Casting New Light on the Retinol and Retinyl Palmitate Functions as Chemical Enhancers for Transdermal/Topical Drug Delivery.

IF 10 2区 医学 Q1 ENGINEERING, BIOMEDICAL
Yun-Hao Ren, Qi Zhou, Yang Xu, Bei-Ning Xu, Peng Shu, Li-Hua Peng
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Abstract

Retinol and retinyl palmitate, with excellent whitening and antioxidant activities, are widely used as essential functional ingredients in transdermal preparations and skincare products. Herein, for the first time, the influence and underlying mechanisms of retinol and retinyl palmitate on the skin penetration of caffeine are investigated. It is found that the penetration of caffeine is very significantly enhanced by retinol and retinyl palmitate with 2.83 and 2.57 folds, respectively. Mechanistic studies showed that they can disrupt the lipids of intercellular orderly arrangement and reduce the content of orthorhombic lattices in the skin, making the skin loose and the barrier function decreased. Furthermore, due to the formation of chemical bonds with the skin keratin, they have a strong affinity with the skin, changing the dense secondary structure of keratin with a reduced skin barrier effect. This study provides new evidence for the potential of retinol and retinyl palmitate as novel skin penetration enhancers with high safety that possess great potential for application in the transdermal delivery of pharmaceutical and cosmetic active substances.

透视视黄醇和视黄醇棕榈酸酯作为透皮/局部给药化学增效剂的功能。
视黄醇和视黄醇棕榈酸酯具有出色的美白和抗氧化活性,被广泛用作透皮制剂和护肤品的重要功能成分。本文首次研究了视黄醇和视黄醇棕榈酸酯对咖啡因皮肤渗透性的影响及其内在机制。研究发现,视黄醇和视黄醇棕榈酸酯可显著增强咖啡因的渗透性,分别为 2.83 倍和 2.57 倍。机理研究表明,它们能破坏细胞间有序排列的脂质,降低皮肤中正交晶格的含量,使皮肤变得松弛,屏障功能下降。此外,由于与皮肤角蛋白形成化学键,它们与皮肤有很强的亲和力,改变了角蛋白致密的二级结构,降低了皮肤屏障作用。这项研究为视黄醇和视黄醇棕榈酸酯作为新型皮肤渗透增强剂提供了新的证据,它们具有很高的安全性,在药物和化妆品活性物质的透皮给药方面具有很大的应用潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
Advanced Healthcare Materials
Advanced Healthcare Materials 工程技术-生物材料
CiteScore
14.40
自引率
3.00%
发文量
600
审稿时长
1.8 months
期刊介绍: Advanced Healthcare Materials, a distinguished member of the esteemed Advanced portfolio, has been dedicated to disseminating cutting-edge research on materials, devices, and technologies for enhancing human well-being for over ten years. As a comprehensive journal, it encompasses a wide range of disciplines such as biomaterials, biointerfaces, nanomedicine and nanotechnology, tissue engineering, and regenerative medicine.
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