Current drug research on PEGylation with small molecular agents

被引：194

作者：

Li, Wenjun ^{[1
]}

Zhan, Peng ^{[1
]}

De Clercq, Erik ^{[2
]}

Lou, Hongxiang ^{[1
]}

Liu, Xinyong ^{[1
]}

机构：

[1] Shandong Univ, Sch Pharmaceut Sci, Dept Med Chem, Key Lab Chem Biol,Minist Educ, Jinan 250012, Shandong, Peoples R China

[2] Katholieke Univ Leuven, Rega Inst Med Res, B-3000 Louvain, Belgium

来源：

PROGRESS IN POLYMER SCIENCE | 2013年 / 38卷 / 3-4期

基金：

中国国家自然科学基金; 高等学校博士学科点专项科研基金;

关键词：

PEGylation; Small molecules drugs; Anti-tumor; Anti-inflammatory; Anti-virus; Antimicrobial; Immunosuppressant; POLY(ETHYLENE GLYCOL) PRODRUG; OPIOID-INDUCED CONSTIPATION; IN-VITRO CYTOTOXICITY; ANTI-HIV ACTIVITY; POLYETHYLENE-GLYCOL; CELLULAR INTERNALIZATION; COVALENT ATTACHMENT; ANTITUMOR-ACTIVITY; PHASE-II; VIVO;

D O I：

10.1016/j.progpolymsci.2012.07.006

中图分类号：

O63 [高分子化学（高聚物）];

学科分类号：

070305 ; 080501 ; 081704 ;

摘要：

PEGylation, covalent attaching polyethylene glycol (PEG) polymers to therapeutic agents, is one of the most promising techniques to improve the therapeutic effect of drugs. Initially, this technology is mainly applied with macromolecular drugs, such as proteins, enzymes, with ten PEGylated biomacromolecules approved by the FDA for the treatment of related diseases. The clinical successful use of PEGylated macromolecular drug has promoted the application of this technology with small molecules drugs to overcome shortcomings associated with therapy, such as possible low solubility, high toxicity, undesirable pharmaceutical characteristics and nonspecific biodistribution profiles. So far, four PEGylated small drugs have been taken into clinical trials. This review mainly focuses on the recent advances of PEGylated small molecules, including their general configuration, and the current merits and limits of PEG modification. Herein PEG delivery systems are distinguished by therapeutic application (anti-tumor, anti-inflammatory, etc.) and their corresponding PEGylated small molecules are described in detail. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：421 / 444

页数：24

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