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小分子干扰RNA和反义寡核苷酸的皮肤/透皮递送——进展与障碍

Dermal/transdermal delivery of small interfering RNA and antisense oligonucleotides- advances and hurdles.

作者信息

Ita Kevin

机构信息

College of Pharmacy, Touro University, Mare Island-Vallejo, CA 94592, USA.

出版信息

Biomed Pharmacother. 2017 Mar;87:311-320. doi: 10.1016/j.biopha.2016.12.118. Epub 2017 Jan 5.

Abstract

A diverse array of nucleic acids has been studied by several researchers for the management of several diseases. Among these compounds, small interfering RNA and antisense oligonucleotides have attracted considerable attention. Antisense oligonucleotides are synthetic single stranded strings of nucleic acids that bind to RNA and thereby alter or reduce expression of the target RNA while siRNAs, on the other hand, are double-stranded RNA molecules which can hybridize with a specific mRNA sequence and block the translation of numerous genes. One of the main obstacles in the dermal or transdermal delivery of these compounds is their low skin permeability. In this review, various techniques used to enhance the delivery of these molecules into or across the skin are described and in some cases, the correlation between enhanced dermal/transdermal delivery and therapeutic efficacy is highlighted.

摘要

几位研究人员对多种核酸进行了研究,以用于多种疾病的治疗。在这些化合物中,小干扰RNA和反义寡核苷酸引起了相当大的关注。反义寡核苷酸是合成的单链核酸,可与RNA结合,从而改变或降低靶RNA的表达,而小干扰RNA则是双链RNA分子,可与特定的mRNA序列杂交并阻断众多基因的翻译。这些化合物经皮给药的主要障碍之一是其皮肤渗透性低。在这篇综述中,描述了用于增强这些分子进入皮肤或透过皮肤递送的各种技术,并且在某些情况下,强调了增强的经皮/透皮递送与治疗效果之间的相关性。

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