Background Aging is responsible for the majority of skin and soft tissue remolding in humans. Retinol and its derivatives or retinoids effectively intervene skin aging process. Nevertheless, retinoids usually induce skin intolerance, especially among the Chinese, and thus, their application to prevent skin aging is yet to be well accepted. The study of optimal composition and concentration of retinoids is necessary to offer strong antiaging efficacies with minimum irritations. Therefore, a better understanding of retinol and its derivatives is acutely needed to develop strategies to combat skin aging. Objective In this study, we aimed to determine the optimal ratio of two retinol derivatives—hydroxypinacolone retinoate (HPR) and retinyl propionate (RP) in terms of dermal remodeling and skin aging prevention—and to investigate their synergistic antiaging effects both in vitro and in vivo. Methods An in vitro human foreskin fibroblast (HFF‐1) cell model was established to evaluate the cell viability of HPR and/or RP treatment. In addition, the antiaging and retinol receptor genes expressions in HFF‐1 cells cotreated with HPR and RP were quantified. The in vivo adverse reaction evaluation of skincare serums containing various levels of retinol or the optimal HPR and RP combination termed Gravi‐A was performed by 24 h patch tests in 33 subjects prior to the clinical research. Last but not the least, clinical research with 42 Chinese urban women was conducted to assess the in vivo antiaging efficacy of the skincare serum containing this optimal retinoid combination. Results The combination of HPR and RP at the weight ratio of 5:9 was shown to achieve the optimal in vitro antiaging performance. Coadministration of 5 μg/mL HPR and 9 μg/mL RP to HFF‐1 cells promoted their proliferation at 24 h and synergistically enhanced the expressions of type IV collagen, CRBP‐I, and RARB genes. In addition, the skincare serum containing HPR and RP combination at 5:9 weight ratio demonstrated superior in vivo anti‐wrinkle and skin elasticity improvement benefits without any adverse reactions, while retinol in the same concentration exerted much higher adverse effect. Skin wrinkles, skin smoothness, TEWL, skin elasticity R2 and R5 were improved by 8.3%, 11.9%, 25.7%, 14.5%, and 22.6%, respectively, after 8‐week use. Conclusion Our results indicated the advanced antiaging effect of HPR and RP combination both in vitro and in vivo. In addition, little adverse effect was observed in this study, in comparison with retinol. This combination named as Gravi‐A is a potential therapeutic strategy to prevent skin aging, especially for Chinese women.
Gravi-A nanoparticles, composed of retinyl propionate (RP) and hydroxypinacolone retinoate (HPR), were prepared by encapsulating the two using the high-pressure homogenization technique. The nanoparticles are effective in anti-wrinkle treatment with high stability and low irritation. We evaluated the effect of different process parameters on nanoparticle preparation. Supramolecular technology effectively produced nanoparticles with spherical shapes with an average size of 101.1 nm. The encapsulation efficiency was in the 97.98–98.35% range. The system showed a sustained release profile for reducing the irritation caused by Gravi-A nanoparticles. Furthermore, applying lipid nanoparticle encapsulation technology improved the transdermal efficiency of the nanoparticles, thereby allowing these to penetrate deep into the dermis layer to achieve precise and sustained release of active ingredients. Gravi-A nanoparticles can be extensively and conveniently used in cosmetics and other related formulations by direct application.
Delaying aging is an eternal goal for humanity. Acetyl hexapeptide‐8 (AHP‐8) is an effective skin anti‐aging drug that locally interrupts the signal transmission of muscle contractions and promotes collagen production, thus smoothening wrinkles. However, its high molecular weight and strong hydrophilicity limit its skin permeation capacity. To solve this problem, an ionic liquid with excellent bioactivity, MAC, is synthesized from l‐malic acid and l‐carnitine and used as a permeation enhancer to improve the anti‐aging effects of AHP‐8. The ratio of MAC's components is optimized based on density functional theory calculations and cytotoxicity experiments. Low concentrations of MAC significantly increase AHP‐8 transdermal delivery, reaching a maximum at 5‐10 wt% MAC. The pro‐permeation mechanism of MAC is investigated using molecular dynamics simulations, and the penetration enhancement and anti‐aging performance of AHP‐8 are demonstrated by conducting cellular, animal, and clinical experiments. The results show that MAC/AHP‐8 outperforms AHP‐8 in terms of collagen and hyaluronic acid synthesis, anti‐inflammation, anti‐oxidation, and inhibition of muscle contraction, thus significantly reducing the number and area of wrinkles and increasing skin moisture and elasticity. This study presents MAC as a simple and efficient transdermal vehicle for the clinical application of AHP‐8.
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