NanoActive™ r-Retinoate(리포좀)

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[NanoActive r-RETINOATE PRODUCT DATA SHEET] PRODUCT DATA SHEET Product Name: NanoActive r-RETINOATE Manufacturer: PuriPharm Co., Ltd. Awards: 2019 Ringier Technology Innovation Award (Personal Care) 1. Product Overview NanoActive r-RETINOATEis a next-generation, high-performance Vitamin A derivative engineered to overcome the traditional limitations of retinoid application in cosmetic science. Utilizing a proprietary 20–30 nm nano-encapsulation delivery system, this bioactive ingredient combines exceptional anti-aging efficacy with unprecedented stability and skin tolerability. Formed by esterifying the hydroxyl group of retinol with retinoic acid, Retinyl Retinoate retains the bioactivity of both precursor molecules. It delivers up to 8x the activity of standard retinol while eliminating the characteristic irritation and photosensitivity. Crucially, its distinctive blue-light absorption profile and high photostability make it a breakthrough retinoid that is completely safe and effective for daytime application. 2. Chemical Description & Composition INCI Name: Retinyl Retinoate, Ascorbic Acid (Vitamin C), Phospholipids, Caprylic/Capric Triglyceride, Glycerin, Water Product Type: Nano-encapsulated Bioactive System Active Concentration: Available in 1.0% or 5.0% Retinyl Retinoate specifications 3. Physical & Chemical Properties Appearance: Yellow-orange viscous liquid Odor: Characteristic pH Value: 5.0 – 8.0 Solubility: Amphiphilic (compatible with both water and oil phases) Photostability: Excellent (not light-sensitive; suitable for day-care formulations) 4. Platform Technology & Delivery System PuriPharm's advanced nano-delivery platform transforms how retinoids interact with the skin structure: Targeted Follicular Absorption: The 20–30 nm particle size allows the nanocarriers to accumulate efficiently within the hair follicle pathway. This creates a deep-skin "follicular reservoir" where actives can be retained rather than merely remaining on the skin's surface. Sustained Release Kinetics: Once deposited in the appendages, the nano-emulsion structure facilitates a controlled, slow-release mechanism that extends the activity window for more than 10 days, ensuring long-lasting efficacy without overwhelming the skin barrier. Unique Occlusion Effect: Nano-sized lipid carriers create a highly uniform, tight surface film, increasing residence time and local deposition of the active compound. 5. Mechanism of Action: The One-Step Advantage Traditional retinol formulations require a slow, three-step metabolic conversion (Retinyl Esters → Retinol → Retinal → Retinoic Acid) to become biologically active. NanoActive r-RETINOATE features a direct "One-Step Conversion."As a direct precursor, it is highly efficient and minimizes intermediate degradation. Biocompatibility & Cytotoxicity: In vitro data demonstrates that Retinyl Retinoate possesses significantly lower cytotoxicity compared to standard retinol. The IC50 of retinol is 25 μM, whereas the IC50 of NanoActive r-RETINOATE is 40 μM (an approximately 60% improvement in cellular tolerability), showcasing its ability to provide intense rejuvenation without the peeling, erythema, and barrier compromise associated with traditional Vitamin A. 6. Proven Cosmetic Benefits & Efficacy Data A. Profound Anti-Aging & UV Repair (12-Week Clinical Study) A controlled clinical trial comparing 0.06% Retinyl Retinoate (Group A) against 0.075% Retinol (Group B) applied twice daily demonstrated superior anti-aging performance: Elasticity Improvement: 90.9% of Group A subjects reported noticeable periocular elasticity improvement (vs. 81.8% in Group B). Photodamage Reversal: Group A exhibited an 8.61% measurable improvement in photodamage repair (vs. 7.43% in Group B). Longevity of Efficacy: NanoActive r-RETINOATE showed a significantly weaker "diminishing marginal effect," meaning anti-wrinkle benefits continued to compound and remain highly visible even over long-term (1 year+) usage. B. Hyaluronic Acid (HA) Expression In vivotesting on epidermal and dermal tissues (HABP staining) confirms that NanoActive r-RETINOATE significantly upregulates endogenous mucopolysaccharide (hyaluronic acid) synthesis, heavily outperforming both standard retinol and retinoic acid. C. Multi-Pathway Skin Enhancement Structural Integrity: Inhibits UV-induced Matrix Metalloproteinases (MMP) activity, reducing the breakdown of endogenous proteins, protecting elastic fibers, and promoting collagen synthesis. Tone & Clarity: Works synergistically with its Vitamin C component to inhibit tyrosinase, accelerate melanin metabolism, and reduce visible redness. Texture & Blemishes: Promotes healthy keratinocyte activity, increases epidermal thickness, and functions via multiple mechanisms to clear blemishes and accelerate the repair of acne marks. 7. Formulation Guidance NanoActive r-RETINOATE is engineered for formulation elegance and versatility: Recommended Use Level: 1.0% – 5.0% Optimum pH Range: 3.0 – 6.5 Processing: Simple to formulate. Add to the system at the final stage of manufacturing (post-emulsification, during the cooling phase) to protect the nanostructure. Compatibility: Highly compatible with a wide range of cosmetic matrices. Works exceptionally well in synergy with additional Hyaluronic Acid, Vitamin C, and biocomposite polysaccharides (e.g., hydrolyzed myrtle) for accelerated wrinkle-reduction claims. 8. Recommended Applications Daytime Anti-Aging Care: Day creams, lotions, and serums targeting fine lines, leveraging its unique photostability. Intensive Photodamage Repair: Post-sun recovery formulations and deep wrinkle repair treatments. Advanced Brightening: Radiance serums addressing hyperpigmentation and uneven skin tone (pairs perfectly with brightening regimens). Acne & Barrier Repair: Clarifying formulations aimed at treating blemishes, repairing acne marks, and thickening the epidermal layer. Disclaimer: This document is provided for informational and technical support purposes only, based on PuriPharm Co., Ltd [NanoActive r-Retinoate] Outline Special absorption spectrum,efficient absorption of blue light、good photostability Product introduction INCI： Retinyl retinoate,ascorbic acid,phospholipids,caprylic/capric triglyceride,glycerin,water Retinyl retinoate is a new vitamin A derivative with higher activity and no fear of light Vitamin A is an essential vitamin for the human body.It has been used in skin care products for more than half a century. Because VA derivatives(retinol、retinoic acid,ect.) are more sensitive to light,oxygen,temperature,and metal ions.And are more likely to cause skin redness,itchiness,tightness and other irritations.The application of skin care products has been relaticelylimited. The VA derivative used for   NanoActive r-Retinoate is retinyl retinoate,  with vitamin C distribution by nano package. Retinyl retinoate is obtained by esterification of the hyfroxyl group of retinol and retinoic acid,while avoiding the limitation of retinoil and retinoic acid in cosmetic applications. The particle size of the NanoActive r-Retinoate is 20-30nm.On the one hand,this particle size of  nano-emulsion can make the ative substance stable suspension in the nano-carrier.At the same time,it can make the active substance penetrate into the skin effectively and control the release rate of active substance. Product description INCI：Retinyl retinoate,ascorbic acid,phospholipids,caprylic/capric triglyceride,glycerin,water Appearance：yellow-orange viscous liquid Odor：characteristic odor PH:5.0-8.0 Retinyl retinoate：1.0% or 5% Recipe guidance Suitable PH：3.0-6.5 Recommended addition amount：1-5% Solubility：water-soluble,oil-soluble Usage：add at the end of the formula Other：Insensitivite to light,can be used in day care products. Applicable to the product [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, K [NanoActive r-RETINOATE] NanoActive r-RETINOATE 8× retinol activity Photostable • Non-irritating A next-generation vitamin A derivative Company Overview PuriPharm Biopharmaceutical Technology Co., Ltd. Delivering Beauty • Creating Value Focused on the research and development of bioactives. Specialized in the development of bioactive materials and functional ingredient systems. Combines scientific delivery technology with application-oriented product design. Dedicated to high-performance ingredients for beauty and personal care. Nano Delivery Technology One of the most widely studied and applied new formulation technologies. Applicable across pharmaceuticals, foods, cosmetics and other fields. Nano-bioactives are new products developed using nanodelivery systems. Improves solubility, stability, irritation profile and odor while offering unique biological effects. Fourth-Generation (4G) Cosmetic Ingredients Clearly defined ingredients and content Clearly defined targets Clear mechanism of action Formulations designed to preserve bioactivity Good solubility Stable and non-discoloring Easy to absorb A perfect combination of traditional medicine, modern biotechnology and nanotechnology. Unique Occlusion Effect Follicular Targeted Absorption Nanocarriers accumulate efficiently around the hair follicle pathway. This supports targeted delivery into deep skin appendages where actives can be retained and released. Key takeaway：Hair follicles provide an efficient access route for targeted nano-delivery. Smaller Particles Penetrate Deeper and in Greater Amounts Reduced particle size increases penetration depth in skin. Smaller particles also increase the delivered amount of active ingredient. The smaller the carrier, the deeper the penetration and the higher the delivery amount. Follicular Reservoir Enables Slow Release for More Than 10 Days Hair follicles act as a storage reservoir for the active ingredient. The active can be released gradually for more than 10 days after deposition. This supports long-lasting efficacy with sustained local availability. Long-lasting delivery：Slow release extends the activity window after follicular deposition. Vitamin A： A core scientific foundation for the product story Functions of Vitamin A in the Human Body Supports vision and visual signaling. Contributes to growth, reproduction and immune support. Involved in antioxidant defense, cell differentiation and gene transcription. Vitamin A and Nobel Prizes Vitamin A Is the Gold Standard in Anti-Aging Skincare Common Vitamin A Actives Used in Skincare Conversion to Retinoic Acid in Vivo Why It Won the Award 2019 Ringier Technology Innovation Award Vitamin A derivative suitable for daytime use Safe and low irritation Nano-encapsulation protects the active ingredient A breakthrough and a new technical approach for retinoid raw materials A distinctive retinoid concept that balances efficacy, stability and tolerability. Unique Absorption Spectrum Distinctive absorption profile Efficient blue-light absorption Good photostability Product Introduction Retinyl retinoate is obtained by esterifying the hydroxyl group of retinol with retinoic acid, while avoiding the application limits of retinol and retinoic acid in cosmetics. NanoActive r-RETINOATE has an encapsulated particle size of 20–30 nm. This nanoemulsion size keeps the active stably suspended in the nanocarrier, enhances skin penetration and helps control the release rate. Particle size：20–30 nm nano-encapsulation； Delivery effect：Stable suspension, enhanced penetration and controlled release Product Introduction Skincare Benefits of Retinyl Retinoate Efficacy Summary Product Description Formulation Guide Suitable Products Anti-aging products： Maintains collagen in the dermis and helps prevent excessive collagen degradation. When combined with hyaluronic acid and biocomposite polysaccharides (hydrolyzed myrtle), improvement in fine lines can be observed within one week. Brightening products： Works synergistically with vitamin C to inhibit tyrosinase, promote metabolism and accelerate fading of melanin. The source deck notes that pairing with vitamin C is also effective for acne-prone skin. Suitable Products Sunscreen products： Inhibits the UV-induced increase of MMP activity and helps protect elastic fibers and dermal collagen. Improves wrinkles and fine lines caused by UV exposure. Repair products： Promotes endogenous hyaluronic acid synthesis and reduces skin TEWL. Promotes keratinocyte activity and increases epidermal thickness, making the epidermis stronger. [纳米包裹视黄醇视黄酸酯（AA酯，NanoActive r-Retinoate）] 浦瑞生物医药大量提供医药级视黄醛（Retinal）、视黄醇（Retinol）、视黄醇视黄酸酯（AA酯）、羟基频哪酮视黄酸酯（HPR）、视黄醇丙酸酯等VA类原料及全系列纳米脂质体包裹维生素A产品。 国内首创，拥有8倍视黄醇活性，无刺激。提升体内粘多糖（如透明质酸）含量；眼周使用，明显减少眼周皱纹、细纹；促进角质层更新，使角质层更强韧；保护皮肤免受UV损伤，改善UV引起的肌肤干燥、粗糙、细纹；抑制酪氨酸酶活性。无惧感光，白天可用。 浦瑞生物医药的纳米包裹AA酯荣获2019年度荣格技术创新奖 8倍Retinol 活性；光稳定；不刺激；新型维生素A衍生物。 INCI： RETINYL RETINOATE 、ASCORBIC ACID、PHOSPHOLIPIDS、CAPRYLIC/CAPRIC TRIGLYCERIDE、GLYCERIN、WATER CAS：15498-86-9 视黄醇视黄酸酯是一种新型的维生素A衍生物，活性更高，无惧光感。 维生素A是人体必需维生素，护肤品中应用的研究已有半个多世纪，由于VA衍生物（视黄醇、视黄酸等）对光、氧气、温度，金属离子比较敏感，而且比较容易引发皮肤红肿、痒、紧绷等刺激，护肤品的应用一直比较受限…… 纳米包裹视黄醇视黄酸酯（NanoActive r-Retinoate）使用的VA衍生物是视黄醇视黄酸酯，通过纳米包裹与维生素C复配；视黄醇视黄酸酯是通过视黄醇的羟基和视黄酸的酯化反应得到，同时避免了视黄醇和视黄酸在化妆品应用中的局限； NanoActive r-Retinoate 纳米包裹AA酯包裹粒径在230-300nm，这个粒径的纳米乳一方面可以使活性物稳定的悬浮于纳米载体中，同时可以使活性物有效渗透入肌肤发挥作用，控制活性物是释放速度。 视黄醇视黄酸酯主要特点： 细胞毒性：IC 50 视黄醇 25μM，视黄醇视黄酸酯为40μM（比视黄醇高60%），视黄酸为处方药，禁止用于个人护理（IC 50为一定浓度的某物质诱导细胞凋亡50%的量，用来衡量物质诱导凋亡的能力。越高表明细胞毒性越弱）； 生物活性：视黄醇视黄酸酯保留了环端基和侧链烯基，依然具有视黄醇和视黄酸的生物活性，体内测试表明：促进皮肤再生能力要优于视黄醇和视黄酸； 改善了视黄醇的光学稳定定、化学稳定性，同时减少了视黄醇和视黄酸的刺激性。 功效 促进皮肤表层更新速度，让皮肤表层更紧实有序 促进真皮层加速生产胶原蛋白，抑制MMP对胶原蛋白的破坏 增加表皮层中粘多糖（如透明质酸等）的含量，让皮肤保水能力更强 促进角质层的新陈代谢，使角质层更紧实，屏障功能恢复 视黄醇视黄酸酯促进体内粘多糖（透明质酸）的表达测试：设置0.05%的视黄醇组、0.05% 视黄酸组，对照组三组，用于脱毛处理后的小鼠皮肤 三天后观察小鼠组织切片中的表皮层和真皮层 透明质酸与蛋白（HABP）结合会有染色反应。 适用产品 抗衰老产品：保持真皮中的胶原蛋白，防止胶原蛋白降解速度过快 与透明质酸和生物复合多糖（水解香桃木）复配，一周内可以观察到细纹的改善。 美白产品：协同VC抑制络氨酸酶，促进新陈代谢，加速黑色素的消失 文献显示，与VC搭配对治疗痤疮肌肤同样有效。 防晒产品：抑制紫外线造成的MMP活性的增强，保护弹性纤维蛋白和真皮层胶原蛋白 改善UV照射引起的皱纹，细纹。 修护产品：促进体内透明质酸的合成，减小皮肤TEWL 促进角质细胞活性，增加表皮层厚度，使表皮层更强韧 。 Tagged 纳米包裹AA酯, 维生素A衍生物, 视黄酸, 视黄醇, 视黄醇视黄酸酯. [NanoActive™ r-Retinoate新一代高性能维A活性物] PURIPHARM · MEDI

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상품명

NanoActive™ r-Retinoate(리포좀)

복합물상품명

미확인

공급사

1곳

제조사

PuriPharm

종류

Actives

용도

Antioxidant, Anti-aging/Wrinkle Care

인증·등록

NMPA

구성 성분 (6)

공급사 (1)

규격 및 사용 정보

INCI

Retinyl Retinoate, Ascorbic Acid (Vitamin C), Phospholipids, Caprylic/Capric Triglyceride, Glycerin, Water

CAS 번호

15498-86-9

EC 번호

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원산지

미확인

성상

Yellow-orange viscous liquid

용해성

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pH

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권장 사용량

1.0%–5.0%

보관 조건

미확인

사용 기한

미확인

포장 단위

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기술 문서 (TDS·SDS·COA)

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안전성 자료

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규제 자료

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PH

5.0-8.0

Solubility

Amphiphilic (compatible with both water and oil phases)

Particle size

20–30 nm nano-encapsulation；

기타 INCI 표기

Retinyl retinoate,ascorbic acid,phospholipids,caprylic/capric triglyceride,glycerin,water / RETINYL RETINOATE 、ASCORBIC ACID、PHOSPHOLIPIDS、CAPRYLIC/CAPRIC TRIGLYCERIDE、GLYCERIN、WATER