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聚乙二醇化是指用一个或多个聚乙烯乙二醇链连接起来针对蛋白质、多肽或非肽分子的一种修饰方法。这种聚合物是无毒,无免疫原性,无抗原性,高度溶于水,已得到美国食品药品管理局﹙FDA﹚的批准。聚乙二醇偶联药物有几个优点:在体内长期滞留性;更不易被代谢酶降解;减少或消除蛋白质免疫原性。由于这些性质,聚乙二醇提高了多肽和蛋白质作为治疗药物的潜力,从而在药物输送系统中发挥重要作用。综述了聚乙二醇修饰的原理与方法,聚乙二醇化在使用中的限制及应用。
Pegylation refers to a modification of a protein, polypeptide or non-peptidic molecule linked by one or more polyethylene glycol chains. This polymer is non-toxic, non-immunogenic, antigen-free and highly soluble in water and has been approved by the U.S. Food and Drug Administration (FDA). Polyethylene glycol coupled drugs have several advantages: long-term retention in the body; more difficult to be degraded by metabolic enzymes; reduce or eliminate protein immunogenicity. Due to these properties, polyethylene glycol enhances the potential of polypeptides and proteins as therapeutic drugs and thus plays an important role in drug delivery systems. The principles and methods of modification of polyethylene glycol are reviewed. The limitations and applications of PEGylation in the application are summarized.