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聚乙二醇在药物传递中的应用:优缺点及潜在替代品。

Poly(ethylene glycol) in drug delivery: pros and cons as well as potential alternatives.

机构信息

Lehrstuhl für Organische und Makromolekulare Chemie (IOMC), Friedrich-Schiller-University Jena, Humboldtstrasse 10, 07745 Jena, Germany.

出版信息

Angew Chem Int Ed Engl. 2010 Aug 23;49(36):6288-308. doi: 10.1002/anie.200902672.

DOI:10.1002/anie.200902672
PMID:20648499
Abstract

Poly(ethylene glycol) (PEG) is the most used polymer and also the gold standard for stealth polymers in the emerging field of polymer-based drug delivery. The properties that account for the overwhelming use of PEG in biomedical applications are outlined in this Review. The first approved PEGylated products have already been on the market for 20 years. A vast amount of clinical experience has since been gained with this polymer--not only benefits, but possible side effects and complications have also been found. The areas that might need consideration and more intensive and careful examination can be divided into the following categories: hypersensitivity, unexpected changes in pharmacokinetic behavior, toxic side products, and an antagonism arising from the easy degradation of the polymer under mechanical stress as a result of its ether structure and its non-biodegradability, as well as the resulting possible accumulation in the body. These possible side effects will be discussed in this Review and alternative polymers will be evaluated.

摘要

聚乙二醇(PEG)是最常用的聚合物,也是新兴聚合物药物递送领域中隐形聚合物的金标准。本文概述了在生物医学应用中PEG 被广泛使用的原因。第一批获得批准的聚乙二醇化产品已经上市 20 年了。自那时以来,已经积累了大量的临床经验——不仅有好处,还发现了可能的副作用和并发症。需要考虑并更深入和仔细检查的领域可以分为以下几类:过敏反应、药代动力学行为的意外变化、毒性副产物,以及由于其醚结构和不可生物降解性,聚合物在机械应力下容易降解而产生的拮抗作用,以及由此导致的可能在体内积累。本文将讨论这些可能的副作用,并评估替代聚合物。

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