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α-山竹黄酮前体脂质体的体外渗透及皮肤滞留情况

In Vitro Permeation and Skin Retention of α-Mangostin Proniosome.

作者信息

Chin Gan Siaw, Todo Hiroaki, Kadhum Wesam Radhi, Hamid Mariani Abdul, Sugibayashi Kenji

机构信息

Institute of Bioproduct Development, Universiti Teknologi Malaysia.

出版信息

Chem Pharm Bull (Tokyo). 2016;64(12):1666-1673. doi: 10.1248/cpb.c16-00425.

Abstract

The current investigation evaluated the potential of proniosome as a carrier to enhance skin permeation and skin retention of a highly lipophilic compound, α-mangostin. α-Mangostin proniosomes were prepared using the coacervation phase seperation method. Upon hydration, α-mangostin loaded niosomes were characterized for size, polydispersity index (PDI), entrapment efficiency (EE) and ζ-potential. The in vitro permeation experiments with dermis-split Yucatan Micropig (YMP) skin revealed that proniosomes composed of Spans, soya lecithin and cholesterol were able to enhance the skin permeation of α-mangostin with a factor range from 1.8- to 8.0-fold as compared to the control suspension. Furthermore, incorporation of soya lecithin in the proniosomal formulation significantly enhanced the viable epidermis/dermis (VED) concentration of α-mangostin. All the proniosomal formulations (except for S20L) had significantly (p<0.05) enhanced deposition of α-mangostin in the VED layer with a factor range from 2.5- to 2.9-fold as compared to the control suspension. Since addition of Spans and soya lecithin in water improved the solubility of α-mangostin, this would be related to the enhancement of skin permeation and skin concentration of α-mangostin. The choice of non-ionic surfactant in proniosomes is an important factor governing the skin permeation and skin retention of α-mangostin. These results suggested that proniosomes can be utilized as a carrier for highly lipophilic compound like α-mangostin for topical application.

摘要

本研究评估了前体脂质体作为载体增强高亲脂性化合物α-山竹黄酮皮肤渗透和皮肤滞留的潜力。采用凝聚相分离法制备了α-山竹黄酮前体脂质体。水化后,对负载α-山竹黄酮的脂质体进行了粒径、多分散指数(PDI)、包封率(EE)和ζ电位的表征。用分离真皮的尤卡坦微型猪(YMP)皮肤进行的体外渗透实验表明,由司盘、大豆卵磷脂和胆固醇组成的前体脂质体能够增强α-山竹黄酮的皮肤渗透,与对照悬浮液相比,增强因子范围为1.8至8.0倍。此外,在脂质体配方中加入大豆卵磷脂可显著提高α-山竹黄酮在活表皮/真皮(VED)中的浓度。与对照悬浮液相比,所有脂质体配方(S20L除外)在VED层中α-山竹黄酮的沉积均显著增强(p<0.05),增强因子范围为2.5至2.9倍。由于在水中加入司盘和大豆卵磷脂可提高α-山竹黄酮的溶解度,这可能与α-山竹黄酮皮肤渗透和皮肤浓度的提高有关。脂质体中非离子表面活性剂的选择是影响α-山竹黄酮皮肤渗透和皮肤滞留的重要因素。这些结果表明,前体脂质体可作为α-山竹黄酮等高度亲脂性化合物的外用载体。

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