维生素E TPGS在给药中的应用

IF 4.3 3区医学 Q1 PHARMACOLOGY & PHARMACY

European Journal of Pharmaceutical Sciences Pub Date : 2013-05-13 DOI:10.1016/j.ejps.2013.02.006

Yuanyuan Guo , Jun Luo , Songwei Tan , Ben Oketch Otieno , Zhiping Zhang

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引用次数: 436

摘要

d-α-生育酚聚乙二醇1000琥珀酸酯(简称TPGS或维生素E TPGS)是由维生素E琥珀酸酯与聚乙二醇1000酯化而成。作为一种新型的非离子表面活性剂，它具有两亲性，在低至0.02 wt%的水溶液中可以形成稳定的胶束。它具有乳化、分散、胶凝和增溶难水溶性药物的作用，已被广泛研究。它还可以作为p -糖蛋白(P-gp)抑制剂，并已被用作克服多药耐药(MDR)和提高许多抗癌药物的口服生物利用度的辅料。由于TPGS已被FDA批准为一种安全的药物佐剂，许多基于TPGS的给药系统(DDS)被开发出来。本文综述了TPGS作为P-gp抑制剂、增溶剂/吸收剂和药物传递渗透增强剂的性能，以及TPGS在纳米晶体、纳米悬浮液、片剂/固体分散体、疫苗系统佐剂、营养补充剂、薄膜增塑剂、抗癌试剂等方面的应用。这一综述将对TPGS在DDS中的应用产生重大影响和带来新的见解。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

The applications of Vitamin E TPGS in drug delivery

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The applications of Vitamin E TPGS in drug delivery

d-α-Tocopheryl polyethylene glycol 1000 succinate (simply TPGS or Vitamin E TPGS) is formed by the esterification of Vitamin E succinate with polyethylene glycol 1000. As novel nonionic surfactant, it exhibits amphipathic properties and can form stable micelles in aqueous vehicles at concentration as low as 0.02 wt%. It has been widely investigated for its emulsifying, dispersing, gelling, and solubilizing effects on poorly water-soluble drugs. It can also act as a P-glycoprotein (P-gp) inhibitor and has been served as an excipient for overcoming multidrug resistance (MDR) and for increasing the oral bioavailability of many anticancer drugs. Since TPGS has been approved by FDA as a safe pharmaceutic adjuvant, many TPGS-based drug delivery systems (DDS) have been developed. In this review, we discuss TPGS properties as a P-gp inhibitor, solubilizer/absorption and permeation enhancer in drug delivery and TPGS-related formulations such as nanocrystals, nanosuspensions, tablets/solid dispersions, adjuvant in vaccine systems, nutrition supplement, plasticizer of film, anticancer reagent and so on. This review will greatly impact and bring out new insights in the use of TPGS in DDS.

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来源期刊

European Journal of Pharmaceutical Sciences 医学-药学

CiteScore

9.60

自引率

2.20%

发文量

248

审稿时长

50 days

期刊介绍： The journal publishes research articles, review articles and scientific commentaries on all aspects of the pharmaceutical sciences with emphasis on conceptual novelty and scientific quality. The Editors welcome articles in this multidisciplinary field, with a focus on topics relevant for drug discovery and development. More specifically, the Journal publishes reports on medicinal chemistry, pharmacology, drug absorption and metabolism, pharmacokinetics and pharmacodynamics, pharmaceutical and biomedical analysis, drug delivery (including gene delivery), drug targeting, pharmaceutical technology, pharmaceutical biotechnology and clinical drug evaluation. The journal will typically not give priority to manuscripts focusing primarily on organic synthesis, natural products, adaptation of analytical approaches, or discussions pertaining to drug policy making. Scientific commentaries and review articles are generally by invitation only or by consent of the Editors. Proceedings of scientific meetings may be published as special issues or supplements to the Journal.