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聚乙二醇化:一种药物递送方法。综述。

PEGylation: an approach for drug delivery. A review.

作者信息

Jain Aviral, Jain Sanjay K

机构信息

Pharmaceutics Research Projects Laboratory, Department of Pharmaceutical Sciences, Dr. Hari Singh Gour Vishwavidyalaya, Sagar (M. P.) 470003, India.

出版信息

Crit Rev Ther Drug Carrier Syst. 2008;25(5):403-47. doi: 10.1615/critrevtherdrugcarriersyst.v25.i5.10.

Abstract

The current review presents an update on polyethylene glycol (PEG), which is widely used as a covalent modifier of macromolecules. This review discusses the polymers suitable for conjugation, their conjugation methods, and their properties. Proteins and bioactive substances can be chemically modified by binding synthetic macromolecules of PEG to the surface of these biomolecules. Protein and peptide PEGylation improves the biopharmaceutical properties of drugs-that is, increased stability, increased resistance to proteolytic inactivation, decreased to nonexistent immunogenicity, increased circulatory lives, and low toxicity. These altered properties improve the delivery and efficacy of proteins.

摘要

本综述介绍了聚乙二醇(PEG)的最新情况,PEG被广泛用作大分子的共价修饰剂。本文讨论了适用于共轭的聚合物、它们的共轭方法及其性质。蛋白质和生物活性物质可以通过将PEG合成大分子结合到这些生物分子表面进行化学修饰。蛋白质和肽的聚乙二醇化改善了药物的生物制药性质,即提高了稳定性、增强了对蛋白水解失活的抵抗力、降低至不存在免疫原性、延长了循环寿命以及降低了毒性。这些改变的性质提高了蛋白质的递送效率和疗效。

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