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自乳化药物传递系统(SEDDS):制剂开发、特性描述和应用。

Self-emulsifying drug delivery systems (SEDDS): formulation development, characterization, and applications.

机构信息

University Institute of Pharmaceutical Sciences (UGC Centre of Advanced Studies), Panjab University, Chandigarh 160 014, India.

出版信息

Crit Rev Ther Drug Carrier Syst. 2009;26(5):427-521. doi: 10.1615/critrevtherdrugcarriersyst.v26.i5.10.

DOI:10.1615/critrevtherdrugcarriersyst.v26.i5.10
PMID:20136631
Abstract

Self-emulsifying drug delivery systems (SEDDS) possess unparalleled potential in improving oral bioavailability of poorly water-soluble drugs. Following their oral administration, these systems rapidly disperse in gastrointestinal fluids, yielding micro- or nanoemulsions containing the solubilized drug. Owing to its miniscule globule size, the micro/nanoemulsifed drug can easily be absorbed through lymphatic pathways, bypassing the hepatic first-pass effect. We present an exhaustive and updated account of numerous literature reports and patents on diverse types of self-emulsifying drug formulations, with emphasis on their formulation, characterization, and systematic optimization strategies. Recent advancements in various methodologies employed to characterize their globule size and shape, ability to encapsulate the drug, gastrointestinal and thermodynamic stability, rheological characteristics, and so forth, are discussed comprehensively to guide the formula-tor in preparing an effective and robust SEDDS formulation. Also, this exhaustive review offers an explicit discussion on vital applications of the SEDDS in bioavailability enhancement of various drugs, outlining an overview on myriad in vitro, in situ, and ex vivo techniques to assess the absorption and/ or permeation potential of drugs incorporated in the SEDDS in animal and cell line models, and the subsequent absorption pathways followed by them. In short, the current article furnishes an updated compilation of wide-ranging information on all the requisite vistas of the self-emulsifying formulations, thus paving the way for accelerated progress into the SEDDS application in pharmaceutical research.

摘要

自乳化药物传递系统(SEDDS)在提高难溶性药物的口服生物利用度方面具有无与伦比的潜力。这些系统经口服给药后,会在胃肠道液中迅速分散,生成含有溶解药物的微乳液或纳米乳液。由于其微小的球粒尺寸,微/纳米乳化药物可以通过淋巴途径轻易被吸收,绕过肝脏首过效应。我们全面而更新地介绍了许多关于各种自乳化药物制剂的文献报告和专利,重点介绍了它们的制剂、特性和系统优化策略。还全面讨论了最近在各种用于表征其球粒大小和形状、包裹药物能力、胃肠道和热力学稳定性、流变特性等方面的方法学方面的进展,以指导制剂师制备有效的和强大的SEDDS 制剂。此外,本综述还明确讨论了 SEDDS 在提高各种药物生物利用度方面的重要应用,概述了无数用于评估在动物和细胞系模型中加入 SEDDS 的药物的吸收和/或渗透潜力的体外、原位和离体技术,并讨论了它们随后的吸收途径。简而言之,本文提供了对自乳化制剂所有必要方面的广泛信息的最新汇编,为加速 SEDDS 在药物研究中的应用铺平了道路。

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