喜树碱类抗肿瘤药物的递送系统研究  

Research on delivery systems of camptothecin-based antitumour drugs

作　　者：赵婷婷 蔡泽东 杜琳琳 宦梦蕾 张邦乐 ZHAO Ting-ting;CAI Zei-dong;DU Lin-lin;HUAN Meng-lei;ZHANG Bang-le(The college of Life Sciences,Northwest University,Xi'an 710069,China;Department of Pharmaceutics and Pharmacy Administration,Air Force Military Medical University,Xi'an 710032,China)

机构地区：[1]西北大学生命科学学院,西安710069 [2]空军军医大学药剂学与药事管理学教研室,西安710032

出　　处：《中国新药杂志》2023年第3期246-254,共9页Chinese Journal of New Drugs

基　　金：国家“重大新药创制”科技重大专项资助项目(2018ZX09J18108-004)。

摘　　要：喜树碱是一种由珙桐科植物喜树中分离得到的喹啉类生物碱,是一种天然的拓扑异构酶I抑制剂,通过与拓扑异构酶I-DNA形成复合物,进而阻止DNA复制及RNA合成产生抗肿瘤作用。临床研究显示,喜树碱及其衍生物具有良好的抗肿瘤活性,但因具有较高的毒副作用和较低的生物利用度而限制了其临床应用。新型药物递送系统可以弥补药物本身的缺陷,通过增强药物在体内的稳定性,提高药物的生物利用度和靶向性来达到增效减毒的目的,一定程度上解决了喜树碱类药物存在的问题。本文通过查阅近年来喜树碱类药物递送系统的国内外相关研究文献,对喜树碱类抗肿瘤药物递送系统的研究进展进行分析和总结,以期为研发满足临床实际应用的喜树碱类抗肿瘤药物提供理论指导,为该药物的新制剂研究提供一定的参考与借鉴。Camptothecin is a kind of quinoline alkaloid and is also a natural topoisomerase I inhibitor isolated from Camptotheca involucrata. After complexing with topoisomerase I-DNA, camptothecin prevents DNA replication and RNA synthesis, indicating an anti-tumor effect. Clinical studies have shown that camptothecin and its derivatives have good antitumor activity. However, the high toxicity and low bioavailability limited its clinical application. Novel drug delivery systems can make up the defects through enhancing the drug stability, bioavailability and targeting ability to improve the anti-tumor effect, which can help reduce the toxicity, and solve the problems of camptothecins to a certain extent. This paper analyzes and summarizes the research progress of camptothecin-based antitumor drug delivery systems in recent published literatures, in order to provide theoretical guidance and suggestion for the development of new preparations of camptothecins that meet the needs of clinical applications.

关 键 词：喜树碱 抗肿瘤药物 药物递送系统 纳米载体 

分 类 号：R979.1[医药卫生—药品] R945[医药卫生—药学]