Yutani Reiko, Morita Shin-ya, Teraoka Reiko, Kitagawa Shuji
Kobe Pharmaceutical University, 4-19-1 Motoyamakita-machi, Kobe 658-8558, Japan.
Chem Pharm Bull (Tokyo). 2012;60(8):989-94. doi: 10.1248/cpb.c12-00230.
As for most other polyphenols, intradermal delivery of curcumin and resveratrol is limited; however, it was significantly improved by a microemulsion using Aerosol OT (Aerosol OT microemulsion) and Tween 80 (Tween 80 microemulsion) as surfactants. Aerosol OT microemulsion was more effective and the incorporation ratio of these polyphenols into skin by Aerosol OT microemulsion was five-fold or ten-fold that by Tween 80 microemulsion. To clarify the mechanism of the enhancement we examined the distribution of these polyphenols and the surfactant component, Aerosol OT, using excised guinea pig skin and Yucatan micropig (YMP) skin. During permeation, polyphenols distributed deep in the skin. In particular, a small molecule, resveratrol, was mainly present in the dermis in YMP skin. Aerosol OT also distributed deep in the skin. These findings suggest the possible involvement of the interaction of surfactant molecules with skin components in the enhanced delivery process of polyphenols. The distribution ratio between the dermis and epidermis of the polyphenols, including quercetin, in the presence of Aerosol OT microemulsion decreased with the increase of molecular weight in YMP skin, suggesting the possibility that distribution to the dermis is regulated by the molecular size.
与大多数其他多酚类物质一样，姜黄素和白藜芦醇的皮内递送受到限制；然而，以气溶胶OT（气溶胶OT微乳液）和吐温80（吐温80微乳液）作为表面活性剂的微乳液显著改善了这种情况。气溶胶OT微乳液更有效，这些多酚类物质通过气溶胶OT微乳液进入皮肤的掺入率是吐温80微乳液的五倍或十倍。为了阐明增强作用的机制，我们使用切除的豚鼠皮肤和尤卡坦小型猪（YMP）皮肤研究了这些多酚类物质和表面活性剂成分气溶胶OT的分布情况。在渗透过程中，多酚类物质分布在皮肤深层。特别是，小分子白藜芦醇主要存在于YMP皮肤的真皮中。气溶胶OT也分布在皮肤深层。这些发现表明，在多酚类物质的增强递送过程中，表面活性剂分子与皮肤成分之间的相互作用可能起到了作用。在气溶胶OT微乳液存在的情况下，包括槲皮素在内的多酚类物质在YMP皮肤的真皮和表皮之间的分布比例随着分子量的增加而降低，这表明分布到真皮可能受分子大小的调节。
