a biologically activated antioxidant: keratinocyte uptake and conversion to α-tocopherol provide a rationale for ROS / RNS stress care.

Evidence: Nishio 2011; Saleh 2021; Nakama 2009.

FORMULATION CONCEPT

CERAMIDE-SUPPORTING MOISTURIZER

Oil-in-water cream · Daily moisturization

Suggested ingredients: Ceramide NP · Glycerin · Squalane

Two complementary routes: direct ceramide supplementation and support for endogenous SPT-related synthesis.

Evidence: Kato & Takahashi 2012.

FORMULATION CONCEPT

AFTER-SUN CARE LOTION

Light emulsion · After-sun comfort

Suggested ingredients: Sodium Ascorbyl Phosphate · Bisabolol · Betaine

A reported combination with magnesium ascorbyl phosphate inhibited PGE2 more than either ingredient alone. This informs a vitamin C phosphate combination concept; the proposed sodium derivative is not the identical tested combination.

Evidence: Kato 2011, Figure 6; Nakama 2009.

These concepts have published mechanistic evidence anchors. Contact PuriPharm Co., Ltd. for formulation collaboration.

SCALP AND HAIRCARE CONCEPT GALLERY

Scalp-first formats informed by skin science

FORMULATION CONCEPT

ANTIOXIDANT SCALP SERUM

Aqueous leave-on serum · Daily use

Suggested ingredients: Niacinamide · Panthenol · Glycerin

A scalp-surface serum with biologically activated antioxidant positioning, derived from epidermal UV-stress evidence.

Evidence: Nakama 2009; Saleh 2021.

FORMULATION CONCEPT

LIGHT SCALP COMFORT EMULSION

Fluid emulsion · Leave-on comfort

Suggested ingredients: Bisabolol · Betaine · Glycerin

Emulsion vehicles provided greater viable-skin deposition in the cited comparison. PGE2 modulation informs a scalp-comfort concept.

Evidence: Saleh 2023; Kato 2011.

FORMULATION CONCEPT

MOISTURIZING SCALP MASK

Cream mask · Weekly intensive care

Suggested ingredients: Ceramide NP · Butyrospermum Parkii (Shea) Butter

Longer contact is consistent with a ceramide-synthesis rationale for dry, tight-feeling scalps.

Evidence: Kato & Takahashi 2012.

Develop a coordinated scalp-care range, from serums to masks, with PuriPharm Co., Ltd.

FOUR KEY POINTS

Why PuriActives® TocoPhos™?

PROTECTED AND BIOLOGICALLY AVAILABLE

Phosphate chemistry protects the antioxidant site, with cellular phosphatases releasing α-tocopherol after uptake.

EVIDENCE FROM RELEVANT MODELS

Human keratinocytes, reconstructed skin, in vivo barrier models and human skin delivery studies provide traceable evidence.

FORMULATION DEVELOPMENT SUPPORT

Aqueous-phase use, published vehicle and pH data, and preservative-testing evidence from an emulsion prototype.

ONE ACTIVE, TWO CARE AREAS

Skin defense and moisturization, alongside scalp-care concepts extrapolated from the same evidence base.

Vitamin E, reimagined for formulation development.

Work with us on your next skincare or scalp-care concept.

PuriPharm Co., Ltd. · Technical and Application Team

SCIENTIFIC REFERENCES

Scientific references

1. Nakama M. et al. Inhibitory effect of sodium dl-α-tocopheryl-6-O-phosphate on UVB-induced reactive nitrogen species in human keratinocytes. J Soc Cosmet Chem Jpn 43(1):19–25, 2009. doi:10.5107/sccj.43.19

2. Kato E., Sasaki Y., Takahashi N. Sodium dl-α-tocopheryl-6-O-phosphate inhibits PGE2 production in keratinocytes induced by UVB, IL-1β and peroxidants. Bioorg Med Chem 19(21):6348–6355, 2011. doi:10.1016/j.bmc.2011.08.067. PMID 21945458.

3. Kato E., Takahashi N. Improvement by sodium dl-α-tocopheryl-6-O-phosphate treatment of moisture-retaining ability in stratum corneum through increased ceramide levels. Bioorg Med Chem 20(12):3837–3842, 2012. doi:10.1016/j.bmc.2012.04.029. PMID 22579618.

4. Nishio K. et al. α-Tocopheryl phosphate is hydrolyzed to α-tocopherol in cells and in vivo. Free Radic Biol Med 50(12):1794–1800, 2011. PMID 21443945.

5. Saleh M. et al. Tocopheryl phosphate in keratinocyte UV-stress models. Scientific Reports 11:22400, 2021. doi:10.1038/s41598-021-01299-y

6. Gianello R. et al. α-Tocopheryl phosphate: chemistry and biological activity. Free Radic Biol Med 39(7):970–976, 2005. PMID 16140216.

7. Nakayama S. et al. Protective effect of α-tocopheryl phosphate against UVB-induced damage in cultured mouse skin. J Invest Dermatol 121:406–411, 2003.

8. De Pascale M.C. et al. Vitamin E upregulates transglutaminase-1 and PPARγ in human keratinocytes. Arch Biochem Biophys 447:97–106, 2006.

9. Zingg J.-M. Vitamin E: regulatory role beyond antioxidant activity. Adv Food Nutr Res 83:311–363, 2018.

10. Ghayour-Mobarhan M. et al. Tocopheryl phosphate: a review of biological properties. J Diet Suppl, 2014. doi:10.3109/19390211.2014.952859

11. Ogru E. et al. Vitamin E phosphate: an endogenous form of vitamin E. Free Radic Res, 2003.

FORMULATION AND PATENT REFERENCES

Formulation and patent references

12. Saleh M. et al. Ionization, pH-dependent solubility, self-association and skin deposition of α-tocopheryl phosphate. Int J Pharm 594:120000, 2020. doi:10.1016/j.ijpharm.2020.120000

13. Saleh M. et al. Vehicle-dependent delivery of α-tocopheryl phosphate to viable skin. Int J Pharm 636:122781, 2023. PMID 36849039 · doi:10.1016/j.ijpharm.2023.122781

14. Patent publication US20090104258A1 (published 2009), cited by publication number and examples: Example 1 (oxidative-stress-induced keratinocyte apoptosis, flow cytometry) and Example 2 (clonogenic assay; large stem-cell-derived colonies +104%).

15. Gavin A. et al. Tocopheryl phosphate mixture (TPM) as a skin-delivery enhancer for co-formulated actives. Drug Deliv Transl Res, 2016. doi:10.1007/s13346-016-0331-x

16. Mozafari M. et al. Tocopheryl phosphate-based delivery systems (review). Int J Transl Res.

NanoActive EGCG 纳米脂质体

NanoActive EGCGLiposomal Epigallocatechin Gallate

PRODUCT & BRAND

NanoActive EGCG · Nanoliposomes

Powered by PURISOME® FlexVes™ Liposome Technology

PuriPharm Co., Ltd. · NanoActive platform ingredient

PRODUCT PLATFORM

One catechin platform, multiple formulation opportunities

EGCG is one of the most studied polyphenols in skin biology, but its practical formulation value depends on protection and delivery.

NanoActive EGCG combines this multifunctional active with liposomal delivery across five evidence-informed skin and scalp development areas.

SKIN

ANTIOXIDANT DEFENSE

Resilience under UV and urban environmental stress.

PHOTOAGING-RELATED MATRIX PROTECTION

Support for collagen-matrix signaling and youthful skin texture.

SEBUM BALANCE AND BLEMISH-PRONE SKIN

Sebocyte lipid biology supported by clinical lesion-count evidence.

A MORE EVEN-TONED APPEARANCE

Melanogenesis signaling rationale from cell studies.

SCALP AND FOLLICLES

SCALP COMFORT AND FOLLICULAR VITALITY

Evidence from dermal papilla cells and human follicle organ culture.

Each development area is based on the scientific literature cited in its corresponding section.

KEY ACTIVE

The active behind the platform

Epigallocatechin gallate (EGCG): 2D structure, PubChem CID 65064.

ACTIVE INCI

EPIGALLOCATECHIN GALLATE

MOLECULAR FORMULA: C22H18O11 · MOLAR MASS: 458.37 g/mol

BOTANICAL SOURCE: the principal catechin in green tea (Camellia sinensis), formed by esterification of a flavan-3-ol with gallic acid.

STRUCTURE–ACTIVITY RELATIONSHIP: eight phenolic hydroxyl groups support radical scavenging but also confer oxidation sensitivity.

PRODUCT POSITIONING

NanoActive EGCG presents the catechin in a liposomal format built on PuriPharm’s PURISOME® platform to protect the active and support delivery to skin.

The INCI shown identifies the active ingredient. Refer to product technical documentation for the complete composition of the liposomal dispersion.

Structure source: PubChem CID 65064, NIH National Library of Medicine.

FORMULATION RATIONALE

Formulation determines EGCG performance

EGCG IN SOLUTION

DEGRADATION DRIVERS

Oxygen and light

Higher temperature

Neutral to alkaline pH

Vehicle and ionic environment

Oxidation and degradation of catechins in solution

IMPLICATIONS FOR FORMULATORS

Protect the active from oxygen, light and heat during processing and storage.

Design the vehicle and pH carefully.

Consider encapsulation to protect the catechin before use.

Design a delivery route to relevant skin compartments.

EGCG is valuable but chemically vulnerable. Solution studies show that pH, temperature and vehicle affect how much intact EGCG remains available, providing the rationale for protection and delivery engineering.

Proniuk S, Liederer BM, Blanchard J. J Pharm Sci. 2002;91(1):111–116. DOI: 10.1002/jps.10009. PMID: 11782902.

DELIVERY TECHNOLOGY

Powered by PURISOME® FlexVes™ Liposome Technology

EGCG

Skin-compatible phospholipid bilayer vesicles

Schematic, not to scale. Refer to PuriPharm technical documentation for the actual structure.

1 PROTECT VULNERABLE ACTIVES

Protect oxidation- and degradation-sensitive ingredients such as EGCG to support shelf-life quality.

2 SUPPORT LOCAL SKIN DELIVERY

Enhance stratum corneum penetration and the bioavailability of encapsulated actives.

3 SUSTAINED AND CONTROLLED RELEASE

Extend release, with a design rationale for reducing irritation risk.

4 FORMULATION COMPATIBILITY

Support compatibility and skin feel in leave-on and rinse-off systems.

All NanoActive products use the PURISOME® platform, drawing on PuriPharm’s more than ten years of nanodelivery R&D and industrial production experience.

PURISOME® platform source: PuriPharm Co., Ltd. brand documentation, V1.0 (2026).

DELIVERY RATIONALE: PUBLISHED RESEARCH

Delivery research informs formulation design

PUBLISHED FIGURE: SKIN DEPOSITION OF EGCG (µg/cm²)

Reproduced from Li et al. 2022, Figure 5 (CC BY 4.0). Mean ± SD, n = 3. EGCG-loaded niosomes are surfactant vesicles. This study informs delivery design and did not measure PURISOME® performance.

PUBLISHED FIGURE: CUMULATIVE EGCG RELEASE (%)

Compared with a simple solution, vesicular encapsulation approximately doubled EGCG deposition in human skin and provided sustained release over 24 hours.

Vesicle engineering can support surface residence, time-dependent release and delivery into viable skin. These findings inform the design rationale for the PURISOME® liposome platform.

Li D et al. Pharmaceutics. 2022;14(4):726. DOI: 10.3390/pharmaceutics14040726. PMID: 35456560.

ADDITIONAL DATA FROM THE SOURCE SPEAKER NOTES

Ex vivo human skin deposition at 12 hours was 69.0 ± 13.87 µg/cm² with niosomes versus 30.02 ± 2.45 µg/cm² with solution. At 24 hours, values were 54.38 ± 8.86 versus 29.00 ± 1.36 µg/cm² (mean ± SD, n = 3). Niosomes showed biphasic release, approximately 35% at 3 hours and 73% at 24 hours; Korsmeyer–Peppas fit r² = 0.996. These are Li et al.’s niosome results, not PURISOME® measurements.

MECHANISM OVERVIEW

From molecular activity to skin appearance

EGCG

One active, five pathways

INFLAMMATORY SIGNALING

Sebocytes and PM10-exposed keratinocytes. Yoon 2013; Seok 2018.

REDOX DEFENSE

Human UV-challenged skin and oxidative endpoints in fibroblasts. Katiyar 2001; Jia 2023.

SEBOCYTE LIPID BIOLOGY

AMPK / SREBP-1 in human sebocytes. Yoon 2013.

MATRIX PROTECTION

MMP-1/3/10, TIMP-1 and TGF-β1 expression. Jia 2023.

MELANOGENESIS SIGNALING

cAMP / CREB / MITF in B16F10 cells. Zhang 2020.

These experimentally studied pathways inform formulation concepts for resilience, clarity, even tone and follicular vitality.

Pathway overview based on Katiyar 2001; Yoon 2013; Seok 2018; Zhang 2020; Jia 2023. Full references appear at the end.

SKIN SCIENCE: ANTIOXIDANT DEFENSE

Antioxidant evidence in human skin

HYDROGEN PEROXIDE GENERATION IN UV-CHALLENGED SKIN

−68%

−90%

0 25 50 75 100 — Reduction versus UV-only control (%)

EPIDERMAL LIPID PEROXIDATION

−41%

−84%

0 25 50 75 100 — Reduction versus UV-only control (%)

STUDY CONTEXT

EGCG was applied topically to human skin before a single UV challenge of four minimal erythema doses. The ranges cover post-exposure assessment time points. EGCG also helped preserve glutathione-related antioxidant defenses.

These are biological stress-defense endpoints, not SPF values or evidence of UV filtering.

FORMULATION RATIONALE

UV exposure can generate ROS faster than endogenous defenses can clear them.

The reduced oxidative burden observed in human skin supports antioxidant and resilience-oriented daily-care concepts.

Katiyar SK et al. Carcinogenesis. 2001;22(2):287–294. DOI: 10.1093/carcin/22.2.287. PMID: 11181450.

SKIN SCIENCE: PHOTOAGING

Matrix support under photoaging stress

PUBLISHED FIGURE: MATRIX MARKERS IN UVA-STRESSED FIBROBLASTS

Reproduced from Jia et al. 2023, Figure 6, panels A–E. Human dermal fibroblasts, UVA model, EGCG 25 µg/mL.

REPORTED FINDINGS

MMP-1 / MMP-3 / MMP-10 expression decreased versus UVA alone (panels A–C).

TGF-β1 secretion increased (panel D; matrix-building signal).

TIMP-1 mRNA increased (panel E; metalloproteinase inhibitor).

Degradation-associated signals decreased as matrix-supporting signals recovered.

ENDPOINTS

MMP-1/3/10 and TIMP-1 mRNA were measured by RT-PCR. Secreted TGF-β1 protein was measured in culture supernatants (*p < 0.05).

Photoaging involves an imbalance between matrix degradation and renewal. EGCG modulated this balance in cultured human fibroblasts, providing a mechanistic basis for photoaging-oriented formulations.

Jia Y et al. Clin Cosmet Investig Dermatol. 2023;16. DOI: 10.2147/CCID.S398547. PMID: 36704608.

SKIN SCIENCE: CELLULAR SENESCENCE

Reducing the cellular burden of UVA stress

Repeated UVA exposure can promote cellular senescence, with loss of cell division and altered tissue signaling.

Senescence-associated β-galactosidase (SA-β-gal) staining identifies blue-stained cells, quantified as a percentage.

In human fibroblasts, EGCG nearly halved the senescent-cell proportion after UVA exposure.

MODEL

Human dermal fibroblasts; EGCG 25 µg/mL for 24 hours. Mean ± SD from three independent experiments (*p < 0.05).

PUBLISHED FIGURE: SA-β-GAL STAINING AND QUANTIFICATION

Approximately 45% lower senescent-cell proportion relative to UVA alone.

Reproduced from Jia et al. 2023, Figure 2. (A) SA-β-gal staining. (B) Quantification: 23.07% with UVA versus 12.75% with UVA + EGCG.

Jia Y et al. Clin Cosmet Investig Dermatol. 2023;16. DOI: 10.2147/CCID.S398547. PMID: 36704608.

SKIN SCIENCE: URBAN ENVIRONMENTAL STRESS

A scientific rationale for urban skin care

AIRBORNE PARTICULATE MATTER: PM10

Particles that contact facial skin and the scalp during everyday exposure.

KERATINOCYTE STRESS RESPONSE

Oxidative stress and inflammatory signaling increase in exposed cells.

EGCG AT 3–10 µM

Attenuation of oxidative and inflammatory responses in PM10-exposed cells.

Urban exposure places an ongoing particulate burden on skin and scalp. Micromolar EGCG attenuated exposure-related stress in primary human keratinocytes.

These findings support a mechanistic rationale for antioxidant day creams, serums and leave-on scalp products focused on environmental resilience.

MODEL

Primary human keratinocytes exposed to PM10; EGCG tested at 3–10 µM.

Mechanistic evidence only: the study did not measure a pollution-blocking percentage for a finished product.

Seok JK et al. Skin Pharmacol Physiol. 2018;31(3):134–143. DOI: 10.1159/000487400. PMID: 29566388.

SKIN SCIENCE: TONE

Supporting a more even-toned appearance

PUBLISHED FIGURES: ZHANG ET AL. 2020, B16F10 CELLS

Figure 4: cellular tyrosinase activity (A) and melanin content (B). Figure 5: MITF / TYR / TRP-1 / TRP-2 proteins (B) and cAMP (C).

Melanogenesis follows a signaling cascade: increased cAMP, CREB activation and MITF-driven tyrosinase expression and melanin synthesis. EGCG modulated this cascade in B16F10 cells, supporting a mechanistic rationale for even-tone and targeted-care concepts. These are cell-level findings, not clinical age-spot results.

CELL CONTEXT

B16F10 melanocyte model. The schematic presents the pathway, while the published figures show experimental data.

Zhang X et al. Fitoterapia. 2020;145:104634. DOI: 10.1016/j.fitote.2020.104634. PMID: 32454171.

SKIN SCIENCE: SEBUM BIOLOGY

Addressing excess lipid production at the cellular level

AMPK: AMP-activated protein kinase, a cellular energy sensor that suppresses anabolic processes.

SREBP-1: sterol regulatory element-binding protein 1, a transcription factor that activates sebocyte lipid-synthesis genes.

Sebum synthesis in sebocytes is regulated by SREBP-1. In cultured human sebocytes, EGCG activated AMPK and reduced this lipogenic program.

This provides cellular evidence relevant to oil-balancing and blemish-prone-skin concepts.

MODEL

Cultured human sebocytes. Clinical evidence from the same study is presented below.

PUBLISHED FIGURE: YOON ET AL. 2013, FIGURE 1

Sebum, AMPK and SREBP-1 measurements in human sebocytes.

Yoon JY et al. J Invest Dermatol. 2013;133(2):429–440. DOI: 10.1038/jid.2012.292. PMID: 23096708.

SKIN SCIENCE: CLINICAL EVIDENCE

Clinical evidence in blemish-prone skin

−89%

Reported reduction in inflammatory lesion count versus baseline in the 1% EGCG group.

PUBLISHED FIGURES: YOON ET AL. 2013, SPLIT-FACE CONTROLLED TRIAL

Figure 4 presents clinical photographs, Leeds scores and lesion-count changes. The other supplied image is a mechanistic summary schematic, rather than a split-face photograph.

STUDY DESIGN

Split-face, vehicle-controlled study; the contralateral side received vehicle.

1% or 5% EGCG, twice daily for 8 weeks.

35 of 37 participants completed: 17 in the 1% group and 18 in the 5% group.

Endpoints: inflammatory and non-inflammatory lesion counts.

This controlled human study connects sebocyte biology with visible changes in blemish-prone skin, providing a clinical anchor within the evidence base.

Yoon JY et al. J Invest Dermatol. 2013;133(2):429–440. DOI: 10.1038/jid.2012.292. PMID: 23096708.

SKIN SCIENCE: SEBUM, MICROBIAL INTERACTIONS AND COMFORT

Linking sebum, microbial interactions and skin comfort

1 · LIPID ENVIRONMENT

Excess sebum contributes to blemish-prone conditions.

2 · MICROBIAL INTERACTIONS

Cutibacterium acnes proliferates in lipid-rich follicles.

3 · INFLAMMATION AND DISCOMFORT

Inflammatory signaling contributes to visible blemishes.

EXPERIMENTALLY STUDIED EGCG EFFECTS

GROWTH INHIBITION

EGCG showed in vitro inhibition of C. acnes, tested under its historical name Propionibacterium acnes ATCC 6919.

INFLAMMATORY SIGNALING

EGCG attenuated NF-κB-related responses in human sebocytes.

Together with effects on sebocyte lipids, these findings provide a multi-level rationale for blemish-care formulation: less lipid substrate, measured microbial inhibition and reduced inflammatory signaling.

PUBLISHED FIGURE: YOON 2013, FIGURE 2

Sebocyte NF-κB / AP-1 inflammatory measurements.

Yoon JY et al. J Invest Dermatol. 2013;133:429–440. Widyaningrum N et al. Asian J Biol Sci. 2015;8(2):93–101. DOI: 10.3923/ajbs.2015.93.101.

APPLICATION CONCEPTS: SKIN

Skin application concepts

Targets and scientific rationale

Formats and formulation focus

These are formulation-development concepts, not tested finished products. Confirm performance at the product level.

Evidence sources are cited in the skin-science sections; full references appear at the end.

SCALP AND FOLLICLE SCIENCE

Bringing skincare science to scalp care

The scalp faces oxidative and inflammatory challenges similar to facial skin, alongside a distinctive structure: the follicle, a living mini-organ that produces hair.

SCALP ENVIRONMENT

Surface skin exposed to UV, pollution and sebum oxidation.

FOLLICLE

Living cells that drive the hair cycle, including dermal papilla signaling cells.

HAIR SHAFT

A non-living fiber whose surface can be conditioned but whose structure is produced by the follicle.

Scalp and follicle anatomy: conceptual illustration from PuriPharm’s asset collection.

Anatomical schematic for structural reference only.

SCALP AND FOLLICLE SCIENCE

A rationale for a more resilient scalp environment

EVERYDAY SCALP STRESSORS

UV, airborne particles, sebum oxidation and styling stress also challenge the scalp.

OXIDATIVE AND INFLAMMATORY LOAD

Redox and inflammatory pathways documented in skin are relevant to perifollicular scalp tissue.

EGCG DEVELOPMENT RATIONALE

Antioxidant defense and inflammatory modulation formulated for the scalp surface.

A resilient scalp surface provides a basis for follicle-focused care.

NanoActive EGCG brings documented redox and inflammatory biology to leave-on scalp concepts, where longer contact supports local availability.

This is a mechanistic extension from skin studies to scalp-care development. Specific cell and follicle evidence follows.

Rationale based on Katiyar 2001; Seok 2018; Jia 2023. Full references appear at the end.

SCALP AND FOLLICLE SCIENCE: DERMAL PAPILLA

Activity in human dermal papilla cells

Dermal papilla cells (DPCs), located at the follicle base, are signaling cells involved in the hair cycle.

In cultured human DPCs, EGCG at 0.01–0.5 µM produced a significant, dose-dependent proliferative response by MTT assay (p < 0.05).

These micromolar responses provide a cellular basis for follicular-vitality concepts.

EXPERIMENT

MTT proliferation assay in cultured human DPCs; Kwon et al. 2007, Figure 1. This is a cellular response, not a clinical hair-density measurement.

PUBLISHED FIGURE: KWON ET AL. 2007, FIGURE 1, MTT ASSAY

DPC proliferation increased with dose versus control at 0.01–0.5 µM (*p < 0.05). The source figure has low resolution.

Kwon OS et al. Phytomedicine. 2007;14(7–8):551–555. DOI: 10.1016/j.phymed.2006.09.009. PMID: 17092697.

SCALP AND FOLLICLE SCIENCE: SIGNALING

Signals associated with follicular vitality

EGCG

p-ERK ↑, DOSE-DEPENDENT

Mitogen-activated growth signaling.

p-AKT ↑, DOSE-DEPENDENT

Cell survival and growth signaling.

Bcl-2 / Bax RATIO ↑

Balance shifts toward cell survival.

PROLIFERATION AND ANTI-APOPTOTIC SUPPORT IN DPCs

INTERPRETING THE RESULTS

Directional summary of Kwon et al. 2007, Figures 2–4, in cultured human DPCs.

This differs from the sebocyte apoptosis reported with EGCG: different cell types can have different outcomes.

PUBLISHED FIGURES: KWON ET AL. 2007, FIGURES 2–4

Responses of p-ERK, p-AKT and Bcl-2/Bax to EGCG in human DPCs. The source figures have low resolution.

EGCG modulated growth (ERK), survival (Akt) and apoptotic balance (Bcl-2/Bax) signals, providing complementary mechanisms relevant to follicular formulation concepts.

Kwon OS et al. Phytomedicine. 2007;14(7–8):551–555. DOI: 10.1016/j.phymed.2006.09.009. PMID: 17092697.

SCALP AND FOLLICLE SCIENCE: ORGAN CULTURE

Evidence from human follicle organ culture

FOLLICLE ELONGATION AFTER 10 DAYS, AS A PERCENTAGE OF VEHICLE CONTROL

Redrawn from Kwon et al. 2007. Mean ± SD: the three EGCG groups had SDs of 9.0, 7.1 and 15.8 percentage points, respectively; p < 0.05 versus vehicle. Human follicles came from three donors and were cultured for 10 days.

Beyond isolated cells, EGCG increased elongation of whole human follicles over 10 days in organ culture.

This model bridges cellular experiments and clinical research and provides preclinical support for follicular-vitality concepts in leave-on scalp care.

EX VIVO HUMAN FOLLICLE MODEL

The same paper also reports a separate, small scalp-biomarker experiment, summarized in the source speaker notes. Neither constitutes a clinical hair-growth outcome.

Kwon OS et al. Phytomedicine. 2007;14(7–8):551–555. DOI: 10.1016/j.phymed.2006.09.009. PMID: 17092697.

ADDITIONAL CONTEXT FROM THE SOURCE SPEAKER NOTES

The paper separately reports a 4-day scalp-biomarker experiment in three volunteers using 10% EGCG in ethanol, with increased dermal papilla p-Erk/p-Akt and Bcl-2/Bax. This small experiment is distinct from ex vivo follicle elongation, is not a clinical hair-growth outcome and is not a product use-level recommendation.

SCALP AND FOLLICLE SCIENCE: DELIVERY DESIGN

Designing local skin and follicular delivery

Conceptual schematic of follicular accumulation of nanocarriers, from PuriPharm’s asset collection.

Published figure: Li et al. 2022, Figure 6. FITC-loaded vesicles concentrated at follicular openings in ex vivo human skin.

This delivery-design concept is consistent with published vesicle research (Li 2022). The image does not establish transport of intact vesicles to the dermal papilla, and smaller particle size does not automatically mean deeper penetration.

Delivery reference: Li D et al. Pharmaceutics. 2022;14(4):726. DOI: 10.3390/pharmaceutics14040726.

APPLICATION CONCEPTS: HAIR AND SCALP

Hair and scalp formulation concepts

Targets and formulation focus

Formats and contact patterns

These are development concepts. Follicle-focused positioning centers on leave-on formats, where contact duration supports local activity.

Evidence sources are cited in the scalp and follicle sections. Full references appear at the end.

FORMULATION DESIGN

Targeted active combinations

NanoActive EGCG provides the core active, while complementary ingredients refine the concept. These are formulation choices; confirm compatibility in the final vehicle.

+ NIACINAMIDE

OIL-BALANCING CONCEPT

EGCG addresses sebocyte lipid biology, while niacinamide adds barrier and tone support. Complementary pathways inform oily- and blemish-prone-skin positioning.

+ PANTHENOL

COMFORT AND SOOTHING CONCEPT

EGCG modulates stress signaling, while panthenol supports hydration and comfort. This pairing is proposed for sensitive-skin and scalp formats.

+ CAFFEINE

SCALP-VITALITY CONCEPT

EGCG dermal papilla biology complements the established use of caffeine in leave-on scalp tonics and serums.

Check vehicle pH, ionic environment, oxidation drivers and preservation together. Factors governing EGCG stability (Proniuk 2002) also apply to multi-active formulations.

Combination concepts: PuriPharm. Stability principles: Proniuk 2002, discussed in the formulation-rationale section.

FORMULATION PRACTICE

Practical formulation integration

ADDITION AND HANDLING

Evaluate cool-down addition to reduce heat exposure.

Review shear exposure during homogenization and pumping.

Minimize residence at high temperature.

BASE ENVIRONMENT

Set pH deliberately; EGCG is more stable in acidic conditions.

Control ionic conditions that may challenge vesicle integrity.

Manage dissolved oxygen, light and pro-oxidant metals.

COMPATIBILITY

Screen surfactants for vesicle compatibility; high levels may disrupt lipid vesicles.

Check interactions with other actives, electrolytes and thickeners.

Confirm preservative-system compatibility.

These are development considerations, not validated processing limits. Refer to PuriPharm’s NanoActive EGCG technical documentation for product-specific addition stage, temperature and use-level guidance.

Stability principles: Proniuk 2002. Product instructions follow PuriPharm technical documentation.

FORMULATION PRACTICE

Protecting active quality through formulation and packaging

FORMULATION

Liposomal encapsulation protects EGCG from bulk-phase oxidation.

Design pH and antioxidant support around catechin chemistry.

Assess metal interactions and use chelation where appropriate.

PACKAGING

Limit light using opaque or UV-protective packaging.

Limit oxygen ingress using airless or low-headspace formats.

Match the pack to application and dose control.

MONITORING

Track color and EGCG content during stability studies.

Characterize carrier integrity, vesicle structure and size.

Use sensory changes as early-warning signals.

Active quality is a system property involving chemistry, packaging and monitoring. Finished-product shelf life and stability claims require product-level testing.

Framework based on EGCG solution chemistry (Proniuk 2002) and vesicular delivery research (Li 2022).

FROM SCIENCE TO BRAND

Translating science into brand value

Consumer wording is limited to cosmetic positioning and anchored to the cited skin and follicle studies.

Evidence anchors: Katiyar 2001; Jia 2023; Yoon 2013; Zhang 2020; Kwon 2007.

CONCLUSION

NanoActive EGCG: from catechin science to formulation opportunity

1 MULTIFUNCTIONAL ACTIVE

Published biological evidence covers antioxidant defense, photoaging, sebum balance, tone and follicular vitality.

2 PURPOSEFUL DELIVERY

PURISOME® liposome technology is designed to protect the catechin and support local, sustained delivery.

3 SKIN AND SCALP OPPORTUNITIES

One platform spans serums, gels, moisturizers, essences, treatments and scalp-care products.

Powered by PURISOME® FlexVes™ Liposome Technology

PuriPharm Co., Ltd.

www.puriactives.com

REFERENCES · SKIN BIOLOGY

Key scientific references: skin biology

Katiyar SK et al. Green tea polyphenol (−)-epigallocatechin-3-gallate treatment of human skin inhibits UV-induced oxidative stress. Carcinogenesis. 2001;22(2):287–294. DOI: 10.1093/carcin/22.2.287. PMID: 11181450.

Jia Y et al. (−)-Epigallocatechin-3-gallate protects human skin fibroblasts from ultraviolet A induced photoaging. Clinical, Cosmetic and Investigational Dermatology. 2023;16. DOI: 10.2147/CCID.S398547. PMID: 36704608. PMCID: PMC9871046.

Seok JK, Lee JW, Kim YM, Boo YC. Punicalagin and (−)-epigallocatechin-3-gallate rescue cell viability and attenuate inflammatory responses of human epidermal keratinocytes exposed to airborne particulate matter PM10. Skin Pharmacology and Physiology. 2018;31(3):134–143. DOI: 10.1159/000487400. PMID: 29566388.

Yoon JY et al. Epigallocatechin-3-gallate improves acne in humans by modulating intracellular molecular targets and inhibiting P. acnes. Journal of Investigative Dermatology. 2013;133(2):429–440. DOI: 10.1038/jid.2012.292. PMID: 23096708.

Zhang X et al. Anti-melanogenic effects of epigallocatechin-3-gallate (EGCG), epicatechin-3-gallate (ECG) and gallocatechin-3-gallate (GCG) via down-regulation of cAMP/CREB/MITF signaling pathway in B16F10 melanoma cells. Fitoterapia. 2020;145:104634. DOI: 10.1016/j.fitote.2020.104634. PMID: 32454171.

Widyaningrum N, Fudholi A, Sudarsono, Setyowati EP. Stability of epigallocatechin gallate (EGCG) from green tea (Camellia sinensis) and its antibacterial activity against Staphylococcus epidermidis ATCC 35984 and Propionibacterium acnes ATCC 6919. Asian Journal of Biological Sciences. 2015;8(2):93–101. DOI: 10.3923/ajbs.2015.93.101.

Only literature cited in the presentation is listed. Microbial names retain the historical terminology used at publication.

Skin biology references. Hair, delivery and formulation references follow.

REFERENCES · HAIR, DELIVERY AND FORMULATION

Key scientific references: hair, delivery and formulation

HAIR AND SCALP

Kwon OS, Han JH, Yoo HG, Chung JH, Cho KH, Eun HC, Kim KH. Human hair growth enhancement in vitro by green tea epigallocatechin-3-gallate (EGCG). Phytomedicine. 2007;14(7–8):551–555. DOI: 10.1016/j.phymed.2006.09.009. PMID: 17092697.

DELIVERY AND FORMULATION

Li D et al. Niosomal nanocarriers for enhanced dermal delivery of epigallocatechin gallate for protection against oxidative stress of the skin. Pharmaceutics. 2022;14(4):726. DOI: 10.3390/pharmaceutics14040726. PMID: 35456560. PMCID: PMC9029719.

Proniuk S, Liederer BM, Blanchard J. Preformulation study of epigallocatechin gallate, a promising antioxidant for topical skin care products. Journal of Pharmaceutical Sciences. 2002;91(1):111–116. DOI: 10.1002/jps.10009. PMID: 11782902.

Structure reference: Epigallocatechin gallate, PubChem CID 65064, NIH National Library of Medicine (active-identity section).

Only literature cited in the presentation is listed. PURISOME® platform descriptions are based on PuriPharm Co., Ltd. brand documentation.

NanoActive EGCG nanoliposomes: scientific marketing report. PuriPharm Co., Ltd.

 

PuriActives® Crystal Retinal

PuriActives® Crystal RetinalCyclodextrin-Included Retinal

PuriPharm Co., Ltd. · Retinal science

PuriActives® Crystal Retinal Cyclodextrin-Included Retinal

High-performance retinal through molecular inclusion science

Retinal · Cyclodextrin inclusion · Skin and scalp renewal

Scientific and technical report for cosmetic formulators and brand R&D teams

PART I · NEXT-GENERATION RETINAL

The evolution of vitamin A skincare

RETINYL ESTERS

Storage forms requiring hydrolysis before entering metabolism.

RETINOL

An established cosmetic benchmark, oxidized to retinal in skin.

RETINAL (RAL)

One oxidation step from retinoic acid: its direct metabolic precursor.

RETINOIC ACID

The receptor-active form; prescription-only in many markets.

Esterases · Retinol dehydrogenases (RDH/ADH) · Retinaldehyde dehydrogenases (ALDH1A)

FROM STORAGE FORM TO SIGNALING MOLECULE

Cosmetic vitamin A ingredients follow the skin’s own metabolic pathway. Moving closer to retinoic acid reduces the number of enzymatic conversions.

Retinal is the direct biosynthetic precursor of retinoic acid, the active form that binds nuclear retinoid receptors and drives epidermal renewal.

Metabolic proximity is a mechanistic rationale, not a clinical conclusion. Relative efficacy requires controlled human studies, reviewed in Part III.

2 → 1

Oxidation steps to retinoic acid: two for retinol, one for retinal.

1994

Topical retinal was first biologically characterized in human skin (Saurat et al.).

125+

Participants indicated in the source’s milestone vehicle-controlled profilometry trial comparing retinal with retinoic acid (1998).

Saurat JH et al. J Invest Dermatol. 1994;103(6):770–774. Creidi P et al. J Am Acad Dermatol. 1998;39(6):960–965. Retinoid metabolism: RDH/ADH and ALDH1A enzyme families.

PART I · NEXT-GENERATION RETINAL

One conversion from retinoic acid: retinal biology

All-trans-retinal (C20H28O; molecular weight 284.4)

The β-ionone ring, conjugated polyene chain and terminal aldehyde underlie both biological activity and chemical vulnerability.

The conjugated system responsible for sensitivity to light and oxidation also contributes to retinal’s biological activity.

Stabilizing this molecule without changing its chemistry is the formulation challenge addressed by cyclodextrin inclusion.

A NATURAL INTERMEDIATE IN VITAMIN A METABOLISM

Retinal forms from retinol in skin and can convert further to retinoic acid.

DIRECT PRECURSOR

One oxidation by retinaldehyde dehydrogenases produces retinoic acid, a ligand for nuclear RAR receptors involved in epidermal gene regulation.

DOCUMENTED BIOACTIVITY IN HUMAN SKIN

Early human studies reported measurable effects of topical retinal, including epidermal hyperplasia and increased dermal elastin, with good tolerability.

THREE DECADES OF CLINICAL LITERATURE

Human studies since 1994 have assessed texture, wrinkles, elasticity, tone, hydration and tolerability.

COSMETIC POSITIONING

The source identifies retinal (INCI: RETINAL) as a cosmetic retinoid, in contrast to retinoic acid, supporting science-led formulation development.

Saurat JH et al. J Invest Dermatol. 1994;103(6):770–774. Sorg O, Saurat JH. Dermatology. 2014;228(4):314–325. Formula and molecular weight: PubChem CID 638015.

PART I · NEXT-GENERATION RETINAL

High potential with demanding formulation requirements

Retinal’s conjugated polyene chain and terminal aldehyde are chemically reactive. In conventional formulations, degradation through several documented pathways can reduce the available active.

PHOTOCHEMICAL SENSITIVITY

UV and visible light induce polyene photoisomerization and photodegradation.

OXIDATIVE DEGRADATION

Autoxidation of the conjugated chain generates peroxide intermediates and breakdown products.

THERMAL INSTABILITY

Heat accelerates degradation, affecting manufacturing, transport and shelf life.

ISOMERIZATION

Light and heat can convert the all-trans form into cis isomers with altered biological activity.

VERY LOW WATER SOLUBILITY

The lipophilic molecule is difficult to disperse uniformly in aqueous and emulsified systems.

ACTIVE RETENTION IN FORMULATIONS

Interactions with oils, surfactants and packaging may reduce the retinal available at the point of use.

PATENT STRESS TESTS

Under accelerated UV aging (200–400 nm, 48 hours), an unstabilized retinal gel faded from deep yellow toward near-complete degradation, with a color score of 1/20. Under thermal stress (45 °C, 7 days), the unstabilized group showed complete degradation, scored 20/20.

US 10,864,148 B2 (2020), Example 3, Table 6: visual color-scoring degradation tests of retinal formulations.

Selecting retinal is the first step. Its molecular environment determines how it can be formulated.

PART II · THE SCIENCE OF CRYSTAL RETINAL

Introducing PuriActives® Crystal Retinal Cyclodextrin-Included Retinal

A cyclodextrin-included retinal system designed around molecular stabilization and formulation flexibility, connecting retinal biology with host–guest chemistry.

PRODUCT

PuriActives® Crystal Retinal Cyclodextrin-Included Retinal

INCI NAME

RETINAL

CORE TECHNOLOGY

Cyclodextrin molecular inclusion

APPLICATIONS

Premium skincare and science-led scalp care

RETINAL BIOLOGY

The direct metabolic precursor of retinoic acid, supported by three decades of human research.

MOLECULAR INCLUSION

Cyclodextrin host–guest chemistry provides a protective environment for a vulnerable active.

FORMULATION INNOVATION

A solid, dispersible ingredient format opens formulation routes that are difficult for free retinal.

Designed for formulators seeking a stabilization strategy at the ingredient level while retaining retinal’s biological identity.

PART II · THE SCIENCE OF CRYSTAL RETINAL

Cyclodextrins: molecular architecture from starch

Cyclodextrins are cyclic oligosaccharides produced by enzymatic conversion of starch. Their truncated-cone geometry creates a relatively hydrophilic exterior and a relatively hydrophobic cavity suited to lipophilic guests such as retinoids.

α-CYCLODEXTRIN

6 glucopyranose units; the smallest cavity, approximately 4.7–5.3 Å.

β-CYCLODEXTRIN

7 glucopyranose units; a medium cavity, approximately 6.0–6.5 Å.

γ-CYCLODEXTRIN

8 glucopyranose units; the largest cavity, approximately 7.5–8.3 Å.

Cavity size affects which guests enter and how they are accommodated. In cited vitamin A tests, the larger γ-cyclodextrin cavity provided greater protection than β-cyclodextrin, making cavity geometry an important formulation variable.

After 48 days of UVA stress, a retinol/γ-CD complex retained 18.0% retinol, while the corresponding β-CD complex retained none (US 5,985,296, Example 3, Table 1).

Structure figures: US 8,410,079 B2 (2013), Figures 1–3. Cavity dimensions: Loftsson T, Brewster ME. J Pharm Sci. 1996;85(10):1017–1025.

PART II · THE SCIENCE OF CRYSTAL RETINAL

Molecular inclusion: a protective environment for retinal

HOST–GUEST ASSOCIATION: SCHEMATIC

Cyclodextrin host: hydrophilic exterior

Hydrophobic

cavity

Retinal guest

Noncovalent association: the guest is accommodated, not chemically modified.

DYNAMIC EQUILIBRIUM

Included retinal ⇌ Free retinal. As free retinal is taken up by skin during use, the equilibrium replenishes available active.

HOST–GUEST ASSOCIATION

Hydrophobic and van der Waals interactions drive lipophilic guests into the nonpolar cavity.

REDUCED ENVIRONMENTAL EXPOSURE

The included fraction has reduced exposure to bulk solvent, oxygen and light, key contributors to retinal degradation.

DISPERSION AND HANDLING

A lipophilic crystalline active becomes a water-dispersible solid ingredient for easier weighing, dispersion and processing.

EQUILIBRIUM-DRIVEN AVAILABILITY

Guest release follows the association equilibrium without shell rupture or a triggered chemical reaction.

DISTINCT FROM COVALENT DERIVATIVES

Inclusion is a physical association. The retinal–cyclodextrin hemiacetals discussed in the patent section are covalently bonded molecules of another class.

Loftsson T, Brewster ME. J Pharm Sci. 1996;85(10):1017–1025. Yap KL et al. Eur J Pharm Sci. 2005;25(1):49–56. Schematic for illustration; partial inclusion geometries of polyene guests have been reported.

PART II · THE SCIENCE OF CRYSTAL RETINAL

Stability through molecular design: interpreting stress tests

RETINOL RETENTION DURING OPEN STORAGE IN DAYLIGHT AT ROOM TEMPERATURE

Intact retinol measured by HPLC relative to day 0. US 5,985,296, Example 4, Table 2.

UVA AT 366 NM FOR 48 DAYS

18.0% retinol retained in the γ-CD complex

0% retained in the β-CD complex under the same conditions

US 5,985,296, Example 3, Table 1.

Protection depends on the molecular environment. In the patent comparisons, the γ-cyclodextrin complex retained most retinol after three weeks of open daylight storage, whereas the lactose triturate lost almost all of it.

Under UVA stress, γ-CD outperformed the smaller β-CD cavity, indicating the importance of inclusion geometry.

These data concern retinol, the immediate precursor of retinal, which shares related conjugated degradation chemistry.

US 5,985,296 A (Wacker-Chemie, 1999), Examples 3–4, Tables 1–2. Stability is complex-specific. These results characterize the tested materials and do not represent a particular commercial ingredient.

PART II · THE SCIENCE OF CRYSTAL RETINAL

Four decades of retinal and cyclodextrin patent science

1983

WATER-SOLUBLE RETINOID COMPLEXES

Retinal–polymer conjugates with cyclodextrin for water-compatible vitamin A systems.

US 4,371,673 (Pitha): an early approach to water-compatible retinoid delivery.

1999

γ-CD INCLUSION FOR VITAMIN A STABILITY

Quantified improvements in light and storage stability of retinol/γ-CD complexes.

US 5,985,296 (Wacker-Chemie): HPLC comparisons with β-CD and lactose controls.

2013

RETINAL–CD HEMIACETAL DERIVATIVES

Covalent retinal–cyclodextrin structures developed for skin-tone applications.

US 8,410,079 B2: chemically distinct from noncovalent inclusion complexes.

2020

MODERN RETINAL STABILIZATION

Cyclodextrin-encapsulated retinal combined with antioxidant systems.

US 10,864,148 B2: thermal and UV stress tests of encapsulated retinal gels.

WHAT THE PATENT HISTORY SHOWS

Successive approaches address retinoid instability through solubilization, inclusion, covalent derivatives and integrated formulations. Cyclodextrin inclusion is a route that protects the active without changing its molecular identity.

General retinal–cyclodextrin acetal structure

CN 103987391 B, Formula (Ib).

Exocyclic retinal–CD hemiacetal (VIII)

EP 2 755 664 B1 / HK 1200172 B, page 8.

US 4,371,673 A (1983) · US 5,985,296 A (1999) · US 8,410,079 B2 (2013) · US 10,864,148 B2 (2020).

PART II · THE SCIENCE OF CRYSTAL RETINAL

Comparing retinal formulation approaches

Three approaches to retinal formulation involve different practical considerations. This table compares formulation principles rather than ranking performance.

This is a qualitative comparison of formulation principles. Actual performance depends on the complex, manufacturing process and finished formulation. Validation parameters must be established during product development.

PART III · RETINAL BIOLOGY AND SKIN BENEFITS

From retinal to skin renewal: the signaling cascade

DOCUMENTED IN SKIN

RETINAL INCREASES CUTANEOUS RETINOIC ACID

Topical retinal increased retinoic acid content and retinoid activity in mouse skin, supporting enzymatic conversion within tissue (Didierjean et al., 1996; Sorg et al., 1999).

HUMAN EPIDERMAL RENEWAL MARKERS

In human skin, topical retinal induced epidermal hyperplasia and increased dermal elastin with good tolerability, consistent with retinoid-mediated renewal (Saurat et al., 1994).

RECEPTOR SPECIFICITY

In human keratinocytes, retinoid signaling at physiological, nanomolar ligand concentrations acts mainly through RAR–RXR heterodimers at βRARE elements (Xiao et al., 1995).

DOWNSTREAM VISIBLE ENDPOINTS

Texture, wrinkles, firmness, tone and barrier quality are mapped to human evidence in the following sections.

Didierjean L et al. J Invest Dermatol. 1996;107(5):714–719. Sorg O et al. Dermatology. 1999;199(Suppl 1):13–17. Saurat JH et al. J Invest Dermatol. 1994;103(6):770–774. Xiao JH et al. J Biol Chem. 1995;270(7):3001–3011.

PART III · RETINAL BIOLOGY AND SKIN BENEFITS

Skin texture: measurable renewal

Skin-surface refinement is an instrumentally measurable retinoid endpoint. Retinal supports orderly keratinocyte renewal, and changes can be assessed by profilometry and 3D imaging.

WHY THE SURFACE RESPONDS

Retinoic acid generated in skin modulates keratinocyte differentiation and epidermal turnover. Replacement of accumulated, disorganized corneocytes produces a more regular surface, measured as lower roughness in 3D imaging.

Retinal’s single-step conversion provides a rationale for renewal at cosmetic use concentrations.

+13.7%

Texture improvement with 0.1% retinal

+12.6%

Texture improvement with 0.05% retinal

Randomized double-blind trial: 40 women with photoaged skin, twice-daily use for 3 months; texture quantified by Antera 3D imaging.

BENCHMARK PROFILOMETRY STUDY

Creidi et al. J Am Acad Dermatol. 1998.

125 participants · 44 weeks · 0.05% retinal

DESIGN

Double-blind comparison of 0.05% retinal, 0.05% retinoic acid and vehicle in photoaged skin, with objective surface profilometry.

RESULTS

Both vitamin A groups reduced wrinkles and roughness versus vehicle, with significant improvement from week 18. Efficacy did not differ significantly between the active groups.

TOLERABILITY

Retinal was significantly better tolerated than retinoic acid at the same concentration.

For formulation development, these results support retinal as a cosmetic option with surface efficacy comparable to retinoic acid under the tested conditions. Inclusion provides a stabilization rationale that must be verified in the formulation.

Kwon HS et al. J Cosmet Dermatol. 2018;17(3):471–476. Creidi P et al. J Am Acad Dermatol. 1998;39(6):960–965. Studies used finished creams; results characterize the retinal active class.

PART III · RETINAL BIOLOGY AND SKIN BENEFITS

Wrinkles and fine lines: clinical evidence

TWELVE WEEKS, TWO CONCENTRATIONS, FOUR ENDPOINTS

Percentage change from baseline; randomized double-blind trial; 40 women; twice-daily use.

All displayed changes were significant versus baseline except the 0.05% group’s melanin endpoint, which was not significant and is therefore shown without a bar. Lower TEWL and melanin index indicate improvement.

LONG-TERM CONTROLLED EVIDENCE

Week 18: significant reduction versus vehicle

44-week follow-up; n = 125

Creidi P et al. J Am Acad Dermatol. 1998.

At the same 0.05% concentration, retinal provided wrinkle improvement comparable to retinoic acid by profilometry, with significantly less irritation.

The response persisted through the 44-week observation period, supporting a sustained rather than transient surface effect.

DOSE-SELECTION RATIONALE

In the reported results, 0.1% showed greater texture and pigment changes, while 0.05% showed the greater TEWL reduction. These endpoints inform different formulation concepts.

Kwon HS et al. J Cosmet Dermatol. 2018;17(3):471–476 (randomized double-blind trial, n = 40, 3 months; Antera 3D, corneometry, TEWL and pigment measurement). Creidi P et al. J Am Acad Dermatol. 1998;39(6):960–965 (n = 125, 44 weeks; profilometry).

PART III · RETINAL BIOLOGY AND SKIN BENEFITS

Dermal matrix: collagen and elastic-fiber support

Photoaging involves disrupted collagen and elastic fibers. Histology in skin explants and instrumental measurements in vivo provide evidence relevant to retinal and matrix-related care.

HUMAN SKIN EXPLANTS: UVA REPAIR MODEL

Fibers restored toward unexposed levels

Human skin explants were photoaged with UVA in organ culture and treated with 0.05% retinal cream for 2 weeks. In all examined specimens, collagen and elastic fibers returned to unexposed-skin levels, and UVA-suppressed collagen synthesis normalized.

Boisnic S et al. Dermatology. 1999;199(Suppl 1):43–48.

CLINICAL STUDY: ULTRASOUND AND RHEOLOGY

Instrumentally measured thickness and elasticity

Topical 0.05% retinal significantly increased epidermal thickness and skin elasticity in aging skin, quantified by high-frequency ultrasound and rheology.

Diridollou S et al. Dermatology. 1999;199(Suppl 1):37–41.

p < 0.01

Significance reported for increased epidermal thickness and elasticity with 0.05% retinal.

These findings provide a rationale for firmness and density concepts alongside surface smoothing.

SIGNALING BEHIND THE STRUCTURE

RAR-mediated transcription in epidermal keratinocytes is the main documented pathway. Explant data show matrix recovery consistent with renewed collagen synthesis after UV damage.

Active retention through stabilization is a formulation prerequisite that requires product-level confirmation.

Boisnic S et al. Dermatology. 1999;199(Suppl 1):43–48 (human skin explants, UVA + 0.05% retinal, 2 weeks). Diridollou S et al. Dermatology. 1999;199(Suppl 1):37–41 (0.05% retinal; ultrasound and rheology endpoints).

PART III · RETINAL BIOLOGY AND SKIN BENEFITS

Skin tone and pigmentation

MELANIN INDEX AT 12 WEEKS

−6.5%

A significant reduction in the 0.1% retinal group in the randomized double-blind photoaging trial.

Kwon HS et al. J Cosmet Dermatol. 2018.

The pigment endpoint was significant at 0.1% and not significant at 0.05%. This supports a concentration-specific rather than universal skin-tone claim.

HOW RETINAL RELATES TO SKIN TONE

PIGMENT CLEARANCE THROUGH TURNOVER

Accelerated epidermal renewal replaces melanin-containing keratinocytes and reduces surface pigment residence.

REPORTED DEPIGMENTING ACTIVITY

A dedicated study in pigmentary disorders reported measurable depigmenting activity of topical retinal, supporting even-tone formulation development.

Sorg O et al. Dermatology. 2013;227(3):231–237.

THE ROLE OF PHOTOSTABILITY

The source proposes light-stable inclusion as a way to retain activity in tone-care products intended for daytime use. This performance must be established for the specific complex and formulation.

POSITIONING

Combine tone-care evidence with texture and tolerability endpoints to support an even, refined skin appearance. Final product claims require validation.

Kwon HS et al. J Cosmet Dermatol. 2018;17(3):471–476 (n = 40, 3 months; significant melanin reduction only at 0.1%). Sorg O et al. Dermatology. 2013;227(3):231–237.

PART III · RETINAL BIOLOGY AND SKIN BENEFITS

Refined skin: pores and blemish-related mechanisms

The source reports direct antibacterial activity of retinal against Cutibacterium acnes, formerly Propionibacterium acnes, distinguishing it from the retinol and retinoic acid comparators discussed.

IN VITRO: MINIMUM INHIBITORY CONCENTRATION

4–8 mg/L

Retinal MIC against three P. acnes reference strains.

COMPARATOR

>128 mg/L

Retinoic acid MIC against the same strains.

This activity is attributed to retinal’s aldehyde group, a property of the molecule rather than a finished product.

Pechère M et al. Dermatology. 1999;199(Suppl 1):29–31.

IN VIVO: SINGLE-BLIND RANDOMIZED STUDY

The source slide records the median viable-count decrease per cm² as “≈ −10² log” after 2 weeks of daily 0.05% retinal. Vehicle alone was ineffective.

The numerical notation is ambiguous and is retained as written rather than converted to a different unit.

COMPLEMENTARY EVIDENCE

COMEDOLYTIC ACTIVITY

Topical retinal reduced comedones in the rhino mouse model, providing a complementary mechanism for pore-focused concepts.

Fort-Lacoste L et al. Dermatology. 1999;199(Suppl 1):33–35.

Use as mechanistic support for clarifying and blemish-prone-skin positioning, rather than a standalone acne-treatment claim.

Pechère M et al. Dermatology. 1999;199(Suppl 1):29–31. Fort-Lacoste L et al. Dermatology. 1999;199(Suppl 1):33–35. In vitro and animal findings provide mechanistic support, not clinical acne efficacy.

PART III · RETINAL BIOLOGY AND SKIN BENEFITS

Barrier function, hydration and tolerability

BARRIER FUNCTION: KWON 2018 RANDOMIZED TRIAL

−14.5%

TEWL in the 0.1% group

−17.9%

TEWL in the 0.05% group

+10.2%

Skin hydration in the 0.1% group

+6.0%

Skin hydration in the 0.05% group

After 12 weeks of twice-daily retinal use, lower TEWL and greater stratum corneum hydration indicated improvements versus baseline.

TOLERABILITY UNDER CHALLENGE

MAXIMIZED AND LONG-TERM EXPOSURE

In a tolerability study with 355 volunteers under maximized and long-term conditions, retinoic acid caused significantly more erythema and scaling, while retinal was closer to vehicle.

Fluhr JW et al. Dermatology. 1999;199(Suppl 1):57–60.

NO PHOTOTOXICITY SIGNAL

A dedicated human tolerability review involving 357 subjects reported a favorable safety profile for topical retinal, including no phototoxic reactions.

Sachsenberg-Studer EM. Dermatology. 1999;199(Suppl 1):61–63.

MINIMAL SYSTEMIC EXPOSURE

Plasma retinoid levels were essentially unchanged after topical use in human skin, supporting local-action positioning.

Sass JO et al. Skin Pharmacol. 1996;9(5):322–326.

FORMULATION VALUE

Tolerability is important for retinoid adherence. The cited barrier and tolerability findings inform the development of everyday retinal products.

Kwon HS et al. J Cosmet Dermatol. 2018;17(3):471–476. Fluhr JW et al. Dermatology. 1999;199(Suppl 1):57–60. Sachsenberg-Studer EM. Dermatology. 1999;199(Suppl 1):61–63. Sass JO et al. Skin Pharmacol. 1996;9(5):322–326.

PART IV · SCALP SCIENCE AND HAIRCARE INNOVATION

The scalp is skin and responds to retinoid signaling

PuriActives® Crystal Retinal: retinal held within a cyclodextrin inclusion complex.

Scalp care draws on skincare concepts such as renewal, barrier support and the microbiome. The scalp is a specialized, follicle-rich skin surface with relevant retinoid biology.

A RETINOID-RESPONSIVE SURFACE

Scalp epidermis shares retinoid receptor mechanisms with facial skin. The retinal-to-retinoic-acid pathway can operate in keratinocytes across body sites.

A MICROBIAL DIMENSION

The follicle-rich scalp carries dense microbial communities, including C. acnes. Retinal’s reported activity against this organism provides a follicular-environment rationale.

FORMULATION CHALLENGES

Scalp products are often water-rich, surfactant-containing and transparent, creating stability challenges for unprotected retinal.

Retinoid skin biology: Saurat JH et al. J Invest Dermatol. 1994;103(6):770–774. Antibacterial activity: Pechère M et al. Dermatology. 1999;199(Suppl 1):29–31.

PART IV · SCALP SCIENCE AND HAIRCARE INNOVATION

Follicular biology: interpreting receptor evidence

The follicle is a retinoid-sensitive mini-organ. Receptor genetics defines the biological rationale and the limits of scalp-care positioning.

GENETIC EVIDENCE: RXRα AND THE HAIR CYCLE

Keratinocyte RXRα is required for a normal hair cycle.

Mice with targeted RXRα loss in epidermal and follicular keratinocytes developed progressive alopecia and failed to initiate anagen, establishing a requirement for this receptor signaling in the hair cycle.

Li M et al. Development. 2001;128(5):675–688.

REVIEW EVIDENCE: THE PILOSEBACEOUS UNIT

Retinoids act on follicular glands and epithelium.

An endocrine review of pilosebaceous biology discusses retinoid effects on sebocyte differentiation and follicular keratinization, processes relevant to scalp condition, oiliness and scaling.

Deplewski D, Rosenfield RL. Endocr Rev. 2000;21(4):363–392.

POSITIONING WITHIN THE EVIDENCE

Retinoid effects are dose-dependent, and excessive systemic exposure is associated with hair loss.

Crystal Retinal’s scalp positioning therefore concerns a balanced, comfortable scalp and follicular environment.

No hair-growth, density-increase or hair-loss-prevention claim is made or implied.

TAKEAWAY

Follicular retinoid sensitivity is established biology; cosmetic development opportunities concern scalp condition.

Li M et al. Development. 2001;128(5):675–688. Deplewski D, Rosenfield RL. Endocr Rev. 2000;21(4):363–392. Mechanistic evidence, not clinical validation of Crystal Retinal.

PART IV · SCALP SCIENCE AND HAIRCARE INNOVATION

Scalp-care opportunities from the formulation bench

Premium haircare increasingly uses skincare actives. Retinal development requires stability in realistic scalp formats: water-rich systems with surfactants and potentially prolonged residence.

THE CHALLENGE

Free retinal is difficult to stabilize in scalp formats.

Water, oxygen, light and surfactant environments can promote loss of unprotected retinal during product development and storage.

THE INCLUSION APPROACH

A protected guest available at the interface.

The inclusion complex reduces exposure of retinal’s conjugated system in the bulk formulation and allows guest exchange at the skin interface through water activity and lipid affinity.

A BRAND DEVELOPMENT CONCEPT

Skincare renewal adapted for the scalp.

Scalp comfort, balance, gentle renewal and follicular-environment care are anchored in published skin biology rather than hair-growth promises.

Stability engineering creates an opportunity to explore retinal in demanding scalp formats.

PART V · FORMULATION AND APPLICATIONS

Formulating Crystal Retinal: working principles

Inclusion chemistry provides a stabilization rationale, but processing remains important. Confirm each of these eight principles in the customer’s own stability program.

01 ADD DURING COOL-DOWN

Introduce the complex below typical hot-process temperatures to protect host–guest equilibrium.

02 CONTROL LIGHT FROM THE START

Use amber or opaque handling through production and filling.

03 BUILD ANTIOXIDANT SUPPORT

Chelators and antioxidant systems remain useful for retinoids, whether included or free.

04 SET pH USING MEASUREMENTS

Mildly acidic conditions are generally favorable; confirm the suitable window in the final base.

05 SCREEN COMPETING GUESTS

Hydrophobic fragrance constituents and oils may compete for the cyclodextrin cavity. Check displacement risk in compatibility tests.

06

AVOID STRONG OXIDATIVE CHALLENGES

Peroxides and aggressive preservative boosters can affect the polyene chain. Screen the full combination.

07

SPECIFY PROTECTIVE PACKAGING

Airless, low-permeability, light-protective packaging supports shelf-life retention.

08

VALIDATE IN THE REAL FORMULATION

Run accelerated and real-time stability tests on the finished product. Complex data guide development but do not replace product-level evidence.

Principles are drawn from retinoid and cyclodextrin literature. PuriPharm technical support can advise on specific bases.

Loftsson T, Brewster ME. J Pharm Sci. 1996;85(10):1017–1025. Yap KL et al. Eur J Pharm Sci. 2005;25(1):49–56. These principles are not validated specifications for a particular formulation.

PART V · FORMULATION AND APPLICATIONS

Skincare concepts informed by the evidence

NIGHT RENEWAL SERUM

Texture and wrinkle endpoints from randomized studies provide claim-development anchors. Inclusion is intended to support active retention during shelf life.

Evidence anchors: Kwon 2018; Creidi 1998.

GENTLE EVERYDAY RETINAL MOISTURIZER

Barrier findings and vehicle-like tolerability support routine-use development.

Evidence anchors: Fluhr 1999; Kwon 2018, TEWL and hydration.

FIRMING AND DENSITY CREAM

Ultrasound and explant evidence concerning thickness, elasticity and matrix recovery informs firmness concepts.

Evidence anchors: Diridollou 1999; Boisnic 1999.

EVEN-TONE SERUM

Significant melanin-index reduction at 0.1% and reported depigmenting activity support a concentration-specific concept.

Evidence anchors: Kwon 2018; Sorg 2013.

CLARIFYING CARE FOR BLEMISH-PRONE SKIN

C. acnes activity and comedolytic findings provide mechanistic support for pore-focused formulations.

Evidence anchors: Pechère 1999; Fort-Lacoste 1999.

EYE-AREA RENEWAL CARE

The source proposes retinal’s efficacy and tolerability profile as a development rationale for thin, sensitive skin around the eyes.

Evidence anchor: the cited tolerability literature.

Concepts only. Validate all claims in the final marketed product. Evidence anchors refer to the skin-benefit studies reviewed above.

PART V · FORMULATION AND APPLICATIONS

Scalp-care concepts

Four dosage-form concepts explore stabilized retinal for scalp care while retaining the limits of the evidence.

LEAVE-ON SCALP SERUM

A night-care concept for surface renewal and comfort, informed by retinal epidermal biology and tolerability literature.

BALANCING TONIC FOR OILY, CONGESTION-PRONE SCALPS

Reported C. acnes activity and follicular keratinization mechanisms support a clean, balanced follicular-environment concept.

INTENSIVE PRE-WASH CARE

A weekly concentrated step in an aqueous base, with active retention as a formulation-development objective.

CONDITIONER AND HAIR-MASK ADDITION

Explore rinse-off systems. Guest release and rinse compatibility require joint engineering by the brand and PuriPharm.

Concepts only. Use scalp-condition wording. The cited evidence does not support hair-growth, density-increase or hair-loss-prevention claims.

PART V · FORMULATION AND APPLICATIONS

Patent evidence: what the documents show

CN 103987391 B: a granted Chinese patent showing retinal–cyclodextrin acetal conjugate structures.

CN 103987391 B patent family: exocyclic retinal–cyclodextrin hemiacetal structure (VIII).

CN 103987391 B patent family: endocyclic structure (VII).

INTERPRETING THE RECORD

Patent documents cover both noncovalent inclusion complexes and covalent conjugates. PuriActives® Crystal Retinal is positioned as a molecular inclusion complex based on physical equilibrium. Related patent test data are discussed in the stability and patent-history sections.

Figures reproduced from granted patent documents for technical discussion: CN 103987391 B; the source also cites the US 10,864,148 B2 family. Patent structures and comparisons are not product specifications for Crystal Retinal.

PART VI · COMMERCIAL POSITIONING

One ingredient, four value pillars

MOLECULAR STABILIZATION

Cyclodextrin inclusion reduces environmental exposure of retinal’s conjugated system, informed by host–guest chemistry and retinoid-stabilization patents.

EFFICACY INFORMED BY RETINOIC ACID COMPARISONS

One metabolic step from the active form, with randomized cosmetic-concentration studies on texture, wrinkles, barrier function, hydration and pigmentation.

FORMULATION FLEXIBILITY

Inclusion enables exploration of creams, aqueous serums and scalp formats, with guest release at the skin interface as the development rationale.

A DOCUMENTED SCIENTIFIC STORY

Peer-reviewed clinical literature, patent tests and receptor biology provide a framework for claim development and review.

PRODUCT & PARTNERSHIP

Retinal science. The possibilities of molecular inclusion.

PuriActives® Crystal Retinal Cyclodextrin-Included Retinal combines a direct cosmetic retinoid precursor with molecular stabilization for skin and scalp formulation development.

PuriPharm Co., Ltd.

PuriActives® Crystal Retinal · INCI: RETINAL

Samples, technical documentation and development support available on request.

www.puriactives.com

This report is intended for professionals and summarizes published research and granted patent documents. Data characterize the retinal active class and the cited test materials. Finished-product claims require product-level validation.

NanoActive Oleu™

NanoActive Oleu™

PuriPharm Co., Ltd. · Technical Report

Liposomal Oleuropein

Mediterranean polyphenol defense

Enhanced by delivery science

INCI: OLEA EUROPAEA (OLIVE) LEAF EXTRACT

Powered by PURISOME® FlexVes™ Liposome Technology

01 · INGREDIENT OVERVIEW

NanoActive Oleu™ at a glance

PRODUCT NAME:NanoActive Oleu™ Liposomal Oleuropein

INCI NAME:Olea Europaea (Olive) Leaf Extract

BOTANICAL SOURCE:Leaves of Olea europaea L.

KEY PHYTOCHEMICAL:Oleuropein, a secoiridoid polyphenol

DELIVERY PLATFORM:PURISOME® FlexVes™ Liposome Technology

PHYSICAL FORM:Liposomal dispersion for aqueous and emulsified systems

APPLICATION AREAS:Skincare · Oral care · Hair and scalp care

PRODUCT POSITIONING:An oleuropein-rich olive leaf extract encapsulated in flexible liposomal vesicles. NanoActive Oleu™ brings Mediterranean polyphenol science to formulation-ready skin, oral and scalp care concepts, informed by human, in vivo and mechanistic research.

Young olive leaves (Olea europaea L.), the botanical source of the actives.

02 · BOTANICAL ORIGIN

Olive leaves: a concentrated source of polyphenols

Olive branch with young leaves and fruit. Leaves are the tree’s richest source of phenolic compounds.

60–90 mg oleuropein per g of dry leaves

The olive tree concentrates its defensive chemistry in its leaves. Oleuropein, the predominant secoiridoid polyphenol, can reach 60–90 mg/g of dry leaves, alongside hydroxytyrosol, verbascoside and flavonoid glycosides.

This phytochemical system evolved under sunlight, microbial and oxidative stress, providing a botanical rationale relevant to daily challenges faced by skin, oral mucosa and scalp.

Nediani C, et al. Antioxidants. 2019;8(12):578. doi:10.3390/antiox8120578

Omar SH. Sci Pharm. 2010;78(2):133–154.

03 · KEY ACTIVE MOLECULE

Oleuropein: secoiridoid chemistry for redox activity

Oleuropein (molecular weight 540.5): hydroxytyrosol + elenolic acid + glucose. Nediani C, et al. Antioxidants. 2019;8:578.

CATECHOL CORE

The catechol hydroxyls of the hydroxytyrosol moiety donate hydrogen atoms to neutralize free radicals.

ACTIVE PRODUCTS OF HYDROLYSIS

Ester hydrolysis releases hydroxytyrosol and elenolic acid, extending the molecule’s functional profile.

NATURAL HYDROPHILICITY

A water-soluble glycoside with biological activity, but limited passage through lipid-rich barriers without delivery support.

This chemistry provides the rationale for complementary delivery engineering.

04 · DELIVERY CHALLENGES

Active polyphenols face practical delivery challenges

CHEMICAL INSTABILITY

Oleuropein’s ester bonds and catechol groups are susceptible to hydrolysis and oxidation, potentially reducing activity during shelf life.

BARRIER MISMATCH

Hydrophilic glycosides partition poorly into lipid-rich stratum corneum and mucosal surfaces, limiting local bioavailability.

SHORT RESIDENCE TIME

Unencapsulated polyphenols can be diluted, metabolized or washed away quickly, particularly in the oral environment.

FORMULATION CONSTRAINTS

Oxidation-sensitive polyphenols constrain pH, processing, packaging and preservative-system design.

DELIVERY APPROACH

Delivery science aims to turn a fragile molecule into a robust, formulation-ready ingredient.

PURISOME® FlexVes™ Liposome Technology

The proprietary liposomal platform behind the NanoActive™ ingredient range is introduced below.

Stability reference: Perugini P, et al. Int J Cosmet Sci. 2008;30(2):113–120.

05 · DELIVERY PLATFORM

PURISOME® FlexVes™ Liposome Technology

Flexible phospholipid vesicles: PuriPharm’s delivery architecture.

PuriPharm’s proprietary platform encapsulates oxidation-sensitive polyphenols in flexible liposomal vesicles, with four proposed formulation benefits.

01 · PROTECTION

Protect actives vulnerable to oxidation and degradation to support shelf life.

02 · PENETRATION

Promote stratum corneum penetration and improve bioavailability.

03 · RELEASE

Provide sustained, controlled release to reduce irritation risk.

04 · COMPATIBILITY

Improve formulation compatibility and skin feel.

PuriPharm Co., Ltd. has more than ten years of liposome R&D experience.

06 · INTEGRATED VALUE

One ingredient, a complete value framework

01

OLIVE LEAVES

BOTANICAL SOURCE

Olea europaea L. leaves, the tree’s most polyphenol-rich plant part.

02

PHYTOCHEMISTRY

ACTIVE FOUNDATION

An oleuropein-rich polyphenol system with published evidence across multiple pathways.

03

PURISOME®

DELIVERY ENGINEERING

FlexVes™ liposomal protection, penetration and controlled release.

04

FORMULATION FIT

FLEXIBLE USE

Dispersion for incorporation into emulsions, gels, serums and oral-care bases.

05

SKIN · ORAL · SCALP

APPLICATION AREAS

Three care areas, each with its own relevant evidence base.

Botanical chemistry informs delivery engineering, delivery supports formulation design, and formulations translate the concept into three care areas.

07 · MECHANISM OVERVIEW

Five pillars of cellular defense

WHY FIVE PILLARS?

UV exposure, pollution, microorganisms and mechanical stress can occur together and converge on shared cellular mechanisms.

Oleuropein research addresses this network from radical scavenging to cellular quality control.

Mechanisms and supporting evidence are reviewed below.

REDOX DEFENSE

Direct radical scavenging and support for endogenous antioxidant systems.

INFLAMMATORY MODULATION

Modulation of NF-κB-related signaling and key inflammatory mediators.

CELLULAR QUALITY CONTROL

Autophagy and proteostasis pathways involving AMPK, mTORC1, SIRT1 and TFEB.

TISSUE REPAIR

Support for re-epithelialization, collagen deposition and VEGF signaling.

MICROBIAL BALANCE

Published inhibitory activity against biofilm-forming, cariogenic oral bacteria.

Mechanistic framework: Nediani C, et al. Antioxidants. 2019;8(12):578.

07 · MECHANISM: REDOX DEFENSE

Quantifying radical-scavenging activity

IN VITRO EVIDENCE

Oleuropein scavenges DPPH radicals in a concentration-dependent manner, with a curve approaching that of the reference antioxidant ascorbic acid. Complementary ABTS assays also support anti-radical activity.

CHEMICAL RATIONALE

· Catechol hydroxyl groups donate hydrogen atoms to neutralize radicals.

· The resulting ortho-quinone structure is resonance-stabilized.

· Hydrolysis releases hydroxytyrosol, contributing further activity.

In vitro radical-scavenging activity provides a rationale for using PURISOME® delivery to improve contact with sites of UV- and pollution-related oxidative stress.

DPPH radical-scavenging activity: oleuropein (●) versus ascorbic acid (○, reference). Perugini P, et al. Int J Cosmet Sci. 2008;30(2):113–120.

Dose-dependent radical scavenging is the first mechanistic step, upstream of inflammation, barrier damage and visible aging.

07 · MECHANISM: INFLAMMATORY MODULATION

Interrupting the oxidative stress–inflammation cycle

Oxidative stress–autophagy–inflammation network. The indicated molecular markers are discussed in the oleuropein literature. Adapted from Nediani C, et al. Antioxidants. 2019;8(12):578.

NF-κB SIGNALING

Modulated upstream of cytokine-cascade amplification.

COX-2 AND iNOS

These inflammatory enzymes are downregulated in experimental models.

IL-6 · TNF-α · IL-1β

Key inflammatory mediators are reduced in cellular and tissue studies.

ICAM-1 · VCAM-1

Reduced adhesion-molecule expression is associated with less immune-cell recruitment and inflammation.

Oleuropein acts at the oxidative entry point of the cycle, providing an upstream intervention rationale.

07 · MECHANISM: CELLULAR QUALITY CONTROL

Autophagy as a quality-control mechanism

Autophagy is the cellular recycling system that identifies and clears damaged proteins and organelles. Oleuropein has been reported as an autophagy inducer in several experimental models.

01

STRESS SENSING

AMPK activation increases, while the mTORC1 brake on autophagy is reduced.

AMPK ↑ · mTORC1 ↓

02

AUTOPHAGY INITIATION

Beclin-1 participates; LC3-I converts to LC3-II as autophagosomes form.

Beclin-1 · LC3-II ↑

03

SUBSTRATE CLEARANCE

p62 directs damaged proteins and organelles toward lysosomal degradation.

p62 turnover ↑

04

CELLULAR RENEWAL

SIRT1 and TFEB support lysosomal biogenesis and cellular renewal.

SIRT1 · TFEB ↑

This cellular clearance mechanism provides a distinctive basis for botanical active development.

Autophagy markers: Nediani C, et al. Antioxidants. 2019;8(12):578. doi:10.3390/antiox8120578

07 · MECHANISM: PROTEOSTASIS

Proteostasis support for lasting skin quality

THE PROTEOSTASIS PERSPECTIVE

The proteostasis network, including synthesis, folding, repair and degradation, maintains functional proteins. Under chronic environmental stress, damaged material can accumulate faster than cells can clear it.

Oleuropein is positioned on both sides of this balance: antioxidant defense slows damage formation, while autophagy induction supports clearance.

Formulation implication: ingredients that support cellular quality control provide a rationale for long-term skin resilience as well as repair.

Proteostasis and autophagy framework: Nediani C, et al. Antioxidants. 2019;8(12):578.

08 · SKINCARE: HUMAN EVIDENCE

Human evidence under UVB stress

STUDY DESIGN

MODEL

UVB-induced erythema in human volunteers, a controlled photobiology challenge model.

TEST FORMULATIONS

Topical oleuropein emulsions and emulgels applied after UVB exposure.

REFERENCE

Vitamin E, a topical antioxidant benchmark.

OBJECTIVE ENDPOINTS

· Erythema index: reflectance colorimetry

· TEWL: transepidermal water loss

· Skin blood flow: laser Doppler flowmetry

WHY THE DESIGN MATTERS

The controlled UVB challenge uses objective biophysical measurements in human volunteers rather than self-assessment.

It evaluates whether the test formulations can help limit redness and preserve barrier function after a defined oxidative challenge.

Perugini P, et al. Int J Cosmet Sci. 2008;30(2):113–120. doi:10.1111/j.1468-2494.2007.00416.x

08 · SKINCARE: HUMAN EVIDENCE

Approximately 35% lower TEWL after UVB exposure

–35%

TEWL: measurable preservation of barrier function

–22%

Erythema index: reduced visible redness

–30%

Skin blood flow: reduced hyperemic response

Approximate mean reductions versus the UVB-exposed control, for oleuropein emulsions and emulgels. Perugini P, et al. Int J Cosmet Sci. 2008;30(2):113–120.

Transepidermal water loss (TEWL)

Erythema index (colorimetry)

Blood flow (laser Doppler)

Three instrumental endpoints support reduced redness, barrier disruption and vascular response under the tested conditions.

08 · SKINCARE: HUMAN EVIDENCE

From acute photostress to photoaging care

The controlled UVB study provides a rationale for daily photoaging care. Longer-term human data on an olive leaf extract cream extend the evidence beyond an acute challenge.

LONGER-TERM HUMAN DATA: OLIVE LEAF EXTRACT CREAM

36 female volunteers; twice daily for 2 months:

· TEWL decreased significantly (p = 0.007), with the effect maintained 1 month after discontinuation.

· Skin hydration increased (p = 0.004).

· Wrinkle parameters improved (p < 0.001).

Visioscan® skin surface images: baseline (A), 1 month (B), 2 months (C), and 1 month after discontinuation (D).

Wanitphakdeedecha R, et al. J Cosmet Dermatol. 2020. doi:10.1111/jocd.13457

08 · SKINCARE: PRECLINICAL EVIDENCE

Tissue repair and matrix renewal

Van Gieson staining of collagen deposition in healing skin: oleuropein-treated versus control groups. Mehraein F, et al. Cell J. 2014;16(1):25–30.

VEGF protein expression by Western blot: oleuropein group (Tg) versus control group (Cg).

Increased VEGF supports microvascular supply to repairing tissue and provides a mechanistic link with matrix renewal.

RESULTS IN AN AGED-SKIN MODEL

Wound closure at day 3: 29.0% versus 19.2% in controls.

At day 7: 55.3% versus 45.3% in controls.

Re-epithelialization was complete by day 7 in treated skin.

Collagen deposition increased; VEGF increased (p < 0.05).

Patent support: EP2570124A1 covers oleuropein compositions for repair of aged and fragile skin.

Intradermal model in aged mice: preclinical evidence, not a human efficacy claim.

08 · SKINCARE: HUMAN AND IN VITRO EVIDENCE

Even skin tone: observations in melanin biology

Melanin content in primary human melanocytes (in vitro).

Intracellular glutathione (in vitro).

Age-spot melanin index versus baseline (D0) in a 12-week human study.

Placebo versus test product at week 12.

IN VITRO: HUMAN MELANOCYTES

Melanin content decreased by up to approximately 65%, while intracellular glutathione increased by 55%, supporting the cellular redox-buffering system.

HUMAN STUDY: AGE SPOTS

In a 12-week double-blind, placebo-controlled study of 12 women aged 46–72 years, the age-spot melanin index decreased by 34.8% at week 12 versus baseline, with visible lightening.

The source connects skin-tone care with the redox rationale used for barrier defense.

Standardized olive polyphenol extract. Lueder M. Cosmet Sci Technol. 2011.

09 · ORAL CARE

The mouth: a redox–microbial ecosystem

Biofilms reform within hours, saliva continuously dilutes actives, and soft tissues face daily mechanical, chemical and microbial stress. Oral care therefore requires both suitable chemistry and effective delivery.

BIOFILM AND PLAQUE

Bacterial biofilms drive plaque accumulation and acid challenges. Daily biofilm control provides an application opportunity for polyphenols.

GINGIVAL ENVIRONMENT

The gingival margin lies at the intersection of microbial and oxidative stress. Redox support and inflammatory modulation provide relevant development pathways.

SOFT-TISSUE REPAIR

Mucosal tissues face daily irritation and discomfort after care procedures. Repair support is a relevant consumer-care concept.

Three application opportunities share the same polyphenol rationale: antioxidant activity, inflammatory modulation and microbial inhibition.

09 · ORAL CARE: IN VITRO EVIDENCE

Published activity against key oral bacteria

In vitro data support a biofilm-management concept and do not constitute therapeutic claims.

Karygianni L, et al. Biomed Res Int. 2014;2014:839019. doi:10.1155/2014/839019.

S. mutans: Golestannejad Z, et al. Dent Res J (Isfahan). 2020;17(3):179–185. doi:10.4103/1735-3327.284730 (acid production and adhesion: p < 0.001).

09 · ORAL CARE: HUMAN EVIDENCE

Biofilm management beyond disinfection

PLAQUE REGROWTH: CROSSOVER CONTROLLED STUDY, N = 17

36% lower plaque index versus water rinsing

After rinsing with a virgin olive oil preparation containing oleuropein, the plaque index was 1.48 ± 0.36 versus 2.30 ± 0.39 with water (p < 0.001), measured in a plaque-regrowth crossover design.

Volunteers suspended oral hygiene and underwent objective plaque-regrowth scoring, providing a direct measure of biofilm management under the study conditions.

Math MV, et al. Int J Dent Health Sci. 2017;4(4).

THE POLYPHENOL RATIONALE FOR BIOFILM CARE

INTERFERING WITH ADHESION

Olive leaf polyphenols reduce S. mutans surface adhesion (p < 0.001).

MODULATING ACID PRODUCTION

Reduced acid production by cariogenic bacteria supports a daily-care rationale relevant to enamel.

REDOX SUPPORT AT THE GINGIVAL MARGIN

Antioxidant activity at the biofilm–gingiva interface provides a rationale for comfort-oriented care.

Golestannejad Z, et al. Dent Res J (Isfahan). 2020;17(3):179–185.

09 · ORAL CARE: CLINICAL AND PRECLINICAL EVIDENCE

Oral soft-tissue defense: cytokines and comfort

Mucosal histopathology scores over time: oleuropein versus controls in a mucositis model.

Tissue MDA, a marker of oxidative damage: oleuropein versus controls (reported p = 0.000).

CLINICAL: RANDOMIZED CROSSOVER TRIAL, 25 PATIENTS

Olive leaf extract mouthwash reduced salivary IL-1β and TNF-α and was associated with lower mucositis severity scores in chemotherapy patients.

PRECLINICAL: MUCOSITIS MODEL

Oleuropein ointment reduced histopathology scores and tissue MDA (reported p = 0.000), indicating less tissue damage and oxidative stress in the experimental mucosal challenge.

Positioning: supportive oral care and comfort. Use adjunctive wording rather than therapeutic claims.

Ahmed KM. Saudi Dent J. 2013;25(4):141–147. doi:10.1016/j.sdentj.2013.09.001.

Showraki N, et al. J Dent (Shiraz). 2016;17(4):334–342.

09 · ORAL CARE: DELIVERY SCIENCE

Why delivery matters in oral care

FOUR ORAL-ENVIRONMENT CHALLENGES

Continuous dilution: saliva washes actives away.

Short contact time: rinsing lasts minutes rather than hours.

Oxidative exposure: polyphenols are vulnerable to degradation in aqueous systems.

Dosage-form constraints: clear rinses, gels and pastes have different formulation requirements.

THE PURISOME® APPROACH

· Vesicles protect polyphenols within the formulation.

· Controlled release aims to extend availability after use.

· The dispersion format suits rinses, gels and pastes.

SUPPORTING LITERATURE

Liposomal encapsulation of olive leaf polyphenols preserved, and under some conditions enhanced, antibacterial activity against S. aureus, including MRSA (MIC 140–240 µg/mL). Vesicles remained stable for up to 90 days at 4 °C.

Prevete G, et al. ACS Appl Mater Interfaces. 2024;16(50):68850–68863. doi:10.1021/acsami.4c13302

10 · HAIR AND SCALP CARE

The scalp: a stressed follicular environment

The scalp is skin with approximately 100,000 follicles, abundant sebum and direct UV exposure, creating a concentrated set of environmental challenges.

PHOTOSTRESS

UV exposure is particularly relevant at partings and areas of thinning hair.

SEBUM OXIDATION

Lipid peroxidation at follicular openings increases the oxidative load.

MICROBIAL PRESSURE

A dense, sebum-supported microbial community contributes to ongoing surface challenges.

FOLLICULAR CYCLE

Transition into anagen is sensitive to oxidative and inflammatory signaling.

Scalp care can draw on the same defensive mechanisms relevant to skin care.

10 · HAIR AND SCALP CARE

Oleuropein as a rationale for scalp resilience

REDOX DEFENSE

Radical scavenging at the scalp surface, where sebum oxidation and UV exposure converge.

Supporting evidence: in vitro and human skin data.

INFLAMMATORY MODULATION

A rationale for perifollicular comfort through modulation of inflammatory mediators.

Supporting evidence: mechanistic studies and human oral-care data.

MICROBIAL BALANCE

Published antibacterial activity against biofilm-forming organisms.

Supporting evidence: in vitro MIC data.

QUALITY CONTROL

Autophagy support as a concept for rapidly dividing cells in the follicular environment.

Supporting evidence: mechanistic literature.

FOLLICULAR SIGNALING

Wnt/β-catenin activation in dermal papilla cells, detailed below.

Supporting evidence: preclinical data.

Each scalp-care pillar is presented with its supporting evidence type.

10 · HAIR AND SCALP: PRECLINICAL EVIDENCE

Follicular biology: Wnt/β-catenin activation

Nanovesicle enrichment through the follicular route: a PURISOME® delivery concept.

HUMAN DERMAL PAPILLA CELLS: IN VITRO

Oleuropein promoted dermal papilla cell proliferation, increased LEF1 and Cyclin D1, and drove nuclear β-catenin accumulation, consistent with Wnt pathway activation.

TELOGEN MOUSE MODEL: TOPICAL APPLICATION FOR 28 DAYS

Anagen entry accelerated, with larger and more numerous follicles. Wnt10b, FzdR1, LRP5, IGF-1, KGF, HGF and VEGF increased in skin tissue.

Evidence level: preclinical. These findings support scalp-care positioning and further development, not a human hair-growth claim.

Tong T, Kim N, Park T. PLoS ONE. 2015;10(6):e0129578. doi:10.1371/journal.pone.0129578

11 · APPLICATIONS

Three application areas, one technology platform

SKINCARE

DEFENSE AND REPAIR

· Human UVB study: TEWL –35%; erythema –22%.

· Photoaging care: TEWL p = 0.007; wrinkles p < 0.001.

· Even tone: age-spot melanin index –34.8%.

· Tissue repair: preclinical wound models.

ORAL CARE

BIOFILM AND SOFT-TISSUE BALANCE

· Antibacterial activity: published MIC/MBC values.

· Human crossover study: plaque regrowth –36%.

· Clinical rinse study: reduced salivary IL-1β and TNF-α.

· Mucosal comfort: preclinical mucositis model.

HAIR AND SCALP

RESILIENCE AND FOLLICULAR SUPPORT

· Wnt/β-catenin activation: preclinical.

· Follicular delivery: PURISOME® concept.

· Redox and microbial rationale: evidence from skin and oral studies.

One ingredient concept connects three care areas through a shared scientific rationale.

11 · APPLICATIONS

From ingredient to formulation: product concepts

SKINCARE

Daily defense serum

After-sun repair emulgel

Even-tone concentrate

Barrier-support lotion

Informed by human UVB, photoaging and skin-tone studies.

ORAL CARE

Daily defense mouthwash

Gingival-care gel

Biofilm-management toothpaste

Soothing rinse after care procedures

Informed by antibacterial, plaque and cytokine evidence.

HAIR AND SCALP

Pre-wash scalp concentrate

Leave-on scalp serum

Clarifying antioxidant shampoo

Informed by preclinical follicular data and the scalp-stress rationale.

These are concepts for joint development. Final product claims require testing of the finished formulation.

11 · APPLICATIONS

NanoActive Oleu™ formulation guidance

HANDLING PRINCIPLES

Supplied as an aqueous liposomal dispersion, with no reconstitution required.

Add during cool-down. Avoid prolonged high shear to protect vesicle integrity.

Suitable formulation areas include emulsions, serums, gels and oral-care systems.

Use mild temperatures and pH conditions; validate the preservative system in the complete formulation.

Detailed specifications, recommended use levels and starter formulations are available from PuriPharm technical services.

WORKING WITH PURIPHARM

Ingredient supply with joint development support.

PuriPharm provides application expertise, formulation guidance and supporting evidence documentation, from the first prototype to market-registration materials.

Contact PuriPharm Co., Ltd. for technical services and joint development.

NANOACTIVE OLEU™ LIPOSOMAL OLEUROPEIN

Protect · Balance · Renew

PHYTOCHEMISTRY: oleuropein-rich Mediterranean polyphenols

DELIVERY: PURISOME® FlexVes™ Liposome Technology

EVIDENCE: published human, in vivo and mechanistic studies

PARTNERSHIP: joint development with PuriPharm Co., Ltd.

NanoActive Oleu™

Powered by PURISOME® FlexVes™ Liposome Technology

PuriPharm Co., Ltd.

REFERENCES

Key references

01 Perugini P, et al. Lenitive effect of oleuropein on UVB-induced erythema. Int J Cosmet Sci. 2008;30(2):113–120. doi:10.1111/j.1468-2494.2007.00416.x

02 Nediani C, et al. Oleuropein, autophagy and oxidative stress–inflammation interplay. Antioxidants. 2019;8(12):578. doi:10.3390/antiox8120578

03 Wanitphakdeedecha R, et al. Olive leaf extract cream: TEWL, hydration and wrinkle outcomes. J Cosmet Dermatol. 2020. doi:10.1111/jocd.13457

04 Mehraein F, et al. Oleuropein and skin tissue recovery in an aged-mouse model. Cell J. 2014;16(1):25–30.

05 Lueder M. Standardized olive polyphenol extract: melanin, glutathione and age-spot studies. Cosmet Sci Technol. 2011.

06 Karygianni L, et al. Olive leaf extract against oral pathogens. Biomed Res Int. 2014;2014:839019. doi:10.1155/2014/839019

07 Golestannejad Z, et al. Olive leaf extract vs Streptococcus mutans. Dent Res J (Isfahan). 2020;17(3):179–185. doi:10.4103/1735-3327.284730

08 Math MV, et al. Plaque regrowth crossover with virgin olive oil rinse. Int J Dent Health Sci. 2017;4(4).

09 Ahmed KM. Olive leaf extract mouth rinse: IL-1β, TNF-α and mucositis severity. Saudi Dent J. 2013;25(4):141–147. doi:10.1016/j.sdentj.2013.09.001

10 Showraki N, et al. Oleuropein in a chemotherapy-induced mucositis model. J Dent (Shiraz). 2016;17(4):334–342.

11 Tong T, Kim N, Park T. Oleuropein and hair-follicle Wnt/β-catenin signaling. PLoS ONE. 2015;10(6):e0129578. doi:10.1371/journal.pone.0129578

12 Prevete G, et al. Liposomal encapsulation of olive leaf polyphenols. ACS Appl Mater Interfaces. 2024;16(50):68850–68863. doi:10.1021/acsami.4c13302

13 Omar SH. Oleuropein in olive and its pharmacological effects. Sci Pharm. 2010;78(2):133–154.

14 EP2570124A1. Oleuropein compositions for healing wounds and ulcers in elderly people and/or diabetics.

These references concern oleuropein or olive leaf preparations in published studies and patent documents. Evidence types are identified in the relevant sections. PURISOME®, FlexVes™, NanoActive™ and Oleu™ are trademarks of PuriPharm Co., Ltd.

PuriActives® AlgiSulf

PuriActives® AlgiSulf

PURIPHARM CO., LTD.

Sodium Algin Sulfate · INCI: SODIUM ALGIN SULFATE

Marine sulfated polysaccharide technology for premium skin and scalp care

For cosmetic formulators, R&D scientists, innovation teams and brand developers · www.puriactives.com

OVERVIEW

From marine chemistry to skin and scalp applications

PuriActives® AlgiSulf (INCI: Sodium Algin Sulfate) is a marine-derived sulfated polysaccharide built on a brown-algal alginate backbone.

This article reviews alginate sulfation chemistry, structure–activity relationships and published evidence relevant to moisturization, barrier support, soothing, antioxidant activity and extracellular matrix care, with extensions to scalp health and hair conditioning.

Research findings are integrated into the mechanisms described below. Source notes accompany each section, with the reference list at the end.

I · SCIENTIFIC FOUNDATIONS

Marine polysaccharide science

Product introduction and INCI identity

Alginate structure and sulfation

Structure–activity relationships

Integrated mechanisms

II · SKIN APPLICATIONS

Skin moisturization and conditioning

Skin barrier support

Soothing and inflammatory pathways

Antioxidant protection

Skin aging and the extracellular matrix

Key scientific evidence

III · SCALP AND HAIR

Rationale for scalp care

Scalp hydration and comfort

Scalp oxidative stress

Hair conditioning

Skin–scalp synergy

IV · APPLICATIONS

Technical properties

Formulation and processing

Application areas

Evidence matrix

Value proposition and references

01 · MARINE SCIENCE

Brown-algal chemistry refined through sulfation

Kelp forests: source ecosystems for brown-algal polysaccharides

Marine algae produce structurally distinctive carbohydrates. Brown algae (Phaeophyceae) use alginate in cell walls and intercellular matrices. This linear polyuronide provides both strength and flexibility in moving seawater.

Marine sulfated polysaccharides, including fucoidan, carrageenan and ulvan, have been widely studied for skin-related benefits. Associations between sulfate content and biological activity are frequently reported.

MARINE CARBOHYDRATE LANDSCAPE

Sodium Algin Sulfate combines an alginate backbone with sulfation characteristic of marine polysaccharides.

Sources: Ngo & Kim, Int. J. Biol. Macromol. 2013; Kim et al., Mar. Drugs 2018.

02 · PRODUCT IDENTITY

One ingredient for skin and scalp care

PuriActives® AlgiSulf is the sodium salt of sulfated alginic acid: a water-soluble anionic polysaccharide produced by controlled sulfation of brown-algal alginate.

Sulfate half-esters introduced onto the uronic-acid backbone increase anionic charge density, giving the structural polymer glycosaminoglycan-like and heparin-like biological interaction properties.

FUNCTIONAL PROFILE

● Moisturization and film formation: the hydroxyl-rich polyuronide binds water at the skin surface.

● Soothing and antioxidant properties: chemokine affinity and sulfation-associated radical scavenging.

● ECM biomimetic support: heparin-like affinity for matrix-related proteins.

● Skin and scalp versatility: one INCI for facial, scalp and hair applications.

PRODUCT IDENTIFICATION

Distinct from unmodified alginate (INCI: Algin / Sodium Alginate), which contains no sulfate groups.

Source: Arlov & Skjåk-Bræk. Molecules 2017;22:778.

03 · MOLECULAR STRUCTURE

The alginate backbone and what sulfation changes

Schematic: (1→4)-linked β-D-mannuronic acid (M) and α-L-guluronic acid (G) residues. Gold bonds indicate sulfate half-esters at C2/C3 hydroxyl groups.

Published figure: chemical sulfation routes for alginate M/G residues (HClSO₃/formamide; SO₃/pyridine; H₂SO₄/DMF). Arlov & Skjåk-Bræk. Molecules 2017;22:778 (CC BY).

BACKBONE STRUCTURE

Alginate is a linear copolymer of M and G units arranged in MM, GG and alternating MG blocks. Block composition affects chain flexibility and ion binding. G blocks associate around Ca²⁺ to form the classic “egg-box” gel structure.

SULFATION CHEMISTRY

Chemical sulfation converts C2/C3 hydroxyl groups into sulfate half-esters (–O–SO₃⁻Na⁺), introducing additional anionic groups on the residues and producing a strongly acidic polyelectrolyte with a heparin-like spatial charge distribution.

Sources: Arlov & Skjåk-Bræk. Molecules 2017. DOI: 10.3390/molecules22050778; Mutch et al. 2024.

04 · STRUCTURE–ACTIVITY RELATIONSHIPS

Degree of sulfation shapes biological properties

Charge density influences protein affinity. Greater sulfation increases anionic charge along the chain and strengthens interactions with heparin-binding proteins, including growth factors, chemokines and coagulation factors (Biomacromolecules 2014).

Radical scavenging increases with sulfation. In human chondrocyte and macrophage models, superoxide scavenging by sulfated alginate correlates directly with the degree of substitution: more sulfate groups produce a stronger antioxidant response (Biomater. Sci. 2017).

Sequence and molecular weight regulate performance. M/G composition, block length and molecular weight shape chain conformation, flexibility and binding geometry. Sequence-defined samples show measurable differences in heparin-like behavior (Molecules 2017).

SODIUM ALGIN SULFATE VS UNMODIFIED SODIUM ALGINATE

Sources: Arlov et al. Biomacromolecules 2014; Kerschenmeyer et al. Biomater. Sci. 2017.

05 · MECHANISMS

Integrated mechanisms of action

Sodium Algin Sulfate

Anionic sulfated polyuronide

HYDRATION AND FILM FORMATION

Hydroxyl and ionic groups bind water. The polymer forms a flexible, breathable conditioning film at the surface.

SOOTHING SIGNALS

Heparin-like affinity can sequester pro-inflammatory chemokines (IL-8, MCP-1) and modulate inflammatory cell behavior.

ANTIOXIDANT DEFENSE

Sulfate-rich chains scavenge superoxide radicals in a sulfation-dependent manner.

ECM BIOMIMETIC SUPPORT

Glycosaminoglycan-like interactions with matrix proteins and growth factors (FGF-2, VEGF, TGF-β1) support the dermal matrix environment.

One anionic backbone provides four complementary mechanisms relevant to skin and scalp care.

Sources: Huang et al. J. Nanobiotechnol. 2023; Freeman et al. Biomaterials 2008.

06 · SKIN APPLICATIONS: HYDRATION

Skin moisturization and conditioning

The structure of sulfated polyuronides supports water management. Dense hydroxyl, carboxylate and sulfate groups form hydrogen-bonding and ion–dipole interactions with water at the skin surface.

MOLECULAR WATER BINDING

Each residue carries hydroxyl groups, a carboxylate group and up to two sulfate half-esters. The source positions this as a high charge density among cosmetic polysaccharides, supporting hydrophilicity and moisture retention.

SURFACE FILM

Alginate materials have long been used in wound dressings for their ability to maintain a moist interface. As a topical film former, the polymer can reduce water loss and smooth surface roughness.

SENSORY CONDITIONING

Reviews of marine carbohydrates report moisturizing, soothing and anti-aging benefits of algal polysaccharides. Alginate-family materials are known for moisture-retaining protective films.

FORMULATION IMPLICATIONS

AlgiSulf can serve as a moisturizing framework in water-based serums, concentrates, gel masks and scalp treatments, providing hydration, slip and a soft-focus film without a heavy occlusive feel. Its anionic character also supports pairing with cationic conditioning complexes in rinse-off products.

Sources: Kim et al. Mar. Drugs 2018;16:459; Yao & Xu. Polysaccharides 2022.

07 · SKIN APPLICATIONS: BARRIER

Skin barrier support

Barrier care begins at the surface. A coherent, hydrated polymer film protects the compromised stratum corneum, while related chemical interactions may modulate inflammatory and oxidative signals that interfere with recovery.

Moist protective interface. Alginate dressings maintain a moist, protected wound environment. Sulfated alginate hydrogels extend this platform in deep partial-thickness burn models, reducing excessive inflammation and supporting organized repair (preclinical).

Fibroblast compatibility. Alginate sulfate showed no cytotoxicity in mouse and human fibroblasts at 0.5–2% w/v, while reducing inflammatory mediator levels in the same cells. This provides a rationale for barrier-care development for reactive skin (in vitro).

Bioadhesive residence. Alginate-family polymers exhibit mucoadhesion and bioadhesion, potentially extending surface film residence, a useful property for leave-on barrier products and overnight masks (material-class evidence).

Barrier support through signaling. By binding IL-8 and MCP-1 and promoting a shift from M1 toward M2 macrophage phenotypes, sulfated alginate acts upstream of low-grade inflammation associated with disrupted barrier homeostasis (preclinical).

Sources: Huang et al. J. Nanobiotechnol. 2023; Balde & Nazeer. Colloids Surf. B 2025.

08 · SKIN APPLICATIONS: SOOTHING

Soothing and inflammatory pathways

Sulfated alginate mimics heparan sulfate. Its negative charge distribution attracts positively charged chemokine domains, potentially intercepting signals before inflammatory cells are recruited into tissue.

Published figure: unmodified sodium alginate from E. amentacea suppresses LPS-induced IL-1β, IL-6, IL-8, TNF-α and MCP-1 in THP-1 macrophages. Mar. Drugs 2026;24:41 (CC BY). DOI: 10.3390/md24010041.

CHEMOKINE SEQUESTRATION

● Sulfated alginate hydrogel platforms have high affinity for IL-8 and MCP-1 and reduce inflammatory cell infiltration (preclinical).

● Macrophage phenotypes shift from M1 toward M2, favoring resolution rather than escalation (preclinical).

INFLAMMATORY MEDIATOR MODULATION

● Alginate sulfate (0.5–2% w/v) reduces inflammatory mediators in mouse and human fibroblasts and inhibits protein denaturation (in vitro).

● Sulfated alginate hydrogels suppress IL-1β-induced inflammatory responses in human chondrocytes (in vitro).

BACKBONE EVIDENCE: UNMODIFIED SODIUM ALGINATE

For unmodified E. amentacea sodium alginate, reductions in THP-1 macrophages were IL-6: 46%; IL-8: 46%; MCP-1: 81%; TNF-α: 23%. iNOS inhibition in RAW 264.7 cells was 70–83%. These data describe the unsulfated backbone. The source separately proposes further enhancement through sulfation.

Sources: Huang 2023; Balde 2025; Arlov 2017; Mar. Drugs 2026;24:41.

09 · SKIN APPLICATIONS: ANTIOXIDANT ACTIVITY

Antioxidant protection

Reactive oxygen species contribute to skin aging and inflammation. Sulfation adds radical-scavenging activity to the alginate film platform, with activity increasing as sulfate content rises.

Published figure: DPPH scavenging (a), ferric reducing power (b) and NO scavenging (c) of unmodified E. amentacea sodium alginate. Mar. Drugs 2026;24:41 (CC BY). DOI: 10.3390/md24010041.

SULFATION-DEPENDENT SCAVENGING

Across sulfated alginate derivatives tested with human chondrocytes and macrophages, superoxide scavenging correlated directly with degree of sulfation, demonstrating a structure–activity relationship (in vitro).

The same study reported immunomodulatory effects, linking antioxidant activity with modulation of inflammatory signaling.

MARINE SULFATED POLYSACCHARIDES AS RADICAL SCAVENGERS

Sulfated polysaccharides from Laminaria japonica showed greater reducing power and radical scavenging at higher sulfate content and lower molecular weight. These are structural variables relevant to alginate sulfation (chemical assays).

QUANTITATIVE BACKBONE DATA: SODIUM ALGINATE

For the unsulfated backbone, DPPH scavenging reached 91% at 1.25 mg/mL (IC₅₀ ≈ 0.410 mg/mL). NO scavenging IC₅₀ was approximately 0.417 mg/mL. Ferric reducing power increased with dose to A₇₀₀ = 1.06. The source cites sulfation literature as a rationale for exceeding this baseline; the plotted data concern unsulfated alginate (chemical assays).

Sources: Kerschenmeyer 2017; Zhao et al. 2008; Mar. Drugs 2026;24:41.

10 · SKIN APPLICATIONS: AGING AND ECM

Skin aging and the extracellular matrix

Sulfated glycosaminoglycans participate in dermal matrix functions. Sulfated alginate uses related sulfate-patterned protein interactions and was originally developed for tissue repair applications.

Published figure: in vivo closure of deep partial-thickness burn wounds over days 0–21 using a tunable sulfated alginate hydrogel platform. Huang et al. J. Nanobiotechnol. 2023;21:305 (CC BY). DOI: 10.1186/s12951-023-02144-2.

GROWTH FACTOR AFFINITY

Sulfated alginate hydrogels bind heparin-binding growth factors, including FGF-2, VEGF and TGF-β1, with high affinity and provide sustained release, mimicking the ECM’s storage of regenerative signals (in vitro).

REPAIR KINETICS

Connective tissue growth factor-loaded alginate sulfate nanoparticles achieved 79.49% wound closure at 72 hours with 5 µg/mL CTGF, the fastest among the tested groups (in vitro scratch assay).

ENZYME-RELATED PROTECTION: RELATED SULFATED POLYSACCHARIDES

Marine sulfated polysaccharides from green and red algae inhibit elastase, collagenase and hyaluronidase in vitro, enzymes relevant to wrinkle formation and loss of firmness. The source uses this material-class behavior as a rationale for AlgiSulf’s sulfate-rich surface.

Sources: Freeman 2008; Karam 2024; Huang 2023; Falcao 2020.

11 · EVIDENCE REVIEW

Key scientific evidence and quantitative findings

These studies used research-grade sulfated alginate or related sulfated polysaccharides. The findings characterize the material class and support the mechanistic rationale for PuriActives® AlgiSulf.

SCALP & HAIR SCIENCE

PART II · SCALP AND HAIR SCIENCE

The scalp is skin.

The hair shaft is keratin.

Hydration, soothing and antioxidant mechanisms relevant to facial skin also inform scalp microenvironment care, with further applications based on the electrostatics of the keratin hair surface.

12 · RATIONALE FOR SCALP CARE

The scientific rationale for scalp care

The scalp has dense follicles, greater sebum production and a resident microbiota, all relevant to hair condition. Common concerns, including tightness, itching, flaking and oiliness, involve hydration, barrier function and inflammation, areas relevant to sulfated polysaccharide research.

SCALP STRESSORS

● Sebum oxidation and UV exposure create oxidative stress in scalp skin and hair.

● Malassezia metabolites, such as oleic acid, disrupt barrier homeostasis and promote flaking.

● Surfactant cleansing and styling remove surface lipids and water.

WHERE ALGISULF FITS

● A moisturizing film addresses scalp dehydration and tightness.

● Chemokine affinity provides a rationale for targeting the itch–inflammation axis.

● Sulfation-related radical scavenging may buffer oxidative stress.

● A non-biocidal polymer approach is positioned for ongoing scalp care.

PATENT PRECEDENT

A patent claims sulfated polysaccharides as non-irritating anti-dandruff actives to prevent Malassezia-associated excessive flaking. Reconstructed skin data show complete suppression of oleic-acid-induced desquamation (EP2794012B1).

This provides a cosmetic application precedent for sulfated polysaccharides in scalp care.

Patent figure: the first page of EP2794012B1, claiming sulfated polysaccharides as cosmetic anti-dandruff actives (international classifications A61Q 5/00 and A61K 8/73).

Sources: Trüeb. Int. J. Trichology 2009; EP2794012B1; DeAngelis et al. 2005.

13 · SCALP HYDRATION

Scalp hydration and comfort

A dehydrated scalp can feel tight or itchy and show fine flaking after frequent washing. AlgiSulf’s polymer-based rationale is to bind water, maintain a film and modulate associated signals.

A surface water reservoir. The sulfate–carboxylate–hydroxyl network binds water without relying on heavy emollients, an important consideration for scalp products that should not weigh down hair.

Comfort through chemokine modulation. IL-8 and MCP-1 help recruit inflammatory cells in irritated skin. Demonstrated sulfated alginate affinity for these chemokines provides a mechanistic route relevant to scalp comfort (preclinical).

A non-stripping approach to flaking. In a patent model, sulfated polysaccharides prevented oleic-acid-induced desquamation in reconstructed skin, reducing the score from 3 to 0. The approach addresses flaking pathways rather than killing scalp microorganisms (patent, ex vivo).

Gentle wash-day feel. A smooth anionic film can reduce friction during massage and rinsing, supporting comfort in shampoos, scalp treatments and pre-wash products for sensitive scalps.

Sources: Huang et al. 2023; EP2794012B1.

14 · SCALP MICROENVIRONMENT

Scalp oxidative stress and the microenvironment

Oxidative stress is a documented contributor to scalp and hair aging. UV exposure and sebum lipid peroxidation increase ROS at the follicular environment, affecting scalp condition and the quality of emerging hair.

THE SCALP OXIDATIVE CASCADE

UV + SEBUM

Light exposure and sebum peroxidation generate ROS at the scalp surface and follicular openings.

OXIDATIVE STRESS

ROS irritate scalp skin, contribute to microinflammation and oxidize hair surface lipids.

VISIBLE EFFECTS

Scalp sensitivity, dull hair and progressive loss of hair quality.

ALGISULF BUFFERING CONCEPT

Sulfation-associated radical scavenging is proposed to interrupt the cascade at the surface.

MICROBIOME-FRIENDLY POSITIONING

Dandruff-associated dysbiosis involves Malassezia and Staphylococcus overgrowth. The source describes recurrence after stopping conventional antifungal treatment. Sulfated polysaccharides offer a proposed complementary, non-biocidal pathway: limiting metabolite-triggered flaking while preserving the resident ecosystem.

Sources: Trüeb. Int. J. Trichology 2009; Kerschenmeyer 2017; EP2794012B1.

15 · HAIR SHAFT

Hair conditioning through electrostatic interactions

Hair keratin has a net negative charge at cosmetic pH. Anionic polysaccharides can reach the hair surface through association with cationic conditioning polymers, which promote deposition and retention.

COMPLEXATION IMPROVES SUBSTANTIVITY

Complexing anionic glycosaminoglycan-like polysaccharides with cationic cellulose (polyquaternium-type polymers) increased keratin-bound polymer after rinsing by up to tenfold, with zeta-potential evidence of deposition (in vitro, hair tresses). The source proposes the same architecture for anionic sulfated polyuronides.

FILM-BASED CONDITIONING

After deposition, the sulfated film provides the conditioning functions associated with hair-care polysaccharides: cuticle smoothing, improved combability, moisture retention and slip, without the heavy feel associated with silicone oils.

The water-binding network helps maintain hair hydration between washes.

FORMULATION TIP

Pair AlgiSulf with cationic conditioners in conditioners and hair masks to engineer deposition. In leave-on scalp serums, the anionic film may function independently. One ingredient supports two delivery approaches.

Source: Pavlichko et al. Int. J. Cosmet. Sci. 1994; PMID 19250478.

16 · SYNERGY

Skin–scalp synergy: one INCI across facial, scalp and hair care

For brand developers, this alignment supports a consistent ingredient story across facial care, scalp care and hair care product lines.

17 · TECHNICAL PROPERTIES

Documented technical properties

Full specifications, including appearance, content, viscosity and microbial limits, are provided in the product COA/TDS and can be requested from PuriPharm technical support. The spectra shown characterize the alginate backbone in a related material.

Published figure: FTIR fingerprint of the brown-algal sodium alginate backbone. Mar. Drugs 2026;24:41 (CC BY). DOI: 10.3390/md24010041.

Published figure: ¹H NMR anomeric-region spectrum used to resolve alginate M/G composition (same source). The presentation states that comparable COA-level characterization supports each AlgiSulf batch.

18 · FORMULATION

Formulation compatibility and processing

The following guidance is based on established polyelectrolyte chemistry of alginate-family polymers. Confirm specific parameters in pilot batches with PuriPharm technical support.

COMPATIBLE SYSTEMS

● Water-based and hydrogel systems: serums, concentrates, masks and scalp treatments.

● Nonionic and anionic ingredients: polyols, humectants and anionic surfactant bases.

● Oil-in-water emulsions: add to the aqueous phase for a light structural contribution.

● Cationic conditioners, when deliberately designed: controlled complexation for hair deposition.

● Near-neutral pH: a typical range for leave-on skin and scalp products.

HANDLE WITH CARE

● Strongly cationic ingredients: spontaneous polyelectrolyte complexation can be useful in hair care but should be avoided in clear gels.

● Low pH: uronic-acid protonation reduces charge and solubility; avoid strongly acidic systems.

● High electrolyte loading: charge screening can reduce viscosity and film quality.

● Multivalent cations, such as Ca²⁺: G-block “egg-box” gelation can be used deliberately as a texture tool.

PROCESSING

Add to the aqueous phase under moderate stirring and hydrate fully. A pre-dissolved solution may suit cold processing. Use levels depend on formulation goals; contact PuriPharm technical support.

19 · APPLICATIONS: SKINCARE

Skincare formulation opportunities

MOISTURIZING SERUMS / CONCENTRATES

A water-binding polyuronide film for a hydrated, plump feel with non-sticky slip.

SOOTHING GELS FOR SENSITIVE SKIN

Chemokine-affinity positioning for reactive, redness-prone or stressed skin in a lightweight hydrogel format.

BARRIER REPAIR CREAMS

Film-forming support inspired by dressings for compromised-barrier care and overnight repair masks.

ANTIOXIDANT DAY CARE

Sulfation-related radical scavenging as a concept for daily urban and photo-oxidative stress care.

FIRMING / ECM CARE CREAMS

GAG biomimetic positioning for matrix-care concepts in anti-aging and firming products.

SHEET MASKS AND ESSENCE SYSTEMS

A marine polysaccharide story with immediate surface smoothing and a soft after-feel.

CLAIM FRAMEWORK

Hydration · Barrier comfort · Soothing · Antioxidant defense · Matrix support. Each concept links to the mechanisms reviewed above.

20 · APPLICATIONS: SCALP AND HAIR

Hair and scalp formulation opportunities

SOOTHING SCALP SERUMS / TREATMENTS

Leave-on aqueous formats address tightness and itching through hydration and chemokine-affinity concepts.

FLAKING-CONTROL SCALP TREATMENTS

Patent precedent for sulfated polysaccharides supports a non-biocidal approach to flaking in daily scalp care.

SCALP HYDRATION MASKS

Pre-wash or overnight hydration for dry, tight scalps, with a light lotion texture and fresh feel.

CONDITIONERS / HAIR MASKS

Cationic complexation and deposition for cuticle smoothing, combability and sustained hair hydration.

AFTER-SUN SCALP SPRAYS

Antioxidant and soothing support for UV-exposed scalp partings, positioned as an emerging product opportunity.

GENTLE DAILY SHAMPOOS

Compatibility with anionic surfactants adds slip and post-wash comfort to mild, sulfate-free cleansing systems.

CLAIM FRAMEWORK

Scalp hydration and comfort · Flaking-control support · Oxidative stress defense · Hair conditioning.

Sources: EP2794012B1; Pavlichko et al. 1994; Trüeb 2009.

21 · EVIDENCE LANDSCAPE

Scientific evidence and application matrix

●●● Primary application area · ●● Strong supporting fit · ● Emerging rationale. These symbols reflect the depth of public evidence reviewed in the source presentation.

22 · VALUE PROPOSITION

What differentiates AlgiSulf

Beyond sodium alginate. Sulfation transforms a commodity texture polymer into a material with biological affinity, higher charge density, chemokine interactions and radical-scavenging properties, with a distinct INCI identity.

Characterized heparin-like chemistry. Two decades of peer-reviewed work on sulfated alginate, covering synthesis, sequence characterization, protein binding and cellular models, provide a substantial mechanistic literature for formulation concepts.

Continuity from skin to scalp. One ingredient carries a consistent marine polysaccharide story across facial, scalp and hair products, simplifying ingredient selection, claims development and supply chains.

Marine sourcing with contemporary relevance. Renewable brown-algal biomass, biodegradable polymer chemistry and a non-biocidal scalp-care concept align with responsible formulation goals.

PuriActives® AlgiSulf: marine sulfation science for formulation development.

23 · CONCLUSION AND REFERENCES

PuriActives® AlgiSulf: ready for your next formulation

A marine sulfated polysaccharide with a defined INCI identity, mechanistic literature and a combined skin–scalp application rationale. Technical support, samples and documentation are available from PuriPharm.

SELECTED REFERENCES

1. Arlov Ø, Skjåk-Bræk G. Sulfated alginates as heparin analogues: chemical and functional properties. Molecules 2017, 22(5), 778. DOI 10.3390/molecules22050778

2. Arlov Ø et al. Heparin-like properties of sulfated alginates with defined sequences and sulfation degrees. Biomacromolecules 2014, 15(7). DOI 10.1021/bm500602w

3. Kerschenmeyer A et al. Anti-oxidant and immune-modulatory properties of sulfated alginate derivatives on human chondrocytes and macrophages. Biomater. Sci. 2017, 5, 1756–1764. DOI 10.1039/C7BM00341B

4. Freeman I, Kedem A, Cohen S. Sulfation of alginate hydrogels: specific binding and controlled release of heparin-binding proteins. Biomaterials 2008, 29(22).

5. Huang C et al. Tunable sulfated alginate-based hydrogel platform for burn wound repair. J. Nanobiotechnology 2023, 21, 305. DOI 10.1186/s12951-023-02144-2

6. Balde A, Nazeer RA. In vitro anti-inflammatory effects of alginate sulfate; AlgS/PVA/CA microneedle system. Colloids Surf. B Biointerfaces 2025.

7. Karam M et al. Alginate and alginate sulfate/PCL nanoparticles for growth-factor delivery in wound healing. Biomed. Pharmacother. 2024.

8. Zhao X, Xue CH, Li BF. Antioxidant activities of sulfated polysaccharides from Laminaria japonica. J. Appl. Phycol. 2008. DOI 10.1007/s10811-007-9282-4

9. Mutch AL et al. Sulfated alginate for biomedical applications. Macromol. Biosci. 2024. DOI 10.1002/mabi.202400237

10. Kim JH et al. Beneficial effects of marine algae-derived carbohydrates for skin health. Mar. Drugs 2018, 16(11), 459. DOI 10.3390/md16110459

11. Ngo DH, Kim SK. Sulfated polysaccharides as bioactive agents from marine algae. Int. J. Biol. Macromol. 2013, 62.

12. Trüeb RM. Oxidative stress in ageing of hair. Int. J. Trichology 2009, 1(1), 6–14.

13. Pavlichko JP et al. Enhanced substantivity of hyaluronic acid on keratin substrates via polymer complexation. Int. J. Cosmet. Sci. 1994, 16(6). PMID 19250478

14. Use of sulphated polysaccharides as antidandruff agent. EP2794012B1 / WO2013093307A1 · Sodium alginate from E. amentacea: characterization & anti-inflammatory profile. Mar. Drugs 2026, 24(1), 41. DOI 10.3390/md24010041

PURIPHARM CO., LTD.

www.puriactives.com · service@puripharm.com · +86-572-2745768

Building 6, No. 1366 Hongfeng Road, Huzhou, Zhejiang, China

PuriActives® is a registered trademark of PuriPharm Co., Ltd.

NanoActive™ Harpa

NanoActive™ HarpaLiposomal Devil’s Claw Phytocomplex for Skin & Scalp Resilience

BRAND & PRODUCT

NanoActive™ Harpa · Liposomal Harpagoside Botanical Complex

Liposomal Devil’s Claw Phytocomplex for Skin & Scalp Resilience

Powered by PURISOME® FlexVes™ Liposome Technology

Soothe inflammatory signals, restore barrier resilience and revitalize the scalp

PuriPharm Co., Ltd.

PRODUCT OVERVIEW

African desert botanical resilience meets modern nano-delivery

TRADE NAME

NanoActive™ Harpa

PRODUCT POSITIONING

Liposomal harpagoside botanical complex

INCI NAME

HARPAGOPHYTUM PROCUMBENS ROOT EXTRACT

BOTANICAL SOURCE

Devil’s claw root

MARKER ACTIVES

Harpagoside and other iridoid glycosides

DELIVERY TECHNOLOGY

PURISOME® FlexVes™ flexible vesicle liposome technology

APPLICATIONS

Skincare · Scalp care · Hair care

KEY BENEFITS

▪ Soothing and redness care

▪ Barrier recovery

▪ Reduced water loss

▪ Inflamm-aging care

▪ Scalp comfort

▪ Root vitality

PRODUCT VALUE

Botanical actives

FlexVes™ flexible liposomes

Skin and scalp applications

NanoActive™ Harpa

MARKET INSIGHT

Skin and scalp face shared inflammatory stress

DAILY STRESSORS

▪ Air pollution

▪ UV exposure and heat

▪ Extreme temperature changes

▪ Frequent cleansing

▪ Surfactant irritation

▪ Cosmetic procedures

▪ Shaving

▪ Hair coloring, bleaching and perming

▪ Heat styling

▪ Sleep and lifestyle stress

BOTANICAL ORIGIN

Devil’s claw: resilience from the African desert

Harpagophytum procumbens grows mainly in arid southern Africa, including Namibia, Botswana, South Africa, Angola and parts of Zimbabwe.

“Harpago” derives from the Latin word for “hook.” The fruit’s sharp hooks give the plant its common name, devil’s claw.

Adapted to extreme dryness: defensive secondary metabolites accumulate under desert heat and water stress.

Secondary storage roots are the traditional plant material used and contain concentrated actives.

Burgundy flowers and hooked fruits create a distinctive visual identity for the African desert botanical story.

Traditional use and scientific interest connect southern African botanical practice with modern inflammation research.

Namib Desert landscape; devil’s claw flowers, hooked fruits, secondary roots and dried roots (reference images).

Source: Zuplex Botanicals. Rosacalm Product Brochure. 2019 [5].

PHYTOCHEMICAL PROFILE

Beyond harpagoside: a multi-active botanical matrix

IRIDOID GLYCOSIDES

  • Harpagoside (marker compound)
  • Harpagide
  • Procumbide

PHENOLIC GLYCOSIDES

  • Acteoside / Verbascoside
  • Isoacteoside

PHYTOSTEROLS

  • β-Sitosterol
  • TRITERPENES
  • Oleanolic acid
  • Ursolic acid

FLAVONOIDS

  • Luteolin
  • Kaempferol

AROMATIC ACIDS

  • Caffeic acid
  • Cinnamic acid
  • Chlorogenic acid

Harpagoside is the principal marker compound. The full devil’s claw root extract also contains multiple complementary actives.

Source: Zuplex Botanicals. Rosacalm Product Brochure. 2019 [5].

FORMULATION PHILOSOPHY

One marker compound, multiple complementary pathways

SINGLE MARKER COMPOUND: HARPAGOSIDE

▪ A defined active marker

▪ A focus of mechanistic research

▪ A clear anchor for scientific communication

FULL DEVIL’S CLAW ROOT PHYTOCOMPLEX

▪ Multiple iridoid glycosides

▪ Complementary polyphenols and flavonoids

▪ Additional triterpenes

▪ Botanical activity across multiple targets

▪ A broader rationale for soothing and repair

NanoActive™ Harpa delivers a botanical active network centered on harpagoside.

Source: Abdelouahab N, Heard C. J Nat Prod. 2008;71:746–749. DOI: 10.1021/np070204u [2].

THE DELIVERY CHALLENGE

Botanical actives need effective delivery

Actives vary in polarity, making a single solvent system difficult to optimize.

Uneven partitioning between aqueous and oil phases affects formulation uniformity.

Suboptimal dispersion can limit active availability.

Limited skin or scalp contact time reduces surface residence.

Some actives are sensitive to light, oxidation and other environmental factors.

Conventional extracts offer limited technological differentiation for premium positioning.

Scalp actives may run off with liquid, further reducing contact efficiency.

PURISOME® FlexVes™ upgrades conventional devil’s claw extract into a functional active with a modern delivery concept.

DELIVERY TECHNOLOGY

Flexible vesicles improve contact with target surfaces

TECHNOLOGICAL DIFFERENTIATION

From conventional botanical extract to NanoActive™ delivery

Dimension Conventional devil’s claw root extract NanoActive™ Harpa
Botanical source Devil’s claw root Active devil’s claw root phytocomplex
Marker constituent Harpagoside Multi-component phytocomplex centered on harpagoside
Dispersion Conventional solution or dispersion Phospholipid flexible vesicle delivery
Surface contact Passive contact Designed to enhance contact with skin and scalp surfaces
Technology story Traditional African botanical African botanical resilience + modern liposome technology
Applications Primarily skin soothing Skin, scalp and hair care platform
Market positioning Natural botanical extract Premium botanical active with nano-delivery

MECHANISM OVERVIEW

Soothing begins with upstream signaling

KEY MESSAGE

Modulation of upstream NF-κB-related signals provides a mechanistic rationale for soothing, redness care and barrier repair with devil’s claw root actives.

Source: Huang THW et al. J Ethnopharmacol. 2006;104:149–155. DOI: 10.1016/j.jep.2005.08.055 [1].

MECHANISM: NF-κB

NF-κB: a key regulator of inflammatory cascades

NF-κB links external stimuli with inflammatory mediator expression.

After stimulation, NF-κB can activate and enter the nucleus, promoting inflammatory mediators associated with redness, heat sensations and barrier discomfort.

Studies of harpagoside report effects on NF-κB activation and nuclear translocation, providing a molecular rationale for upstream inflammatory signal management.

The mechanistic evidence comes from published cellular and molecular studies and supports the product’s soothing rationale [1].

Source: Huang THW et al. J Ethnopharmacol. 2006;104:149–155 [1].

MECHANISM: INFLAMMATORY MEDIATORS

Inflammatory mediator regulation at multiple levels

iNOS

Inducible nitric oxide synthase

▪ Involved in NO production during inflammation

▪ Excess activity is associated with oxidative stress

▪ May increase cellular stress

COX-2

Inducible cyclooxygenase

▪ An important inducible enzyme in inflammation

▪ Participates in prostaglandin production

▪ Associated with redness, burning and discomfort

PGE2

Prostaglandin E2

▪ Involved in local vasodilation and inflammatory signaling

▪ May contribute to redness, swelling and barrier discomfort

NANOACTIVE™ HARPA: MECHANISTIC POSITIONING

NF-κB — iNOS — COX-2 — PGE2 inflammatory signaling axis

Harpagoside and the full phytocomplex provide a rationale for soothing at multiple levels of this axis.

Sources: Huang THW et al., 2006 [1]; Abdelouahab N, Heard C., 2008 [2].

SKIN INTERFACE RESEARCH

From cellular signaling to topical skin applications

▪ Devil’s claw root extract and its major glycosides have been studied in skin-related models [2].

▪ Research includes epidermal COX-2 responses relevant to redness and discomfort signals.

▪ Constituent ratios may influence overall effects; a single compound may not substitute for the full extract.

▪ Skin models indicate complementary value from multiple constituents.

▪ Transcutaneous and topical studies provide a mechanistic basis for cosmetic soothing applications [3].

Skin model research connects molecular mechanisms with topical use, supporting the rationale for soothing and barrier repair.

Sources: Abdelouahab N, Heard C. J Nat Prod. 2008 [2]; Int J Pharm. 2009 (ex vivo skin model study) [3].

INFLAMM-AGING

Managing low-grade inflammatory stress for skin resilience

Persistent low-grade inflammatory stress may affect skin cells, barrier function and the extracellular matrix. Inflamm-aging is therefore a concept used in premium anti-aging product development.

APPLICATION TERRITORIES

▪ Anti-aging for sensitive skin

▪ Repair-focused anti-aging

▪ Urban environmental care

▪ Barrier-focused anti-aging

▪ Soothing support alongside potent actives

▪ Skin longevity and resilience concepts

Upstream signal management provides a scientific rationale for combining soothing with anti-aging product concepts.

Mechanistic sources: Huang THW et al., 2006 [1]; Abdelouahab N, Heard C., 2008 [2].

EFFICACY BENCHMARK: THIRD-PARTY DEVIL’S CLAW ROOT EXTRACT DATA

Redness and water loss improvements over 24–48 hours

TEST DESIGN

TEST LABORATORY:Dermaconsult GmbH

PARTICIPANTS:20 participants, plus 1 reserve participant

SEX AND AGE:14 women and 6 men; 23–61 years

TEST AREA:Inner forearm

ACTIVE CONCENTRATION:5%

ASSESSMENTS:Skin redness · Transepidermal water loss · Skin irritation patch test

INSTRUMENTS:CR-400 chroma meter · Tewameter Triple TM 330 T

INSTRUMENTAL RESULTS

Endpoint 24 hours 48 hours
Reduction in skin redness 9.1% 14.7%
Reduction in TEWL 16.7% 22.95%

▪ Redness improvement observed at 24 hours

▪ Greater improvement at 48 hours

▪ Continued reduction in transepidermal water loss

▪ Supports positioning for rapid soothing and barrier recovery

▪ Relevant to products for sensitive, irritated or environmentally stressed skin

Note: These data come from a third-party human efficacy test of 5% conventional devil’s claw root extract. They serve as botanical benchmarks for NanoActive™ Harpa product development and efficacy positioning.

Sources: Zuplex Botanicals. Rosacalm Product Brochure. 2019 [5]; Dermaconsult GmbH Test Summary [6].

SKINCARE PLATFORM

From rapid soothing to lasting barrier resilience

CALM

▪ Help reduce visible redness

▪ Soothe tightness and discomfort

▪ Help restore skin comfort

RESTORE

▪ Support barrier recovery

▪ Help reduce transepidermal water loss

▪ Improve dryness, roughness and fragility

DEFEND

▪ Help manage inflammatory signals associated with external stressors

▪ Support care under pollution and climate stress

▪ Provide soothing support in formulations with potent actives

REVITALIZE

▪ Help restore a healthy, balanced appearance

▪ Improve softness and moisturized feel

▪ Support repair-focused anti-aging and skin resilience concepts

Rapid botanical soothing supports skin recovery and resilience.

SKINCARE APPLICATIONS

For repair-focused and sensitive-skin products

01 Redness rescue serum

Rapid soothing care for environmental irritation, temperature changes, sleep loss and fragile skin.

02 Urban repair cream

For skin stressed by pollution, dryness and demanding lifestyles.

03 Soothing serum to complement potent actives

For concepts featuring retinol, retinal, acids or high-concentration niacinamide.

04 After-sun soothing lotion

Comfort care following UV and heat exposure.

05 Eye-area soothing serum

For the appearance of fatigue, dryness and puffiness.

06 Post-shave barrier repair lotion

For redness, tightness and discomfort after shaving.

OTHER APPLICATIONS

Soothing masks · Body repair lotions · Hand and foot care · Cosmetic aftercare for tattoos · Local repair gels

COMPLEMENTARY INGREDIENT CONCEPTS

Panthenol · Ectoin · β-Glucan · Niacinamide · Ceramides · Bisabolol · Allantoin · Hyaluronic acid

SCALP SCIENCE

Scalpification brings barrier and soothing science to the scalp

SCALP STRESSORS

▪ Frequent shampooing

▪ Surfactants

▪ Sebum oxidation

▪ Pollutant accumulation

▪ UV and heat

▪ Hair coloring, bleaching and perming

▪ Blow-drying and heat styling

▪ Scratching and mechanical friction

POTENTIAL IMPACT

▪ Tightness and discomfort

▪ Visible redness

▪ Barrier imbalance

▪ Dryness or sebum imbalance

▪ Affected root environment

▪ Reduced hair strength and healthy appearance

Close-up scalp and hair-root images (reference images).

NanoActive™ Harpa extends sensitive-skin soothing science to scalp microenvironment care.

HAIR CARE DIRECTION: PATENT-SUPPORTED APPLICATION CONCEPTS

From botanical soothing to root vitality

HENKEL AG & CO. KGAA

Patent WO2008031685A1

Root Extract of Harpagophytum for Stimulating Hair Growth

Published patent concerning devil’s claw root extract for hair applications [4].

▪ Devil’s claw actives appear in hair strengthening and thickening concepts.

▪ The patent addresses root vitality and hair-condition improvement.

▪ Applications include shampoos, conditioners, scalp serums, sprays, lotions and scalp tonics.

▪ Patent examples include formulations with devil’s claw extract.

▪ Studies involve dermal papilla cells and keratinocytes.

▪ The patent discusses advantages of liposomal encapsulation in scalp and hair care products.

These patent-supported development directions provide technical and conceptual references for NanoActive™ Harpa scalp and hair care applications.

Source: Henkel AG & Co. KGaA. Patent WO2008031685A1 [4].

SCALP DELIVERY

Improving botanical contact with scalp and root surfaces

CONVENTIONAL WATER-SOLUBLE BOTANICAL EXTRACT

▪ Can run off with liquid

▪ Limited surface residence

▪ Potentially uneven distribution

▪ Shorter scalp contact time

NanoActive™ Harpa

FLEXVES™ LIPOSOMAL DELIVERY

▪ Delivery associated with phospholipid vesicles

▪ Improved scalp surface distribution

▪ Enhanced contact with follicular openings

▪ Suitable for leave-on scalp serums and tonics

▪ A modern technology concept for root care

▪ Integration of soothing and root vitality concepts

Liposomal delivery is designed to support retention, uniform distribution and longer contact on the scalp.

SCALP & HAIR PLATFORM

Scalp comfort, root strength and revitalized hair

SCALP COMFORT

▪ Help soothe tightness and discomfort

▪ Improve comfort in irritated scalps

▪ Support scalp barrier balance

ROOT VITALITY

▪ Support a healthy root microenvironment

▪ Suitable for volumizing, strengthening and anti-hair-loss product concepts

▪ Help improve the appearance of thinning and fragile hair

HAIR STRENGTH

▪ Support damaged and fragile hair care

▪ Help improve perceived strength and healthy shine

▪ Suitable for care after coloring and perming

MARKET DIFFERENTIATION

African devil’s claw botanical story · Harpagoside mechanisms · Skin and scalp applications · Nano-liposome technology · Soothing combined with root vitality

Scalp soothing is the starting point for a stronger, fuller-looking hair concept.

SCALP & HAIR PRODUCT CONCEPTS

From daily scalp balance to intensive root care

01 Scalp soothing serum

For tightness, dryness and scalp discomfort.

02 Root vitality serum

For volume, strength and healthy-root concepts.

03 Sensitive-scalp shampoo

Combines gentle cleansing with scalp soothing.

04 Root strengthening conditioner

Supports smoothness and a stronger hair appearance.

05 Scalp repair serum after chemical treatments

Comfort care after coloring, bleaching or perming.

06 Volumizing leave-on spray

Lightweight, non-sticky daily root care.

COMPLEMENTARY INGREDIENT CONCEPTS

Caffeine · Niacinamide · Panthenol · Zinc PCA · Amino acids · Peptides · Ceramides · Botanical antioxidants

NANOACTIVE™ HARPA

African desert resilience translated into beauty care

SOOTHE INFLAMMATORY SIGNALS

A multi-component botanical system centered on harpagoside supports modern skin and scalp soothing concepts.

RESTORE BARRIER RESILIENCE

Third-party instrumental testing of the conventional extract supports positioning for redness care, reduced water loss and barrier recovery.

REVITALIZE THE SCALP

Patent-supported root-care directions and PURISOME® flexible vesicle delivery expand the possibilities for premium scalp and hair products.

NanoActive™ Harpa combines devil’s claw botanical resilience with modern nano-liposome technology in an integrated concept for skin soothing, barrier recovery, scalp balance and root vitality.

NanoActive™ Harpa · Powered by PURISOME® FlexVes™ Liposome Technology

PURIPHARM CO., LTD.

REFERENCES

References and source materials

[1] Huang THW, Tran VH, Duke RK, et al. Harpagoside suppresses lipopolysaccharide-induced iNOS and COX-2 expression through inhibition of NF-kappa B activation. Journal of Ethnopharmacology. 2006;104(1–2):149–155. DOI: 10.1016/j.jep.2005.08.055

[2] Abdelouahab N, Heard C. Effect of the major glycosides of Harpagophytum procumbens on epidermal COX-2 in vitro. Journal of Natural Products. 2008;71(5):746–749. DOI: 10.1021/np070204u

[3] A Novel Ex Vivo Skin Model for the Assessment of the Potential Transcutaneous Anti-inflammatory Effect of Topically Applied Harpagophytum procumbens Extract. International Journal of Pharmaceutics. 2009.

[4] Henkel AG & Co. KGaA. Root Extract of Harpagophytum for Stimulating Hair Growth. Patent WO2008031685A1.

[5] Zuplex Botanicals. Rosacalm Product Brochure. 2019.

[6] Dermaconsult GmbH. Third-party instrumental evaluation of skin redness, transepidermal water loss and skin irritation, as summarized in the Rosacalm technical presentation.

[7] European Commission CosIng Database. HARPAGOPHYTUM PROCUMBENS ROOT EXTRACT.

NanoActive™ Oryzanol

01 · NanoActive™ Oryzanol: Oryzanol Nanoliposomes

Cosmetic active ingredient product introduction. INCI: ORYZANOL. Rice-derived antioxidant defense, reinvented by liposomal delivery.

Powered by PURISOME® FlexVes™ Liposome Technology. PuriPharm Co. Ltd.

02 · From Rice-Bran Active to Nano-Delivered Antioxidant

γ-Oryzanol is a group of phytosterol/triterpene alcohol ferulate esters naturally found in rice bran oil. Sterol lipids provide lipid affinity, while ferulate groups provide radical-defense potential.

Antioxidant: radicals/lipid peroxidation. Photoaging care: light-induced oxidative stress. Aging care: collagen/elastic-network concepts. Skin + Hair: skin, scalp, and hair.

NanoActive™ uses lipid vesicles to improve practical cosmetic formulation design.

03 · γ-Oryzanol Ingredient Science

A mixture of ferulate esters in the unsaponifiable fraction of rice bran oil. Representative components: Cycloartenyl Ferulate, 24-Methylene Cycloartanyl Ferulate, Campesteryl Ferulate, and Sitosteryl Ferulate.

An ester bond links the phenolic antioxidant ferulic-acid moiety with a lipid-affine phytosterol/triterpene-alcohol moiety.

Sources: Lerma-García et al. Food Chem. 2009;115:389–404; Ramazani et al. Curr Pharm Des. 2021;27(19):2299–2316. DOI: 10.2174/1381612826666201102101428.

Source link: https://doi.org/10.2174/1381612826666201102101428

References: Lerma-García JM, et al. Food Chemistry. 2009;115:389–404. | Ramazani E, et al. Curr Pharm Des. 2021;27(19):2299–2316. DOI: 10.2174/1381612826666201102101428

04 · Plant Antioxidant and Skin Lipid Science

Image: rice bran, the natural source.

01 Radical defense and oxidative-chain inhibition. 02 Lipid antioxidant activity in lipid-rich environments. 03 Ferulate UV-absorption/antioxidant properties as a basis for photostress care. 04 Research on collagenase, elastase, hyaluronidase, and tyrosinase.

05 · Multiple Antioxidant and Aging-Care Pathways

The mechanism map includes lower ROS, lipid peroxidation, oxidative damage, collagenase, elastase, hyaluronidase, and tyrosinase.

Concepts: antioxidant/photoaging care, elasticity, hydration-related structures, even tone, soothing defense, and scalp/hair antioxidants. These summarize in vitro/model literature and do not establish finished-product clinical efficacy.

06 · Radical-Chain Management and Lipid Protection

Ferulate esters participate in radical scavenging and reduced radical-induced lipid peroxidation. Relevant lipid environments include stratum-corneum lipids, sebum, cellular membranes, hair surface lipids, and oxidizable formulation oils.

Pathway: radical scavenging, lipid protection, and biological-structure protection.

Juliano C, Cossu M, Alamanni MC, Piu L. Int J Pharm. 2005;299:146–154. DOI: 10.1016/j.ijpharm.2005.05.018.

Source link: https://doi.org/10.1016/j.ijpharm.2005.05.018

Juliano C, Cossu M, Alamanni MC, Piu L. Antioxidant activity of gamma-oryzanol: mechanism of action and its effect on oxidative stability of pharmaceutical oils. Int J Pharm. 2005;299:146–154. DOI: 10.1016/j.ijpharm.2005.05.018

07 · Oxidative Stress Connects Exposure and Skin Aging

UV/pollution/ROS, oxidative stress, cellular damage, ECM degradation, and loss of elasticity/roughness/uneven tone form the schematic pathway.

NanoActive™ Oryzanol uses antioxidant design for daily aging-care concepts. This does not replace sunscreen and provides no SPF/PA claims.

08 · 2026 Nanoencapsulated γ-Oryzanol Research

Literature nanoemulsion, H₂O₂-induced NIH/3T3 mouse fibroblast aging model: reduced intracellular ROS, supported survival/migration, and inhibition of collagenase, elastase, hyaluronidase, and tyrosinase.

Reported parameters: approximately 162 nm particle size, PDI 0.2, and zeta potential −51 mV. These are Yadav’s independent nanoemulsion values, not NanoActive™ product parameters.

Yadav P, Sankar J, Mora C, et al. Nanoencapsulated gamma-oryzanol enhances fibroblast proliferation, migration, and reduces oxidative stress in H₂O₂-induced cellular aging model. J Funct Foods. 2026;136:107130. DOI: 10.1016/j.jff.2025.107130.

Source link: https://doi.org/10.1016/j.jff.2025.107130

Yadav P, Sankar J, Mora C, et al. Nanoencapsulated gamma-oryzanol enhances fibroblast proliferation, migration, and reduces oxidative stress in H₂O₂-induced cellular aging model. J Funct Foods. 2026;136:107130. DOI: 10.1016/j.jff.2025.107130

09 · Protecting Collagen, Elastin, and Hyaluronic-Acid Networks

The dermal ECM schematic shows collagen, elastin, and hyaluronic acid. Oxidative stress and collagenase/elastase/hyaluronidase activity can contribute to network breakdown.

Multi-enzyme defense extends the literature concept from ROS management to structural-network preservation.

10 · Fibroblast Vitality

Dermal fibroblasts maintain collagen, elastin, and ECM. Oxidative pressure can reduce vitality/migration and accelerate structural decline.

Yadav’s 2026 nanoemulsion study reported ROS reduction, viability support, and migration in an oxidative model, informing cellular vitality, matrix defense, and resilience concepts.

J Funct Foods. 2026;136:107130. DOI: 10.1016/j.jff.2025.107130. Independent formulation evidence.

Source link: https://doi.org/10.1016/j.jff.2025.107130

Source: Yadav P, et al. J Funct Foods. 2026;136:107130 (literature nanoemulsion, not this product)。DOI: 10.1016/j.jff.2025.107130

11 · Tone and Brightening Research

2025 in vitro B16F10 mouse melanoma research: DPPH/FRAP antioxidant activity, lower cellular ROS, mushroom tyrosinase inhibition, reduced cellular melanin, and melanogenesis-related inhibition.

Concepts: antioxidant brightening, tyrosinase modulation, and even tone. In vitro potential does not establish clinical brightening or product efficacy.

Emami SA, Hadipour E, Boozari M, et al. Comparison of Antioxidant and Anti-Melanogenic Activity of γ-Oryzanol and Gallic Acid by Inhibiting Tyrosinase Activity in B16F10 Mouse Melanoma Cells. Food Sci Nutr. 2025;13:e70946. DOI: 10.1002/fsn3.70946.

Source link: https://doi.org/10.1002/fsn3.70946

Emami SA, Hadipour E, Boozari M, et al. Comparison of Antioxidant and Anti-Melanogenic Activity of γ-Oryzanol and Gallic Acid by Inhibiting Tyrosinase Activity in B16F10 Mouse Melanoma Cells. Food Sci Nutr. 2025;13:e70946. DOI: 10.1002/fsn3.70946

12 · UV-Associated Antioxidant Defense

Schematic: UV exposure, ROS generation, lipid peroxidation, inflammatory stress, and ECM damage.

Cosmetic language: helps defend against UV-induced oxidative stress; supports daily photostress protection; helps protect skin lipids from oxidative challenge.

No SPF/PA values, sunscreen replacement, or core regulatory claim of a natural sunscreen.

13 · Nanoethosome Delivery Evidence

2021 γ-oryzanol nanoethosomes improved delivery/cellular uptake, offered long-term storage protection, and showed protection in UVB-related models.

The original mouse work involved UV-induced skin cancer; this article retains it as delivery/photostress research, without disease-prevention/treatment claims.

Zeinali M, et al. Prevention of UV-induced skin cancer in mice by gamma oryzanol-loaded nanoethosomes. Life Sci. 2021;283:119759. DOI: 10.1016/j.lfs.2021.119759.

Source link: https://doi.org/10.1016/j.lfs.2021.119759

Zeinali M, et al. Prevention of UV-induced skin cancer in mice by gamma oryzanol-loaded nanoethosomes. Life Sciences. 2021;283:119759. DOI: 10.1016/j.lfs.2021.119759

14 · Formulation Challenges

Low water dispersibility; crystallization/precipitation with system or temperature changes; reliance on oils, emulsions, or solubilizers; limited effective delivery of free active; and prolonged environmental exposure.

Published approaches include solubilization, dispersion, emulsification, phospholipid complexes, and nanodelivery.

Patent examples: JP6803732B2, Cosmetics containing γ-oryzanol; WO2012110303A2, Aqueous cosmetic composition containing composite material particles and gamma-oryzanol; EP1957041B1, Oil-in-water emulsion and its use for delivery of functionality.

Patent examples (publication number and title): JP6803732B2 · Cosmetics containing γ-oryzanol;WO2012110303A2 · Aqueous cosmetic composition containing composite material particles and gamma-oryzanol;EP1957041B1 · Oil-in-water emulsion and its use for delivery of functionality。

15 · From Lipophilic Active to Formulation-Ready Nano Active

Oryzanol, PURISOME® FlexVes™, and NanoActive™ Oryzanol form the design pathway.

Protection: a phospholipid microenvironment. Dispersion: an adapted form for cosmetics. Delivery: effective skin-surface contact potential. Flexibility: serums, lotions, creams, scalp, and hair products.

The design changes incorporation and contact rather than merely adding free Oryzanol.

16 · Biomimetic Lipid Vesicle Architecture

The scientific schematic labels a hydrophilic aqueous core, phospholipid hydrophilic heads, and a hydrophobic bilayer domain. Highly lipophilic γ-Oryzanol is proposed to associate preferentially with the bilayer rather than the inner aqueous core.

Oryzanol, lipid-bilayer association, vesicular dispersion, and cosmetic delivery. The localization drawing is proposed architecture rather than a direct measurement.

17 · More Than 15 Years of Liposome Research

2009 topical γ-oryzanol liposomes: phosphatidylcholine, cholesterol, CHAPS, and sodium taurocholate. Initial loading levels 3%, 5%, and 10%.

Endpoints: size, zeta potential, entrapment, release, antioxidant activity, and cellular compatibility. Antioxidant activity remained after loading; some systems showed enhanced cellular antioxidant activity.

Viriyaroj A, Ngawhirunpat T, Sukma M, et al. Physicochemical properties and antioxidant activity of gamma-oryzanol-loaded liposome formulations for topical use. Pharm Dev Technol. 2009;14(6):665–671. DOI: 10.3109/10837450902911937. Literature formulation, not product data.

Source link: https://doi.org/10.3109/10837450902911937

Viriyaroj A, Ngawhirunpat T, Sukma M, et al. Physicochemical properties and antioxidant activity of gamma-oryzanol-loaded liposome formulations for topical use. Pharm Dev Technol. 2009;14(6):665–671. DOI: 10.3109/10837450902911937 —literature formulation supporting NanoActive™ design, not product data.

18 · Research from Liposomes to Lipid Nanocarriers

2009 topical liposomes; 2009 solid lipid nanoparticles/nanoemulsions (SLN/NE); 2021 nanoethosomes; 2024 liposomal nanocarriers; 2026 cellular-aging nanoencapsulation.

Independent teams use these strategies for stability, dispersion, and delivery, providing continuity for NanoActive™ design.

Ruktanonchai U, et al. J Microencapsul. 2009;26(7):614–626. DOI: 10.3109/02652040802586571; Jasim AJ, et al. ACS Omega. 2024;9:3554–3564. DOI: 10.1021/acsomega.3c07339. Other sources appear in their sections.

Source link: https://doi.org/10.3109/02652040802586571

Source link: https://doi.org/10.1021/acsomega.3c07339

Ruktanonchai U, et al. J Microencapsul. 2009;26(7):614–626. DOI: 10.3109/02652040802586571 | Jasim AJ, et al. ACS Omega. 2024;9:3554–3564. DOI: 10.1021/acsomega.3c07339 (see other research sections)

19 · Human Evidence from Composite Rice-Bran Vesicles

Composite system: Ferulic Acid + γ-Oryzanol + Phytic Acid + Niosomes. 30 volunteers, 28 days.

Endpoints: hydration, elasticity, thickness, roughness, and pigmentation. Gels/creams containing the composite vesicles improved multiple aging-related indicators.

All human effects cannot be attributed to γ-oryzanol alone. The study supports composite rice-bran actives and vesicular delivery, not direct NanoActive™ efficacy.

Manosroi A, Chutoprapat R, Abe M, Manosroi W, Manosroi J. Pharm Biol. 2012;50(2):208–224. DOI: 10.3109/13880209.2011.596206.

Source link: https://doi.org/10.3109/13880209.2011.596206

Manosroi A, Chutoprapat R, Abe M, Manosroi W, Manosroi J. Anti-aging efficacy of topical formulations containing niosomes entrapped with rice bran bioactive compounds. Pharm Biol. 2012;50(2):208–224. DOI: 10.3109/13880209.2011.596206

20 · Antioxidant Defense and Inflammatory Stress

Non-skin models suggest effects on NF-κB-associated inflammatory signaling. These provide research clues for oxidative/inflammatory-stress care.

Cosmetic concepts: comfort support, environmental defense, and reduced oxidative burden in sensitive/tired/stressed skin. No medicinal anti-inflammatory or disease-treatment claims.

Ramazani E, Akaberi M, Emami SA, Tayarani-Najaran Z. Curr Pharm Des. 2021;27(19):2299–2316. DOI: 10.2174/1381612826666201102101428.

Source link: https://doi.org/10.2174/1381612826666201102101428

Ramazani E, Akaberi M, Emami SA, Tayarani-Najaran Z. Biological and Pharmacological Effects of Gamma-oryzanol: An Updated Review of the Molecular Mechanisms. Curr Pharm Des. 2021;27(19):2299–2316. DOI: 10.2174/1381612826666201102101428

21 · From Skin Lipids to Hair Lipids

Hair surface lipids face oxidative/environmental stress. Concepts: scalp antioxidant defense; hair lipid protection; sun/pollution/heat-styling care; and phospholipid conditioning support.

Patents: EP0945122A1, Haircare composition containing gamma-oryzanol and calcium salts; WO2012110303A2, skin/hair photoprotection context.

Claims stay within antioxidants, lipid care, and smoothness, excluding hair growth or hair-loss prevention.

EP0945122A1 — Haircare composition containing gamma-oryzanol and calcium salts WO2012110303A2 — relates to skin and/or hair photoprotection against ultraviolet radiation

22 · One Platform, Skin and Hair

Skin: antioxidants, photoaging-related stress, collagen/elastic matrix, hyaluronic-acid-related structures, tone, and environmental comfort.

Scalp/hair: antioxidants, fiber oxidation protection, photostress, lipids, and conditioning. Hair-growth/hair-loss claims are excluded.

23 · Modern Formulation Applications

Skin: antioxidant/aging/day-defense serums, photoaging-care lotion, recovery cream, brightening serum, urban protection, after-sun care, eye-aging care, and premium rice-bran concepts.

Scalp: antioxidant serum, comfort care, post-sun care, and urban-pollution care. Hair: conditioner, mask, leave-on serum, oil/emulsion, sun-exposure care, post-color/perming care, and heat-styling care.

The source cites commercial approximately 5% γ-oryzanol emulsion ingredients for soap/facial wash, lotion, shampoo, and conditioner as market context, not this product’s active content or recommended use level.

24 · A Formulation-Friendly Oryzanol Design

Free active challenges: hydrophobicity, poor aqueous dispersion, crystallization, oil/solubilizer dependence, complex processing, restricted formats, and delivery limitations.

NanoActive™ design: lipid-vesicle organization, aqueous dispersion, handling convenience, a lipid-compatible microenvironment, serum/emulsion use, and skin/hair applications.

This is qualitative dosage-form/process comparison, without unverified fold-improvement claims. Actual performance requires formulation validation.

25 · Rice Antioxidant, Reinvented

Rice-derived science; radical/lipid-peroxidation defense; ECM protection concepts; antioxidant tone support; skin/scalp/hair use; and PURISOME® FlexVes™ liposomal delivery.

NanoActive™ Oryzanol brings a classic rice-bran antioxidant into precision lipid-delivery design.

PuriActives® SLL

01 · PuriActives® SLL: Sodium Lauroyl Lactylate

Technical product presentation. INCI: SODIUM LAUROYL LACTYLATE. Formula C18H31NaO6, MW approximately 366.4 g/mol.

Multifunctional lactylate interface technology for skin and hair care. More Than an Emulsifier. PuriPharm Co., Ltd.

02 · More Than an Emulsifier

Positioning: a multifunctional interface ingredient.

01 Emulsification: uniform oil/water dispersion and O/W interface stability. 02 Mild cleansing: an anionic structure supporting mild-system design. 03 Lipid compatibility: a C12 chain and lactylated headgroup for complex lipid formulations. 04 Skin/hair sensory properties: softer, refined cleansing and care experiences.

Its amphiphilic structure participates in oil/water interfaces, surfactant assemblies, and lipid formulations across skin and hair applications.

03 · From Strong Cleansing to Cleansing Quality

Traditional focus: strong cleansing, high foam, and simple emulsions. Modern needs: mild cleansing, barrier-conscious design, lipid compatibility, refined sensory properties, multifunctionality, and skin/scalp-friendly concepts.

SLL offers an interface-chemistry approach to these formulation needs.

04 · Product Identity

The product information table and molecular structure are retained below.

Class: acyl lactylate, anionic surfactant. CosIng function: Surfactant–Emulsifying.

Sources in the presentation: PubChem—Sodium Lauroyl Lactylate; EU CosIng; Johnson et al. Int J Toxicol. 2024.

Source link: https://pubchem.ncbi.nlm.nih.gov/compound/Sodium-lauroyl-lactylate

Source link: https://ec.europa.eu/growth/tools-databases/cosing/

Item Information
Product PuriActives® SLL
INCI SODIUM LAUROYL LACTYLATE
Chinese INCI 月桂酰乳酰乳酸钠 (Sodium Lauroyl Lactylate)
CAS No. 13557-75-0
EC No. 236-942-6
Molecular Formula C18H31NaO6
Molecular Weight Approximately 366.4 g/mol
Ingredient Class Acyl Lactylate · Anionic Surfactant
CosIng Function Surfactant – Emulsifying

05 · Fatty Acid × Lactic Acid Chemistry

Lauric acid, a C12 fatty acid, combines with lactic-acid/lactylate chemistry. The schematic shows esterification followed by neutralization to the sodium salt.

Fatty-acid-derived lipophilicity and lactylate-derived hydrophilicity produce a balanced amphiphilic architecture: a molecular bridge between water and lipids.

06 · How SLL Works at the Interface

The hydrophilic lactylated head faces water; the hydrophobic C12 lauroyl chain enters the oil/lipid phase.

01 Adsorption: molecules migrate to the oil/water interface. 02 Organization: the chain anchors in oil and the head faces water. 03 Dispersion support: interface organization provides a structural basis for stability.

This amphiphilic architecture supports emulsions, cleansing systems, and lipid formulations.

07 · Emulsification and Interface Management

The schematic shows an oil droplet in a continuous water phase, surrounded by SLL with heads toward water and chains into oil.

Supports uniform dispersion, O/W emulsions, homogeneity/stability, combined emulsifier systems, and a refined feel in creams, lotions, and serum emulsions.

The presentation cites EU CosIng: SURFACTANT–EMULSIFYING.

Source link: https://ec.europa.eu/growth/tools-databases/cosing/

08 · Interface Engineering Across Formulation Structures

Oil/water interfaces: stabilization of emulsions and dispersions. Surfactant assemblies: complex cleansing structures, foam, and after-feel. Lipid-rich systems: dispersion and organization of ceramides, cholesterol, and other lipids.

SLL participates at multiple structural levels from adsorption to system organization.

09 · Mild Cleansing System Design

SLL’s anionic surfactant structure supports soil/sebum removal in combined systems, balancing cleansing with after-feel.

Formats: facial cleansers, body/hand washes, bathing products, and mild-cleansing concepts.

Patent context: cleansing, moisturization, lather, and skin feel. WO1998027193A1, Personal cleansing bar composition containing sodium lauroyl lactylate (1998); WO2007100784A2, Acyl lactylate compositions for rinse-out and leave-on applications for skin and hair (2007).

10 · From Clean to Comfortable Clean

The source compares conventional clean/tight/dry after-feel with an SLL formulation concept of clean/soft/comfortable/refined after-feel.

Published formulation goals: skin softness, moisturization, creamy lather, and improved after-feel. These reflect combined formulations, not effects attributable entirely to one ingredient.

Patent sources: WO1998027193A1; WO2007100784A2.

11 · An Interface Partner for Barrier Lipid Formulations

Ceramides + Cholesterol + Fatty Acids + SLL interface support.

Roles: dispersion, interface activity, co-emulsification, and lipid-delivery design. The lipid matrix is schematic.

US20240000681A1 (2024) includes SLL in designs containing Ceramide NP/AP/EOP, cholesterol, and free fatty acids/precursors. This is a patent disclosure, not PuriActives® SLL clinical data.

Patent title: Chemical compositions providing long-lasting skin pH control for improving skin-barrier function and treatment of skin-barrier disorders.

12 · Barrier-Friendly Formulation Architecture

SLL supports the architecture of lipid-based barrier-care products.

Combination logic: SLL interface support + Ceramides + Cholesterol + Phytosphingosine + Fatty Acids + Humectants.

Formats: barrier cream, ceramide lotion, sensitive/dry skin care, post-cleansing care, and lipid-rich serum. This formulation rationale does not by itself demonstrate clinical barrier repair.

13 · Moisturization Starts at the Interface

Hydration involves humectancy, occlusion, lipid organization, cleansing mildness, and emulsion quality.

SLL primarily supports interface, lipid, and cleansing dimensions of comfortable moisturization systems.

Patent context: skin softness, moisturization, cleansing, and foaming. WO2007100784A2 (2007); WO1998027193A1 (1998).

14 · From Skin to Hair

One molecule supports skin/hair formulation contexts. Published directions include shampoo, mild shampoo, scalp cleansing, rinse-off care, leave-on hair/scalp concepts, and hair grooming products.

15 · From Foam Quantity to Foam Quality

EP0562720A1, Hair shampoo (1993), examines acyl lactylates with alkyl polyglucosides (APG), including Sodium Lauroyl Lactylate-related systems, to address coarse APG foam.

Patent example range: acyl lactylates 3–15%, preferred 4–8%. These are patent-system ranges, not PuriActives® SLL recommendations.

Fine-Tune the Foam. Elevate the Cleansing Experience.

16 · Published Shampoo Formulation Examples

WO2007100784A2 (2007): approximately 3.0% SLL in a clear mild shampoo example concerned with cleansing, foam, viscosity, and pH stability; approximately 2.0% in another shampoo example for mild cleansing/sensory performance.

These are published examples, not recommended use levels. SLL has a documented hair-cleansing formulation history. Relevant attributes: cleansing, foaming, viscosity, pH stability, and sensory properties.

17 · Hair Fiber and Scalp Interface

Scalp: cleansing-system design, sebum/soil removal, freshness, mild formulations, and lipid-compatible care.

Hair: cleansing sensory properties, softer after-feel concepts, creamy foam, lipid-containing formulations, and conditioner/mask support.

Cosmetic scope excludes hair growth, anti-hair-loss, follicle repair, and hair-thickening claims.

18 · SLL and Modern Hair-Care Concepts

Reduced-sulfate cleansing, APG shampoos, scalp barrier care, ceramide hair care, lipid-replenishing shampoos, sensitive-scalp cleansing, premium cream shampoos, and scalp/hair serum emulsions.

An interface ingredient bridging cleansing technology and lipid care.

19 · SLL Interactions with Model Lipid Membranes

Gooran N, Tan SW, Yoon BK, Jackman JA. Int J Mol Sci. 2023;24(11):9283. DOI: 10.3390/ijms24119283.

Methods: QCM-D, quartz crystal microbalance with dissipation monitoring; EIS, electrochemical impedance spectroscopy; SLB, supported lipid bilayer; tBLM, tethered bilayer lipid membrane.

The study tracked SLL insertion, reorganization, and disruption of model membranes. The schematic shows aqueous phase, SLL, membrane perturbation, and solid support. Model lipid membranes are not equivalent to the human stratum corneum.

Source link: https://doi.org/10.3390/ijms24119283

20 · Research Possibilities Beyond Emulsification

Lactylate membrane-interactive behavior offers research perspectives for cleansing and lipid-care design.

Directions: advanced cleansing, scalp hygiene, personal cleansing, microbial membrane research, and functional surfactant systems. These are research concepts without therapeutic claims.

Source: Gooran et al. 2023.

21 · Application Matrix

Skin: facial cleanser, cream cleanser, body wash, hand wash, moisturizing lotion, barrier cream, ceramide cream, facial emulsion, sensitive-skin care, lipid-rich serum, body lotion, and post-cleansing care.

Hair: shampoo, mild/cream shampoo, scalp cleanser/care, conditioner, mask, hair milk, leave-on emulsion, ceramide hair care, and lipid-replenishing care.

22 · Combination Design

Surfactants: APG, amphoteric, anionic, and nonionic systems. Lipids: ceramides, cholesterol, fatty acids, vegetable oils, and esters. Conditioning: glycerin, panthenol, hyaluronic acid, phytosphingosine, niacinamide, proteins, and amino acids.

Formulation versatility requires experimental compatibility testing; not every combination is presumed compatible.

23 · pH and Formulation Window

Published patent window: pH 4.0–8.5; preferred pH 5.0–7.0. The scale shown spans 3–9.

These are WO2007100784A2 acyl-lactylate skin/hair formulation windows, not product specifications.

pH 5–7 informs mildly acidic skin-care, gentle scalp-care, and hair-cleansing concepts.

24 · Reported Cosmetic Use

2024 CIR safety-assessment reported maximum use concentrations: 10% in rinse-off skin cleansing; 6.1% in leave-on body/hand products. These are reported concentrations, not product recommendations.

Chinese historical-use references in the PPT: approximately 10% rinse-off and 1.25% leave-on. Historical use is not a recommended level; the latest official inventory/public information governs interpretation.

The source describes peer-reviewed assessment, multiple categories/concentrations, Chinese use records, and rinse-off/leave-on applications.

Sources: Johnson et al. Int J Toxicol. 2024; Chinese ingredient-inventory public-use information. Regulatory/database statements are retained from the supplied PPT and have not been independently updated for this conversion.

25 · Safety Assessment Foundation

Johnson W Jr, Bergfeld WF, Belsito DV, et al. Safety Assessment of Alkanoyl Lactyl Lactate Salts as Used in Cosmetics. Int J Toxicol. 2024;43(4 Suppl). DOI: 10.1177/10915818241259694.

The source summarizes the Expert Panel conclusion as safe under current uses/concentrations when formulated to be nonirritating and nonsensitizing. This assessment includes the family containing Sodium Lauroyl Lactylate.

Foundation: established use, peer-reviewed assessment, rinse-off/leave-on contexts, and INCI recognition. This is a formulation-safety framework.

Source link: https://doi.org/10.1177/10915818241259694

26 · One Ingredient, Multiple Formulation Advantages

Emulsify: oil/water interface management. Cleanse: mild-system design. Stabilize: uniform dispersions. Condition: skin/hair sensory properties. Lipid compatibility: support for barrier-lipid formulations. Skin + Hair: dual application.

PuriActives® SLL integrates emulsifier, surfactant, and lipid-system support functions in a lactylated amphiphilic molecule.

27 · More Than an Emulsifier

Smarter interface management. Better cleansing/care sensory experience. Broader possibilities from skin to hair.

PuriActives® SLL: The Lactylate Interface for Modern Skin & Hair Care.

PuriPharm Co., Ltd. INCI: SODIUM LAUROYL LACTYLATE.

28 · Scientific References

Peer-reviewed literature, patent publications, databases, and regulatory sources from the presentation are retained below. Patents list publication numbers, titles, and years; applicant information is outside the source material.

Source link: https://doi.org/10.3390/ijms24119283

Source link: https://doi.org/10.1177/10915818241259694

Source link: https://pubchem.ncbi.nlm.nih.gov/compound/Sodium-lauroyl-lactylate

Source link: https://ec.europa.eu/growth/tools-databases/cosing/

PEER-REVIEWED LITERATURE

1. Gooran N, Tan SW, Yoon BK, Jackman JA. Unraveling Membrane-Disruptive Properties of Sodium Lauroyl Lactylate and Its Hydrolytic Products: A QCM-D and EIS Study. International Journal of Molecular Sciences. 2023;24(11):9283. DOI: 10.3390/ijms24119283

2. Johnson W Jr, Bergfeld WF, Belsito DV, et al. Safety Assessment of Alkanoyl Lactyl Lactate Salts as Used in Cosmetics. International Journal of Toxicology. 2024;43(4 Suppl). DOI: 10.1177/10915818241259694

PATENTS

WO2007100784A2 (2007)— Acyl lactylate compositions for rinse-out and leave-on applications for skin and hair.

EP0562720A1 (1993)— Hair shampoo.

WO1998027193A1 (1998)— Personal cleansing bar composition containing sodium lauroyl lactylate.

US20240000681A1 (2024)— Chemical compositions providing long-lasting skin pH control for improving skin-barrier function and treatment of skin-barrier disorders.

DATABASES & REGULATORY SOURCES

PubChem — Sodium Lauroyl Lactylate

EU CosIng — Sodium Lauroyl Lactylate

Cosmetic Ingredient Review / Expert Panel for Cosmetic Ingredient Safety

Current Chinese Inventory of Existing Cosmetic Ingredients and official public ingredient-use information

Patents list publication numbers, titles, and years; applicant information is outside this material.

NanoActive™ 10-HDA

01 · NanoActive™ 10-HDA: Nano-Encapsulated Royal Jelly Acid

Advanced liposomal active ingredient. Powered by PURISOME® FlexVes™ flexible-vesicle liposome technology. Royal Jelly, Re-Engineered. PuriPharm Co., Ltd.

02 · The Royal Jelly Signature Molecule

Royal jelly contains proteins, sugars, lipids, amino acids, and trace components. 10-HDA is a characteristic fatty acid and a marker in research and quality evaluation. It provides a defined molecular active beyond the traditional natural-ingredient concept.

Identity: 10-Hydroxy-2-Decenoic Acid; 10-HDA/10-H2DA; Queen Bee Acid; Royal Jelly Acid; a medium-chain ω-hydroxy unsaturated fatty acid and characteristic royal jelly lipid.

10-HDA is a multifunctional bioactive lipid. Whole-royal-jelly effects cannot all be attributed to it; this presentation focuses on the lipid’s evidence.

03 · From Royal Jelly to 10-HDA

Traditional natural origin, molecular precision, and nano delivery.

1 Royal jelly, a traditional natural ingredient. 2 Identify the signature bioactive lipid. 3 Define molecular 10-HDA. 4 Study multiple skin biological pathways. 5 NanoActive™ liposomal delivery.

Applications: premium skin and scalp care. Defined. Studied. Delivered.

04 · 10-HDA Molecular Science

2D structure source: PubChem CID 5312738.

Formula C10H18O3; molecular weight approximately 186.25. Structure: α,β-unsaturated carboxylic acid, terminal hydroxyl, and a medium-chain fatty acid backbone. Class: medium-chain ω-hydroxy unsaturated fatty acid.

Potential: lipid interactions with skin lipids; hydroxyl-mediated hydrogen bonding; amphiphilic biofilm interactions; and a structural basis for epidermal biology research.

05 · One Royal Jelly Lipid, Multiple Skin Pathways

Seven research directions: barrier support, moisture/NMF, environmental stress defense, collagen/photoaging, skin tone, microbiome support, and soothing.

The presentation organizes an evidence network around one defined bioactive lipid. This mechanism map does not establish finished-product clinical efficacy.

06 · Filaggrin: From 10-HDA to Natural Moisturizing Factors

Gu, Zeng, and Maeda (2017) found induction of filaggrin and free amino acids in cultured 3D human epidermis. This extends hydration concepts into cornification and NMF biology.

Key findings: increased filaggrin expression, FLG mRNA/protein, stratum-corneum free amino acids, and support for NMF formation.

Pathway: 10-HDA, increased filaggrin, free amino acids, NMF reserves, and moisture-retention/barrier appearance concepts.

Source: Cosmetics. 2017;4(4):48. DOI: 10.3390/cosmetics4040048. In vitro 3D epidermis.

07 · Barrier Mechanism Map

From keratinocytes to the stratum corneum: differentiation support, increased granular-layer filaggrin, amino acid release, NMF reserves, hydration, and a stronger-looking barrier.

Layer schematic: stratum corneum, NMF/hydration; stratum granulosum, filaggrin processing and amino acids/NMF; keratinocytes, differentiation/cornification and the proposed 10-HDA starting point.

Source: Gu et al. Cosmetics. 2017;4(4):48. DOI: 10.3390/cosmetics4040048. The diagram illustrates mechanisms and does not establish product penetration depth.

08 · NQO1: Supporting Epidermal Stress Defense

Okumura et al. (2021) identified 10-HDA as an important royal jelly fatty acid inducing NQO1, an antioxidant/detoxification enzyme.

Care contexts: UV oxidative stress, ROS accumulation, pollution/environmental stress, and early oxidative-aging signs. The positioning is defense support, without sunscreen or medicinal claims.

Pathway: 10-HDA, cellular stress-response signals, increased NQO1, enhanced antioxidant defense, and reduced oxidative-stress burden.

Source: Int J Mol Sci. 2021;22(23):12973. DOI: 10.3390/ijms222312973. In vitro cellular/epidermal models.

09 · 10-HDA and UVA-Induced Dermal Damage

Human dermal fibroblast pathway: UVA, increased ROS, JNK/p38 signaling, increased MMP-1/MMP-3, and collagen breakdown/photoaging.

10-HDA findings: lower ROS and senescence-related changes, modulated MMP-1/MMP-3, supported type I collagen expression, and protection against UVA cellular damage.

Zheng et al. (2013) connect ROS management with downstream MMP modulation and collagen protection.

Source: J Eur Acad Dermatol Venereol. 2013;27:1269–1277. DOI: 10.1111/j.1468-3083.2012.04707.x. In vitro human fibroblasts.

10 · Royal Jelly Biology and Collagen Science

This section concerns whole royal jelly, separate from purified 10-HDA.

Park et al. (2011), human skin fibroblast UVB model: royal jelly enhanced collagen production, with TGF-β1-related responses, type I procollagen, and extracellular-matrix support.

Concept: protect and preserve youthful-looking skin. Whole royal jelly and 10-HDA findings inform complementary collagen narratives, but whole-royal-jelly results cannot be fully attributed to 10-HDA. The source schematic includes Royal Jelly/10-HDA; the experiment itself tested whole royal jelly.

Source: J Med Food. 2011;14(9):899–906. DOI: 10.1089/jmf.2010.1363. In vitro.

11 · 10-HDA and Melanogenesis

Peng et al. (2017) studied B16F1 melanoma cells and topical mouse skin, showing melanogenesis inhibition involving MITF, Tyrosinase, and TRP pathways.

Models assessed melanin/tyrosinase and topical tone-related indicators. Multi-target concepts support clearer-looking tone and appearance; no pigment-disease treatment claims.

Pathway: 10-HDA inhibition, MITF modulation, Tyrosinase, TRP-1/TRP-2, and melanin synthesis.

Source: BMC Complement Altern Med. 2017;17:392. DOI: 10.1186/s12906-017-1888-8.

12 · Staphylococcus aureus Biofilm Research

In vitro findings: reduced biofilm formation, EPS production, adhesion, aggregation, and mature-biofilm viability.

Genes: reduced sarA, agrA, and hla, associated with biofilm regulation, quorum signaling, and α-hemolysin virulence.

Positioning: a microbiome-friendly skin-purifying strategy managing unfavorable biofilms and environments. Care concepts include oily/blemish-prone skin, sensitive-skin microbiome care, scalp care, skin cleansing care, and fragile barriers. These findings do not establish selective support for all beneficial species.

Gao et al. Molecules. 2022;27(5):1485. DOI: 10.3390/molecules27051485.

13 · The Delivery Challenge

01 Poor aqueous solubility limits direct water-based use. 02 Limited oil solubility constrains conventional oil delivery. 03 Free-state penetration depends on dosage-form design. 04 Direct addition can be difficult to disperse and restrict formulation options.

Biological activity does not by itself establish bioavailability at the intended interface.

14 · PURISOME® FlexVes™: Why Liposomes

A lipid-bilayer vesicle is a membrane-related carrier architecture for loading/dispersing 10-HDA. It aims to improve aqueous dispersion, compatibility with stratum-corneum lipids, and delivery/deposition potential.

Values: nanoscale delivery, lipid compatibility, dispersion, skin-deposition potential, controlled skin interactions, and formulation flexibility.

The vesicle image is a mechanism schematic, not measured particle-size or encapsulation-efficiency data.

15 · 2026 Independent Nano-Delivery Evidence

Gao et al. (2026) studied Hyalurosomes encapsulating a 10-HDA/matrine deep eutectic solvent, using ex vivo skin and cellular models.

Formulation/delivery: improved dissolution/dispersion and stability, with increased deposition in stratum corneum, viable epidermis, and dermis.

Cells: reduced HaCaT ROS, IL-1α/IL-6/TNF-α; increased HaCaT migration; reduced HFF-1 senescence phenotype.

The formulation is distinct from NanoActive™ 10-HDA. It supports the delivery strategy and does not constitute direct product evidence.

Int J Pharm. 2026;701:127150. DOI: 10.1016/j.ijpharm.2026.127150.

16 · Free and Nano-Encapsulated 10-HDA

Free 10-HDA: limited solubility, dispersion, penetration, and formulation choices.

NanoActive™ 10-HDA with PURISOME® FlexVes™: liposomal dispersion, a skin-compatible lipid carrier, improved delivery potential, greater formulation versatility, and modern skin-care design.

Better delivery offers greater opportunity for biological activity; product performance still requires direct testing.

17 · Integrated Mechanism Network

Epidermis: filaggrin, amino acids/NMF, moisture/barrier. Dermis: lower ROS/MMP-1/MMP-3, collagen preservation. Stress defense: NQO1 and oxidative-defense support. Pigmentation: MITF/Tyrosinase/TRP and even-looking tone. Microbiome: biofilm/virulence modulation and skin-environment concepts.

One bioactive lipid, multiple pathways. The network combines Gu 2017, Okumura 2021, Zheng 2013, Peng 2017, and Gao 2022, retaining their original model-level attribution.

18 · Five Core Skincare Values

01 Barrier recovery: filaggrin/NMF and hydration foundations. 02 Anti-stress defense: NQO1-related epidermal defenses. 03 Photoaging care: ROS/MMP and collagen protection. 04 Tone: MITF/Tyrosinase-related pathways for dull/uneven appearance. 05 Microbiome: unfavorable-biofilm management and skin-environment support.

Barrier × Defense × Collagen × Tone × Microbiome connects mechanisms to formulation concepts.

19 · Scalp Is Skin

Scalp pressures: fragile barrier/moisture loss, oxidative stress, microbial imbalance, inflammatory environments, and sebum/pollution.

Skin mechanisms inform scalp concepts: Filaggrin/NMF for hydration; NQO1 for stress defense; biofilm management for microbial care; soothing pathways for comfort. These concepts require scalp-specific validation.

Healthy scalp, a better environment for beautiful hair. The positioning does not claim direct hair growth.

20 · Royal Jelly and Scalp Research Clues

A 2024 clinical observation of a medicated hair tonic containing royal jelly extract associated the combination product with improved scalp moisture/condition and hair condition. Dermal papilla experiments reported changes in some growth-related genes.

Other actives were present; results cannot all be attributed to royal jelly extract or 10-HDA.

NanoActive™ positioning: scalp barrier, moisture, soothing, antioxidant defense, and microbiome care. Skin health guides scalp ecological concepts.

J Soc Cosmet Chem Jpn. 2024;58(1):55–64. DOI: 10.5107/sccj.58.55. Combination-product clinical observation and cell experiments.

21 · Skincare Applications

Anti-aging serum, repair serum, barrier cream, sensitive-skin serum, overnight recovery, tone-care serum, blemish-prone care, microbiome products, urban-defense serum, eye-contour care, premium royal jelly concepts, and post-treatment-inspired care.

Royal Jelly Renewal Serum: photoaging/collagen concept. Barrier Defense Cream: Filaggrin–NMF hydration concept. Bio-Balance Repair Essence: biofilm-management concept.

22 · Scalp and Hair Applications

Scalp serum, ampoule, shampoo, soothing mist, dry-scalp lotion, oily-scalp essence, post-color/perming scalp care, anti-pollution serum, and premium aging scalp care.

Royal Scalp Defense Serum: antioxidant/environmental defense. Scalp Barrier Booster: daily barrier/hydration care. Nano Royal Jelly Scalp Essence: premium nano-delivery and microbiome concepts.

23 · Value for Formulators

01 Easier incorporation addresses free-active solubility, dispersion, and penetration challenges. 02 Lipid-compatible delivery. 03 Water-based formulation design for serums/lotions. 04 Multiple barrier, antioxidant, aging, tone, and microbiome concepts. 05 Premium storytelling: Royal Jelly × Molecular Science × Nano Delivery.

Nature × Molecule × Nanotechnology combines natural-origin narrative, molecular evidence, and delivery design.

24 · Royal Jelly, Re-Engineered

01 A signature royal jelly lipid. 02 Filaggrin/NMF hydration. 03 Epidermal defense and collagen-protection research. 04 Microbiome/tone concepts. 05 Advanced liposomal design to address practical delivery barriers.

NanoActive™ 10-HDA, powered by PURISOME® FlexVes™.

25 · Positioning Matrix

Traditional royal jelly: a strong natural narrative with complex composition. Free 10-HDA: a defined molecule with formulation/delivery challenges. NanoActive™ 10-HDA: Defined Bioactive + Nano Delivery; Molecular Precision + Advanced Delivery.

Horizontal axis: evolution of active form. Vertical axis: narrative/scientific level. The schematic positions the product at molecular precision and advanced delivery; it is a qualitative positioning map, not quantitative comparative data.

26 · References

All ten references from the presentation are retained below.

Molecular-structure source: PubChem CID 5312738. The science concerns 10-HDA (10-Hydroxy-2-Decenoic Acid, C10H18O3), distinct from 10-Hydroxydecanoic Acid (10-HDAA). Final INCI follows the formal PuriPharm Co., Ltd. TDS/SPEC.

PuriPharm Co., Ltd. Royal Jelly, Re-Engineered.

1. Gu L, Zeng H, Maeda K. 10-Hydroxy-2-Decenoic Acid in Royal Jelly Extract Induced Both Filaggrin and Amino Acid in a Cultured Human Three-Dimensional Epidermis Model. Cosmetics. 2017;4(4):48. DOI: 10.3390/cosmetics4040048.

2. Zheng J, Lai W, Zhu G, et al. 10-Hydroxy-2-Decenoic Acid Prevents Ultraviolet A-Induced Damage and Matrix Metalloproteinases Expression in Human Dermal Fibroblasts. J Eur Acad Dermatol Venereol. 2013;27:1269–1277. DOI: 10.1111/j.1468-3083.2012.04707.x.

3. Park HM, Hwang E, Lee KG, et al. Royal Jelly Protects Against Ultraviolet B-Induced Photoaging in Human Skin Fibroblasts via Enhancing Collagen Production. J Med Food. 2011;14(9):899–906. DOI: 10.1089/jmf.2010.1363.

4. Peng CC, Sun HT, Lin IP, et al. The Functional Property of Royal Jelly 10-Hydroxy-2-Decenoic Acid as a Melanogenesis Inhibitor. BMC Complement Altern Med. 2017;17:392. DOI: 10.1186/s12906-017-1888-8.

5. Okumura N, Ito T, Degawa T, et al. Royal Jelly Protects against Epidermal Stress through Upregulation of the NQO1 Expression. Int J Mol Sci. 2021;22(23):12973. DOI: 10.3390/ijms222312973.

6. Gao K, Su B, Dai J, et al. Anti-Biofilm and Anti-Hemolysis Activities of 10-Hydroxy-2-Decenoic Acid against Staphylococcus aureus. Molecules. 2022;27(5):1485. DOI: 10.3390/molecules27051485.

7. Perminaite K, Fadda AM, Sinico C, Ramanauskiene K. Formulation of Liposomes Containing Royal Jelly and Their Quality Assessment. DOI: 10.1166/jnn.2021.19053.

8. Gao C, Liu F, Yang S, Wang Q, Yang C, Liang R. 10-Hydroxy-2-Decenoic Acid/Matrine Deep Eutectic Solvent Encapsulated in Hyalurosomes for Enhanced Transdermal Delivery and Antioxidant Efficacy. Int J Pharm. 2026;701:127150. DOI: 10.1016/j.ijpharm.2026.127150.

9. Enhanced Skin Penetration of 10-Hydroxy-2-Decenoic Acid via Anionic Polymer Formulations and Skin Hydration Modulation. J Dermatologic Sci Cosmet Technol. 2026;3(1):100144. DOI: 10.1016/j.jdsct.2025.100144.

10. The Effectiveness of Medicated Hair Tonic Containing Royal Jelly Extract. J Soc Cosmet Chem Jpn. 2024;58(1):55–64. DOI: 10.5107/sccj.58.55.