NanoActive™ r-Retinoate

NanoActive™ r-Retinoate

A new-generation, high-performance vitamin A active

8×RETINOL POWERHigh efficacy at low concentration · High stability · Potential for high tolerabilityA new-generation hybrid retinoid INCI Retinyl Retinoate

PuriPharm Co. Ltd.

Source:Structure: PubChem CID 10303376. The 8× claim refers only to the low-concentration in vitro collagen synthesis experiment detailed in “8× Retinol-Level Collagen Performance.”

01 MOLECULAR DESIGN

The traditional vitamin A trade-off

Traditional vitamin A actives rarely combine activity, stability, and tolerability

Retinoid Core attribute Key limitation
Retinoic Acid High activity Higher irritation potential and greater restrictions on use
Retinol Gold standard Sensitive to light, heat, oxygen, and other factors
Retinyl Esters High stability Usually lower biological activity

High activity + High stability + High tolerability

What if one vitamin A molecule could offer all three?

Next: the hybrid retinoid architecture

Source:Kim H, Kim B, Kim H, et al. “Synthesis and in vitro biological activity of retinyl retinoate, a novel hybrid retinoid derivative.” Bioorganic & Medicinal Chemistry. 2008;16(12):6387–6393. DOI: 10.1016/j.bmc.2008.05.005.

01 MOLECULAR DESIGN

Hybrid Retinoid molecular architecture

One molecule combines the structural logic of two classic retinoids

RETINOL + RETINOIC ACID

Esterification forms RETINYL RETINOATE

No. Design logic
01 Block the Retinoic Acid carboxyl group
02 Preserve the key retinoid ring structure and polyene chain
03 Rebalance activity, stability, and tolerability

Source:Kim H, Kim B, Kim H, et al. “Synthesis and in vitro biological activity of retinyl retinoate, a novel hybrid retinoid derivative.” Bioorganic & Medicinal Chemistry. 2008;16(12):6387–6393. DOI: 10.1016/j.bmc.2008.05.005. Structure: PubChem CID 10303376.

01 MOLECULAR DESIGN

NanoActive™ r-Retinoate · Product overview

Core molecular information and market positioning

Item Information
Product NanoActive™ r-Retinoate
INCI name Retinyl Retinoate
Category Hybrid RetinoidVitamin A derivativeAnti-aging active
Molecular data Formula C₄₀H₅₆O₂Molecular weight 568.87CAS 15498-86-9
Absorption maximum λmax 333 nm; Retinol 323 nm

8× Retinol collagen performancePhotostable retinoidImproved thermal stabilityDirect retinoid bioactivityHyaluronan boostHigh efficacy at low concentrationSkin and scalp applicationsCompatible with nano-delivery

Source:PubChem CID 10303376; Kim H, Kim B, Kim H, et al. “Synthesis and in vitro biological activity of retinyl retinoate, a novel hybrid retinoid derivative.” Bioorganic & Medicinal Chemistry. 2008;16(12):6387–6393. DOI: 10.1016/j.bmc.2008.05.005. Appearance, active content, particle size, PDI, carrier composition, recommended use level, pH, addition temperature, and storage conditions must follow the latest PuriPharm TDS / SPEC / COA.

02 COLLAGEN PERFORMANCE

8× Retinol-level collagen performance

Approximately eight times the collagen synthesis response of Retinol at low concentration

8×Collagen biosynthesis at low concentration41.29% ÷ 4.94% ≈ 8.36× Retinol+4.94%Retinyl Retinoate+41.29%

Test concentration: 10⁻⁶% (w/v)

Lower concentration, more collagen

Source:*In an in vitro collagen synthesis experiment at 10⁻⁶% (w/v), Retinyl Retinoate increased collagen synthesis by 41.29%, versus 4.94% with Retinol, equivalent to approximately 8.36×. US7173062B2, “Method for the Improvement of Skin Wrinkles Using Retinyl Retinoate.” See also Kim H, Kim B, Kim H, et al. “Synthesis and in vitro biological activity of retinyl retinoate, a novel hybrid retinoid derivative.” Bioorganic & Medicinal Chemistry. 2008;16(12):6387–6393. DOI: 10.1016/j.bmc.2008.05.005.

02 COLLAGEN PERFORMANCE

Lower concentration, more collagen

Retinyl Retinoate shows strong collagen synthesis performance even at low concentrations

Concentration Retinoic Acid Retinol Retinyl Palmitate Retinyl Retinoate
0.1 μM 1% 1.5%
1 μM 14% 10% 2% 14%
10 μM 52% 42% 14% 48%

High efficacy at low concentration

Outperforms Retinol in the low-concentration range and approaches Retinoic Acid at some concentrations

Metric: increase in collagen synthesis (%)

Source:Kim H, Kim B, Kim H, et al. “Synthesis and in vitro biological activity of retinyl retinoate, a novel hybrid retinoid derivative.” Bioorganic & Medicinal Chemistry. 2008;16(12):6387–6393. DOI: 10.1016/j.bmc.2008.05.005. Redrawn from Figure 6. Bar values are visual readings from the axes and preserve the trend reported in the article.

02 COLLAGEN PERFORMANCE

A retinoid with direct biological activity

The molecule can display retinoid activity without first undergoing complete hydrolysis

Route Sequence Interpretation
Traditional Retinyl Ester Retinyl Ester → Retinol → Retinal → Retinoic Acid → RAR Requires multiple conversion steps before entering RAR signaling
Retinyl Retinoate Retinyl Retinoate → observed biological effect Direct retinoid activity

HPLC evidence

After two days of incubation with normal human skin fibroblasts, HPLC detected no new peaks corresponding to Retinol or Retinoic Acid.

The authors therefore attributed the observed biological activity to the molecule itself rather than simple hydrolysis.

Not an ordinary retinyl ester

Source:Kim H, Kim B, Kim H, et al. “Synthesis and in vitro biological activity of retinyl retinoate, a novel hybrid retinoid derivative.” Bioorganic & Medicinal Chemistry. 2008;16(12):6387–6393. DOI: 10.1016/j.bmc.2008.05.005.

02 COLLAGEN PERFORMANCE

Promotes synthesis and limits degradation

Bidirectional collagen management through RAR, AP-1, and collagen signaling

Photoaging cascade Direction associated with NanoActive™ r-Retinoate
UV / environmental stress → c-Jun / AP-1 ↑ → collagenase / MMP ↑ → collagen degradation → wrinkles Retinoid signaling / RAR → AP-1 / c-Jun ↓
Collagen degradation Promotes synthesis: Collagen Biosynthesis ↑
Increased collagenase / MMP Reduces degradation signals: Collagenase / MMP ↓

52%

Collagenase inhibition

Retinyl Retinoate > Retinol

Source:Kim H, Kim B, Kim H, et al. “Synthesis and in vitro biological activity of retinyl retinoate, a novel hybrid retinoid derivative.” Bioorganic & Medicinal Chemistry. 2008;16(12):6387–6393. DOI: 10.1016/j.bmc.2008.05.005. With RARα expression, collagenase expression was inhibited by approximately 33% with Retinol, 52% with Retinyl Retinoate, and 64% with Retinoic Acid; also supported by US7173062B2, “Method for the Improvement of Skin Wrinkles Using Retinyl Retinoate.”

03 STABILITY & TOLERABILITY

Designed for photostability

Retinoid performance that withstands light exposure

48 h

UVA photostability

The main structure retained markedly greater stability even after 48 hours of UVA exposure.

UVA: 356 nm; observations at 2, 12, 24, and 48 hours

Compound 0 h 2 h 12 h 24 h 48 h
Retinyl Retinoate Baseline Stable Stable Stable Only minor noise / no qualitative change
Retinol Baseline Clear degradation No longer reliably identified qualitatively No longer reliably identified qualitatively No longer reliably identified qualitatively

λmax: Retinol 323 nm; Retinyl Retinoate 333 nm

Source:Kim H, Kim B, Kim H, et al. “Synthesis and in vitro biological activity of retinyl retinoate, a novel hybrid retinoid derivative.” Bioorganic & Medicinal Chemistry. 2008;16(12):6387–6393. DOI: 10.1016/j.bmc.2008.05.005.; US7173062B2, “Method for the Improvement of Skin Wrinkles Using Retinyl Retinoate.” Photostability experiment: UVA 356 nm and qualitative ¹H NMR. “48 h” is the study duration, not a direct quantitative claim of percentage remaining.

03 STABILITY & TOLERABILITY

Stability beyond light exposure

Thermal stability was clearly better than Retinol after four weeks under accelerated conditions

Four-week condition Retinol remaining Retinyl Retinoate remaining
Room temperature 52.23% 89.21%
40°C 34.51% 68.23%
4°C 95.52% 99.65%

Improved thermal stabilityMore robust formulationsMore reliable retinoid performance

Source:US7173062B2, “Method for the Improvement of Skin Wrinkles Using Retinyl Retinoate.” Thermal stability experiment: HPLC quantification after four weeks at room temperature, 40°C, and 4°C.

03 STABILITY & TOLERABILITY

High performance with greater mildness

A wider cellular tolerance window and evidence from a human occlusive patch test

In vitro MTT IC₅₀
+60%IC₅₀ versus RetinolLower cytotoxicity in this in vitro model In vitro MTTIC₅₀Retinol25 μMRetinyl Retinoate40 μM
24 h human occlusive patch test Concentration Irritation index; lower is better
Retinol 0.075% 2.5
r-Retinoate 0.075% 1.3
r-Retinoate 0.30% 1.3
r-Retinoate 0.55% 1.3

High performance and low irritation in the same profile

Source:Kim H, Kim B, Kim H, et al. “Synthesis and in vitro biological activity of retinyl retinoate, a novel hybrid retinoid derivative.” Bioorganic & Medicinal Chemistry. 2008;16(12):6387–6393. DOI: 10.1016/j.bmc.2008.05.005. Normal human skin fibroblast MTT assay: IC₅₀ 40 μM versus 25 μM for Retinol. Human occlusive patch data: US7173062B2, “Method for the Improvement of Skin Wrinkles Using Retinyl Retinoate.”

04 BEYOND COLLAGEN

7.8× hyaluronan production

Extending from wrinkle care to hydration, plumpness, and barrier support

7.8×

Hyaluronan production

Primary human keratinocytes; 1 μM / 24 hRetinaldehyde ≈ 7.6× control

Mechanistic path Outcome
Retinyl Retinoate → HAS2 ↑ Hyaluronan ↑
Hyaluronan ↑ → CD44 interaction Hydration · ECM support · Homeostasis

Retinyl Retinoate upregulated HAS2 and increased CD44-related expression.

Source:Kim JE, Kim B, Kim H, et al. “Retinyl retinoate induces hyaluronan production and less irritation than other retinoids.” Journal of Dermatology. 2010;37(5):448–454. DOI: 10.1111/j.1346-8138.2010.00808.x. In primary human keratinocytes, Retinyl Retinoate at 1 μM for 24 h induced hyaluronan production to approximately 7.8 times the control level.

04 BEYOND COLLAGEN

High activity with less barrier disruption

Lower TEWL impact at the same 0.05% concentration

Retinoid Relative TEWL / barrier disruption ranking
Retinyl Retinoate Lowest
Retinol Low
Retinoic Acid High
Retinaldehyde High

7.8× hyaluronan production + lower TEWL disruption

A better balance of efficacy and tolerability

Source:Kim JE, Kim B, Kim H, et al. “Retinyl retinoate induces hyaluronan production and less irritation than other retinoids.” Journal of Dermatology. 2010;37(5):448–454. DOI: 10.1111/j.1346-8138.2010.00808.x. Hairless-mouse TEWL model with 0.05% comparative application. The ranking redraws the irritation order reported in the article.

05 CLINICAL EVIDENCE

Human evidence with a Retinol comparator

Uncommon direct human comparison against Retinol

0.06%Retinyl RetinoateSignificantly better than 0.075% Retinol 46Korean women · Periorbital wrinklesTwo randomized clinical studies
Study Duration and completers Intervention Frequency
Study 1 12 weeks; 24 completed 0.06% Retinyl Retinoate versus placebo Twice daily
Study 2 8 weeks; 22 completed 0.06% Retinyl Retinoate versus 0.075% Retinol Twice daily

Assessments: global photoaging score · photographs · skin replicas · Visiometer

Wrinkles improved significantly with Retinyl Retinoate versus placebo and Retinol.

Source:Kim H, Kim N, Jung S, et al. “Improvement in skin wrinkles from the use of photostable retinyl retinoate: a randomized controlled trial.” British Journal of Dermatology. 2010;162(3):497–502. DOI: 10.1111/j.1365-2133.2009.09483.x. Skin-replica analysis showed significant improvement, particularly in mean roughness.

05 CLINICAL EVIDENCE

22% greater improvement in maximum roughness

A 12-week double-blind randomized comparison versus 0.075% Retinol

Study design Information
+22%R2 maximum roughnessImprovement rate versus Retinol Study designInformationDesignProspective · Double-blind · Randomized · ControlledParticipants11 Korean women; 35–56 yearsDuration / frequency12 weeks; twice dailyComparison0.06% Retinyl Retinoate versus 0.075% RetinolAnalysisVisiometer R2; 12-week head-to-head comparison

Validated dimensions: fine-line reduction, elasticity, visual wrinkle grade, skin roughness, and dermal distance / intensity.

Source:Kim H, Koh J, Baek J, et al. “Retinyl retinoate, a novel hybrid vitamin derivative, improves photoaged skin: a double-blind, randomized-controlled trial.” Skin Research and Technology. 2011;17(3):380–385. DOI: 10.1111/j.1600-0846.2011.00512.x. At 12 weeks, the improvement rates for visual wrinkles and R2 maximum roughness were 22% higher than with Retinol.

05 CLINICAL EVIDENCE

Beyond anti-aging

Retinoid science for blemish-prone and oily skin

Protocol: 0.05% Retinyl Retinoate · 8 weeks · double-blind · vehicle-controlled · split-face; 15 women with mild-to-moderate acne.

Eight-week outcome Vehicle Retinyl Retinoate
Total lesion count −26.47% −38.58%
Inflammatory lesions −35.14% −43.62%
Non-inflammatory lesions −19.79% −33.98%

−27.18%

Forehead sebum

Baseline 104.86 μg/cm²; week 8: 76.36 μg/cm²

Blemish-prone skin careSebum balanceFollicular keratinization careClearer-looking skin

Source:Kim B, et al. “Retinyl Retinoate, a Retinoid Derivative Improves Acne Vulgaris in Double-blind, Vehicle-controlled Clinical Study.” Tissue Engineering and Regenerative Medicine. 2013;10(5):260–265. DOI: 10.1007/s13770-012-1088-z. Percentages are reductions in lesion counts after eight weeks; the change in sebum was statistically significant.

06 DELIVERY PLATFORM

Molecule × nano-delivery

Unlocking the full potential of r-Retinoate

Retinyl Retinoate is highly lipophilic, so formulation must solve several engineering challenges:

01 Dispersibility02 Stability03 Drug loading04 Skin delivery05 Controlled release

RETINYL RETINOATE + Nano-delivery

A performance-optimized retinoid delivery system

Published NLC feasibility evidence Value
Particle size 230–300 nm
PDI No value listed in the source slide
PRECIROL-NLC encapsulation efficiency 97.8%
COMPRITOL-NLC encapsulation efficiency 93.8%

These values describe a published NLC system and are not specifications for NanoActive™ r-Retinoate.

Source:Lee SG, Jeong JH, Kim SR, et al. “Topical formulation of retinyl retinoate employing nanostructured lipid carriers.” Journal of Pharmaceutical Investigation. 2012;42(5):243–250. DOI: 10.1007/s40005-012-0036-1. Particle size, PDI, encapsulation efficiency, and carrier parameters for NanoActive™ itself must follow authentic PuriPharm TDS / SPEC / COA documents.

06 DELIVERY PLATFORM

Encapsulation amplifies delivery performance

Independent research shows that advanced delivery can further enhance Retinyl Retinoate

Form Exposure / penetration Delivery performance
Free RR Conventional exposure; limited penetration
Encapsulated RR Improved penetration More efficient delivery; enhanced anti-wrinkle performance

Encapsulation → Improved penetration → More efficient delivery → Enhanced anti-wrinkle performance

+6.05%Visual wrinkle improvement +8.03%R2 maximum roughness

Source:Kim H, et al. “Novel anti-wrinkle effect of cosmeceutical product with new retinyl retinoate microsphere using biodegradable polymer.” Skin Research and Technology. 2012;18(1):70–76. DOI: 10.1111/j.1600-0846.2011.00533.x. Outcomes compare a 3% PLA–retinyl retinoate (2%) microsphere cream with a 0.06% Retinyl Retinoate cream over four weeks. Published PLA microsphere evidence does not represent NanoActive™ technology.

07 APPLICATIONS

From face to scalp

Advanced retinoid science for scalp care

SkinWrinkle careCollagen renewalHyaluronan boostFirmingRefined texturePhotoaging careBlemish-prone skinSebum balance ScalpScalp renewalSebum balanceFollicular keratinization careScalp anti-agingPilosebaceous unit careHealthy follicular environment

Retinoid signaling is present in hair follicles, sebaceous glands, and interfollicular epidermis, and participates in epithelial differentiation, sebaceous biology, and follicular keratinization.

Source:Mechanistic background: Everts HB, Sundberg JP, King LE Jr, Ong DE. “Immunolocalization of enzymes, binding proteins, and receptors sufficient for retinoic acid synthesis and signaling during the hair cycle.” Journal of Investigative Dermatology. 2007;127(7):1593–1604. DOI: 10.1038/sj.jid.5700753. Scalp positioning covers scalp health, anti-aging, oil control, and support for the follicular environment. No direct hair-growth claim should be made without product-specific clinical evidence.

07 APPLICATIONS

One retinoid, multiple performance dimensions

Eight efficacy dimensions create a complete premium active platform

No. Performance dimension
01 8× Collagen Performance
02 Wrinkle Reduction
03 Photostability
04 Thermal Stability
05 Hyaluronan Boost
06 Better Tolerance
07 Blemish & Sebum Care
08 Scalp Renewal

Source:The efficacy dimensions summarize the preceding evidence. Each quantitative claim retains its experimental model, comparator, concentration, and source in the corresponding section.

07 APPLICATIONS

Designed for the next generation of beauty innovation

Premium dual applications across skin and scalp

Skin carePremium anti-aging serumLine-smoothing serumEye serum / eye creamNight repairDay-and-night retinoid productsPhotoaging careFirming and elasticity productsHydrating anti-aging productsBlemish-prone skin careOily-skin serum Scalp and hair careScalp anti-aging essenceScalp anti-aging serumScalp renewal serumOily-scalp serumFollicular environment careLeave-on scalp carePremium scalp ampoule

Formats: serum · cream · lotion · ampoule · eye care · scalp serum · leave-on care

Source:Application guidance is conceptual and based on published Retinyl Retinoate evidence. Recommended use level, pH, addition temperature, solubility, compatibility, storage conditions, and finished-product stability for NanoActive™ r-Retinoate must follow official PuriPharm TDS / SPEC / COA documents. No product-specific parameters are inferred here.

CLOSING

NanoActive™ r-Retinoate

Higher performance at a lower concentration. Redefining next-generation vitamin A anti-aging technology.

8× collagen performancePhotostabilityClinically evaluatedHyaluronan boostNano-delivery

A new-generation, high-performance vitamin A active

PuriPharm Co. Ltd.

Source:*“8× Retinol Power” is a marketing shorthand for an approximately 8.36-fold difference in low-concentration in vitro collagen synthesis performance: 41.29% versus 4.94% at 10⁻⁶% w/v. Source: US7173062B2. It does not mean 8× RAR activation, 8× human wrinkle reduction, 8× lower irritation, or 8× performance across all biological endpoints.

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