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纳米载体:一种提高吸收差或预体内代谢药物口服生物利用度的通用策略。

Nanocarriers: a general strategy for enhancement of oral bioavailability of poorly absorbed or pre-systemically metabolized drugs.

机构信息

Department of Pharmaceutics, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, China.

出版信息

Curr Drug Metab. 2010 Feb;11(2):197-207. doi: 10.2174/138920010791110836.

Abstract

Oral delivery remains the preferred route for chronic drug administration thanks to its patient convenience and compliance. However, many drug candidates are unsuitable for conventional oral formulations due to low solubility, poor membrane permeability, or extensive pre-systemic metabolism. This review describes a promising strategy that incorporates or encapsulates the molecules with biodegradable and biocompatible nanoparticulate carriers. The entrapped drug substances can be protected against degradation by gastrointestinal fluids, while drug absorption through the gastrointestinal epithelium or lymphatic transport can be enhanced. Possible mechanisms for transport of these nanocarriers across gastrointestinal mucosa are introduced that focus on effects of size and surface properties of the nanocarriers on the non-specific or targeted uptake by enterocytes and/or M cells. Applications of various oral nanocarrier formulations, such as lipid nanoparticles, nanoemulsions and chitosan nanoparticles, are reviewed. Nanoparticulate drug carriers show great potential for improving the bioavailability of orally administered drugs.

摘要

口服给药因其患者便利性和顺应性仍然是慢性药物给药的首选途径。然而,由于溶解度低、膜通透性差或广泛的前体药物代谢,许多候选药物不适合传统的口服制剂。本综述描述了一种有前途的策略,即将分子与可生物降解和生物相容的纳米颗粒载体结合或包封。包封的药物可以防止被胃肠道液降解,同时可以增强药物通过胃肠道上皮或淋巴转运的吸收。介绍了这些纳米载体跨胃肠道黏膜转运的可能机制,重点是纳米载体的大小和表面特性对肠细胞和/或 M 细胞非特异性或靶向摄取的影响。综述了各种口服纳米载体制剂,如脂质纳米粒、纳米乳剂和壳聚糖纳米粒的应用。纳米颗粒药物载体在提高口服药物的生物利用度方面具有很大的潜力。

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