载紫杉醇的大黄酸偶联物胶束对MCF-7细胞的毒性与细胞摄取研究  

Cytotoxicity and cellular uptake of paclitaxel-loaded carboxymethyl chitosan-rhein polymeric micelles in MCF-7 cells

作　　者：王晓颖[1] 王夏英 邱梁桢 欧阳惠枝 徐伟[1] WANG Xiaoying;WANG Xiaying;QIU Liangzhen;OUYANG Huizhi;XU Wei(School of Pharmacy,Fujian University of Traditional Chinese Medicine,Fuzhou 350122,China)

机构地区：[1]福建中医药大学药学院,福州350122

出　　处：《中国药科大学学报》2020年第1期33-37,共5页Journal of China Pharmaceutical University

基　　金：国家自然科学基金资助项目(No.81603301);福建省卫计委中青年骨干人才培养项目(No.2016-ZQN-69);中医药公共卫生服务补助专项(财社〔2017〕66号)。

摘　　要：通过MTT法评估了羧甲基壳聚糖-大黄酸偶联物(CR偶联物)和载紫杉醇(PTX)的CR偶联物胶束(PTX/CR偶联物胶束)对MCF-7细胞的细胞毒性,结果显示,CR偶联物具有良好的安全性;PTX/CR偶联物胶束24 h内表现出优于Taxol?的抗肿瘤活性。通过包载环境响应型荧光探针P4,考察了共载P4和PTX的CR偶联物胶束[(P4+PTX)/CR偶联物胶束]在MCF-7细胞中的摄取情况,结果显示,MCF-7细胞对其具有较好的摄取效果,(P4+PTX)/CR偶联物胶束组与其加维拉帕米组摄取量无显著性差异,提示CR偶联物胶束可以保护其所载荧光探针和/或药物不被P-gp外排到细胞外。该研究结果为CR偶联物及PTX/CR偶联物胶束的进一步体内研究奠定了基础。In this study,in vitro cytotoxicity of carboxymethyl chitosan-rhein conjugate(CR conjugate)and paclitaxel-loaded carboxymethyl chitosan-rhein polymeric micelles(PTX/CR PMs)was evaluated by MTT method in MCF-7 cells.The results showed that CR conjugate displayed good security;PTX/CR PMs in 24 h showed better antitumor activity than Taxol?.Environment-responsive fluorescent probe P4 was used to determine the cellular uptake of PTX/CR PMs in MCF-7 cells.The results also showed that P4 and PTX co-loaded carboxymethyl chitosan-rhein polymeric micelles[(P4+PTX)/CR PMs]could be taken up by MCF-7 cells.There was no difference between(P4+PTX)/CR PMs group and(P4+PTX)/CR PMs with verapamil group,suggesting that CR PMs could protect fluorescent probe and/or drugs in their cores avoiding efflux by P-glycoprotein.These results will contribute to in vivo study of CR conjugate and PTX/CR PMs in the future.

关 键 词：紫杉醇 羧甲基壳聚糖-大黄酸偶联物 聚合物胶束 抗肿瘤 细胞摄取 

分 类 号：R944[医药卫生—药剂学]