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聚合物胶束是一种很有前景的药物递送系统,可提高难溶性药物的生物利用度。

Polymeric micelles, a promising drug delivery system to enhance bioavailability of poorly water-soluble drugs.

作者信息

Xu Wei, Ling Peixue, Zhang Tianmin

机构信息

School of Pharmaceutical Science, Shandong University, Jinan 250012, China ; Department of Pharmacy, Shandong Provincial Qian Foshan Hospital, Jinan 250014, China.

出版信息

J Drug Deliv. 2013;2013:340315. doi: 10.1155/2013/340315. Epub 2013 Jun 27.

Abstract

Oral administration is the most commonly used and readily accepted form of drug delivery; however, it is find that many drugs are difficult to attain enough bioavailability when administered via this route. Polymeric micelles (PMs) can overcome some limitations of the oral delivery acting as carriers able to enhance drug absorption, by providing (1) protection of the loaded drug from the harsh environment of the GI tract, (2) release of the drug in a controlled manner at target sites, (3) prolongation of the residence time in the gut by mucoadhesion, and (4) inhibition of efflux pumps to improve the drug accumulation. To explain the mechanisms for enhancement of oral bioavailability, we discussed the special stability of PMs, the controlled release properties of pH-sensitive PMs, the prolongation of residence time with mucoadhesive PMs, and the P-gp inhibitors commonly used in PMs, respectively. The primary purpose of this paper is to illustrate the potential of PMs for delivery of poorly water-soluble drugs with bioavailability being well maintained.

摘要

口服给药是最常用且最易被接受的药物递送形式;然而,人们发现许多药物经此途径给药时难以获得足够的生物利用度。聚合物胶束(PMs)作为能够增强药物吸收的载体,可以克服口服给药的一些局限性,具体方式包括:(1)保护所载药物免受胃肠道恶劣环境的影响;(2)在靶部位以可控方式释放药物;(3)通过粘膜粘附延长在肠道中的停留时间;(4)抑制外排泵以提高药物蓄积。为了解释提高口服生物利用度的机制,我们分别讨论了PMs的特殊稳定性、pH敏感型PMs的控释特性、粘膜粘附型PMs延长停留时间的作用以及PMs中常用的P-糖蛋白抑制剂。本文的主要目的是说明PMs在递送难溶性药物并良好维持生物利用度方面的潜力。

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