水溶性及靶向性紫杉醇前药的研究进展  

Research progress in improving water solubility and targeting of paclitaxel by prodrugs

作　　者：马晶晶 杨政 郭惠[1] 张莹莹 刘理想 周静 靳如意 李治[1] 唐于平 MA Jing-jing;YANG Zheng;GUO Hui;ZHANG Ying-ying;LIU Li-xiang;ZHOU Jing;JIN Ru-yi;LI Zhi;TANG Yu-ping(Key Lab Basic&New Herbal Medicament Research,Shaanxi University of Chinese Medicine,Xianyang 112046,China)

机构地区：[1]陕西中医药大学中药基础与新药研究重点实验室,咸阳712046

出　　处：《中国新药杂志》2021年第16期1489-1497,共9页Chinese Journal of New Drugs

基　　金：国家自然科学基金青年基金资助项目(81001669);陕西省中医药管理局资助项目(ZYMS005);陕西中医药大学学科创新团队资助项目(2019-PY02);陕西省自然科学基础研究重点资助项目(2020JZ-55);陕西中医药大学大学生创新创业计划资助项目(201805118,S201910716061)。

摘　　要：获得美国FDA批准的第一个来自天然植物的化学药物紫杉醇(paclitaxel,PTX)是一个广谱抗肿瘤药物,具有良好的抗肿瘤活性。但由于其本身复杂的化学结构、水溶性差、吸收不好等缺点限制了其在临床上的广泛应用。因此,如何改善其水溶性,提高生物利用度及其在肿瘤组织的靶向性,是近年来亟待解决的难点与重点。本文就近年来以改善其水溶性及靶向性的紫杉醇前药的研究进展进行简单综述。Paclitaxel,the first natural plant-derived chemical approved by the US FDA,is a broad-spectrum antitumor drug with good antitumor activity.However,due to its complex chemical structure,disadvantages such as poor water solubility and poor absorption limit its widespread clinical application.Therefore,how to improve its water solubility,bioavailability and targeting effect in tumor tissues has been a difficult and important issue to be solved.In this article,we briefly reviewed the research progress of paclitaxel prodrugs that improve its water solubility and targeting in recent years.

关 键 词：紫杉醇前药 水溶性 靶向性 抗肿瘤 

分 类 号：R979.1[医药卫生—药品]