摘要
7-乙基-10-羟基喜树碱(SN38)是伊立替康的活性代谢物,在体外的抗肿瘤效果是伊立替康的100~1 000倍。然而,SN38水溶性差、在pH>9.0时完全水解开环为不具有治疗效果的羧酸盐形式。SN38新型给药系统均可提高药物在各种不同癌症模型中的理化性质和体内性能,从而提高其抗肿瘤活性和减少不良反应。因此从物理封装、化学偶联和主动肿瘤靶向3种策略对基于SN38的新型给药系统进行介绍,为后续开发出有效SN38新型给药系统提供参考。
7-Ethyl-10-hydroxycamptothecin(SN38),the active metabolite of irinotecan,has 100-1000 times the antitumor effect of irinotecan in vitro.However,SN38 has poor water solubility,and when pH>9.0,it was completely hydrolyzed and ring opened into the form of carboxylate without therapeutic effect.The novel SN38 drug delivery system could improve the physicochemical properties and in vivo performance of drugs in various cancer models,thereby enhancing anti-tumor activity and reducing adverse reactions.This article introduces the novel drug delivery system of SN38 from three strategies:physical encapsulation,chemical coupling,and active tumor targeting,to provide reference for the subsequent development of effective SN38 novel drug delivery systems.
作者
徐传锡
王志强
孙勇兵
XU Chuan-xi;WANG Zhi-qiang;SUN Yong-bing(National Engineering Research Center of Solid Preparation Manufacturing Technology of Traditional Chinese Medicine,Jiangxi University of Traditional Chinese Medicine,Nanchang 330006,China)
出处
《现代药物与临床》
CAS
2023年第7期1793-1797,共5页
Drugs & Clinic
基金
国家自然科学基金资助项目(81860630)
江西省重点研发计划项目(20192ACB70012)
江西中医药大学1050计划
南昌市重大科技攻关项目(2020-201-15)。
