聚合物胶束,一个有前途的药物传递系统,以提高生物利用度的低水溶性药物。

Journal of drug delivery Pub Date : 2013-01-01 Epub Date: 2013-06-27 DOI:10.1155/2013/340315
Wei Xu, Peixue Ling, Tianmin Zhang
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引用次数: 407

摘要

口服给药是最常用和最容易接受的给药方式;然而,人们发现许多药物在通过这种途径给药时难以获得足够的生物利用度。聚合物胶束(PMs)可以通过提供(1)保护负载药物免受胃肠道恶劣环境的影响,(2)在靶点以受控的方式释放药物,(3)通过黏附延长药物在肠道中的停留时间,(4)抑制外排泵以改善药物积累,从而克服口服给药作为载体的一些局限性。为了解释提高口服生物利用度的机制,我们分别讨论了pm的特殊稳定性,ph敏感pm的控释特性,与黏附pm的停留时间延长以及pm常用的P-gp抑制剂。本文的主要目的是说明pm在生物利用度保持良好的情况下递送难水溶性药物的潜力。
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Polymeric micelles, a promising drug delivery system to enhance bioavailability of poorly water-soluble drugs.

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.

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Journal of drug delivery
Journal of drug delivery PHARMACOLOGY & PHARMACY-
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