期刊
PHARMACEUTICS
卷 14, 期 11, 页码 -出版社
MDPI
DOI: 10.3390/pharmaceutics14112412
关键词
retinol; retinoid; cosmetics; photoaging; retinoic acid receptor; hydroxylation
Retinoids, a type of bioactive material, are widely used for dermatological and pathological conditions. However, their effectiveness is limited due to the body's natural regulation and irritation. This study presents methods to enhance the efficacy of retinoids and demonstrates their effectiveness in improving facial wrinkles. These findings not only improve compliance among users but also provide insights into the mechanisms of retinoids.
Retinoids, one of the most robust bioactive materials, have been widely used to improve various dermatological and pathological conditions. The body has an endogenous mechanism that modulates the exogenous retinoid above physiological concentrations, which limits the bioavailability or pharmacological efficacy of retinoids. Considering that most retinoids trigger extensive irritation in users, it is necessary to enhance the pharmacological efficacy of retinoids, thereby achieving a higher efficacy at a lower dosage. Here, we present approaches for enhancing the efficacy of retinol by enhancing retinoid-induced RAR gamma (RAR-gamma) activity and inhibiting the hydroxylation of retinoic acid. Using both in vitro and ex vivo experiments, retinoid boosters were demonstrated to enhance pharmacological efficacy. A small pilot study was conducted to investigate the efficacy for improvement of facial wrinkles, whose results revealed that these boosters could enhance the pharmacological efficacy of topical applications of both retinol and retinoic acid for cosmetic use. These results promote not only a higher compliance among retinoids users, but also provide significant insights into the mechanisms underlying the action of retinoids.
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