喜树碱及其衍生物的聚乙二醇化学修饰药物研究进展

目的：喜树碱及其衍生物药物是一类重要的抗肿瘤药物，但其存在水溶性差、生物利用度低、毒副作用大等问题，喜树碱及其衍生物的聚乙二醇化学修饰具有十分诱人的前景，但目前国内研究较少，本文综述近年来喜树碱及其衍生物药物的聚乙二醇化学修饰研究进展。方法：以喜树碱（Camptothecin, CPT）、伊立替康（Irinotecan, CPT-11）、7-乙基-10-羟基喜树碱（7-ethyl-10-hydroxycamptothecin, SN38）、聚乙二醇（Polyethylene glycol, PEG）、聚乙二醇化喜树碱（PEG-CPT）等为关键词，查阅近几年国内外相关研究文献。结果与结论：综述了喜树碱及其衍生物的聚乙二醇化学修饰药物的研究进展与临床研究报道，为发掘结构明确、组成稳定的新型化学修饰药物提供理论基础和技术支撑。

Research progress on polyethylene glycol chemical modification drugs of camptothecin and its derivatives

Objective: As important antitumor drugs, camptothecin and its derivatives are limited in further application due to several problems such as poor water solubility, low bioavailability, and high toxic side effects. Based on these drawbacks, chemical modification using polyethylene glycol (PEG) has become an effective way to show great promise and significance, and there are few related studies in domestic. This paper reviews the recent research progress on the chemical modification of camptothecin and its derivatives by PEG in recent years. Methods: Based on the keywords of Camptothecin (CPT), Irinotecan (CPT-11), 7-ethyl-10-hydroxycamptothecin (SN38), Polyethylene glycol (PEG), and PEG-CPT, we reviewed the relevant research literature in recent years at home and abroad. RESULTS & CONCLUSION: This paper reviews the research progress and clinical study reports on PEG modification of camptothecin and its derivatives, providing theoretical basis and technical support for the discovery of novel chemically modified drugs with clear structures and stable compositions.