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经皮给药的脂质体制剂-过去三十年来技术的发展。

Transdermal delivery from liposomal formulations - Evolution of the technology over the last three decades.

机构信息

Fraunhofer Institute for Molecular Biology and Applied Ecology, Project group for Translational Medicine & Pharmacology, 60596 Frankfurt/Main, Germany.

Institute for Pharmaceutical Technology, Goethe University, 60438 Frankfurt/Main, Germany.

出版信息

J Control Release. 2016 Nov 28;242:126-140. doi: 10.1016/j.jconrel.2016.09.008. Epub 2016 Sep 10.

DOI:10.1016/j.jconrel.2016.09.008
PMID:27620074
Abstract

Strong barrier properties of stratum corneum often limits the efficiency of drug delivery through skin. Several strategies were tried to improve permeation of drug through skin for local as well as systemic drug delivery. Incorporation of the drug within flexible liposomal vesicles has been one of the popular and well-studied approaches for delivering drug to deeper layers of the skin or even systemic circulation. Flexible/deformable/elastic liposomal systems such as invasomes, Transfersomes, ethosomes, niosomes, etc. have demonstrated encouraging results in delivering small molecules and large proteins to the skin. It is necessary to recognize the promising concepts and analyze their potential, since a clear understanding of the drawbacks and advantages of these approaches will lead towards future development. In the current review we have attempted to give an overview of different liposomal drug carriers for transdermal drug delivery and their efficiency as drug delivery system through different in vivo and in vitro studies. Also, an overview of the studies which investigated the interactions between skin and vesicles, which have lead us to our current understanding of the skin penetration mechanisms of liposomal formulations is presented.

摘要

角质层的强屏障特性常常限制药物通过皮肤的传递效率。为了实现局部和全身药物传递,人们尝试了多种策略来提高药物透过皮肤的渗透能力。将药物包裹在柔性脂质体囊泡中是将药物递送至皮肤深层甚至全身循环的一种常用且经过充分研究的方法。柔性/可变形/弹性脂质体系统(如侵入体、转胞体、醇质体、非离子体等)已在将小分子和大蛋白递送至皮肤方面取得了令人鼓舞的结果。有必要认识到有前途的概念并分析它们的潜力,因为对这些方法的优缺点有清晰的认识将有助于未来的发展。在当前的综述中,我们试图概述不同的用于透皮药物传递的脂质体药物载体及其作为药物传递系统的效率,通过不同的体内和体外研究。此外,还概述了研究皮肤与囊泡相互作用的研究,这些研究使我们对脂质体制剂的皮肤渗透机制有了当前的认识。

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