摘要
聚乙二醇(polyethylene glycol,PEG)目前被广泛应用于肿瘤药物的修饰,当与药物分子偶联时,可以将其优良性质赋予修饰后的药物分子,改变药物的溶解性,在其修饰的药物周围产生空间屏障,减少药物的酶解,避免药物在肾脏的代谢中很快被消除,同时能被动靶向肿瘤细胞,降低药物毒性。聚乙二醇是中性、无毒且具有独特理化性质和良好生物相容性的高分子聚合物,也是经美国食品药物管理局(FDA)批准的极少数能作为体内注射给药的合成聚合物之一,已得到市场的认可。该文综述了近几年聚乙二醇修饰的前药研究进展,且就聚乙二醇修饰的原理、设计、运用及面临的挑战进行了论述。
Polyethylene glycol （PEG） has been widely used in the modification of cancer drugs, when PEG coupling with the drug molecule, its excellent properties can be given to the drug molecules ＇after modification for changing the drug solubility, producing the space barriers around its modified drugs, reducing the enzymatic hydrolysis of drugs, avoiding the rapid elimination in the kidney metabolism, at the same time can passively targeting to tumor cells and reducing the drug toxicity. PEG is a neutral, non-toxic, high- molecular polymer with unique physical and chemical properties and good biocompatibility, one of very small number of in vivo injection of synthetic polymers approved by USFDA and has been recognized by the market. This article reviews the research progress of PEG modified prodrugs in recent years and discusses the principle, design, application and facing challenges of PEG modification.
出处
《中国药业》
CAS
2014年第15期1-4,共4页
China Pharmaceuticals
关键词
聚乙二醇
前药
被动靶向
修饰
polyethylene glycol
prodrug
passive targeted
modification
