Auraptene (Aur) is a naturally occurring monoterpene coumarin ether that exhibits numerous therapeutic properties. Its high lipophilicity and low skin penetration, however, limit its potential application for local and transdermal delivery. Biocompatible non-ionic sugar esters (SEs) possess beneficial properties for the development of transdermal formulations in delivering pharmaceutically challenging molecules such as graphene and Aur. In the present study, we conducted a series of experiments to demonstrate the effect of several previously unstudied SEs on the skin permeation and distribution of Aur by preparing gel- and dispersion-type formulations. Skin permeation and deposition experiments were conducted using a Franz diffusion cell with rat skin as the membrane. The dispersion-type formulations prepared using SEs had higher entrapment efficiency, as well as better skin permeation and retention profiles. The dispersion-type formulation containing sucrose palmitate (sSP) exhibited the highest skin permeation over 8 h. Notably, the enhancement effects on Aur concentration in full-thickness skin after the application of the dispersion-type formulation was higher than those of the control formulation. These results indicated that the prepared formulation has potential for use in the transdermal delivery of Aur in pharmaceutical and cosmetic products.

Aurapten (Aur) 是一种天然存在的单萜香豆素醚，具有多种治疗特性。然而，其高亲脂性和低皮肤渗透性限制了其局部和透皮递送的潜在应用。生物相容性非离子糖酯 (SE) 具有有益于开发透皮制剂的特性，可传递具有药学挑战性的分子，例如石墨烯和 Aur。在本研究中，我们进行了一系列实验，通过制备凝胶和分散型制剂来证明几种以前未研究过的 SE 对 Aur 的皮肤渗透和分布的影响。采用以大鼠皮肤为膜的Franz扩散池进行皮肤渗透和沉积实验。使用 SE 制备的分散型制剂具有更高的包封效率以及更好的皮肤渗透和保留特性。含有蔗糖棕榈酸酯（sSP）的分散型制剂在8小时内表现出最高的皮肤渗透性。值得注意的是，应用分散型制剂后对全层皮肤Aur浓度的增强效果高于对照制剂。这些结果表明所制备的制剂具有用于药物和化妆品中 Aur 透皮递送的潜力。