叶酸偶联纳米紫杉醇靶向治疗卵巢癌的细胞实验研究  

Experimental study of folic acid coupling nano-paclitaxel drugs in targeting targeting treatment of ovarian cancer cell-lines

作　　者：佟玲霞[1,2] 李红霞[1,2] 

机构地区：[1]北京大学第九临床医学院 [2]首都医科大学附属北京世纪坛医院,北京100038

出　　处：《现代妇产科进展》2013年第10期777-781,共5页Progress in Obstetrics and Gynecology

基　　金：北京市科委"叶酸纳米偶联紫杉醇药物靶向治疗卵巢癌的实验研究"项目资助(No:Z080507030808028)

摘　　要：目的:研究叶酸(FA)偶联纳米紫杉醇对卵巢癌的体外治疗效果,并初步探讨其作用机制。方法:共孵育法制备FA偶联纳米紫杉醇,荧光显微镜和流式细胞仪定性和定量测定其对SKOV3细胞的靶向作用,绘制细胞生长曲线;噻唑蓝法、流式细胞术及电子显微镜下观察FA偶联纳米紫杉醇对SKOV3细胞和SKOV3/TAX细胞的体外杀伤效应。结果:(1)FA偶联纳米紫杉醇的粒径为(140.5±10.3)nm,包封率为97%;(2)FA偶联纳米紫杉醇在FA受体(FR)介导下对SKOV3细胞有靶向杀伤作用,并且随时间延长,细胞内药物浓度逐渐增加;(3)FA偶联纳米紫杉醇对SKOV3细胞及SKOV3/TAX细胞的药效显著强于纳米紫杉醇,SKOV3/TAX细胞对FA偶联纳米紫杉醇的耐药指数有下降趋势。结论:FA偶联纳米紫杉醇可能利用FR为作用靶点,将药物主动靶向肿瘤细胞,提高药物在肿瘤细胞内的分布。其抗肿瘤疗效优于传统的紫杉醇。Objective： To study the effect and the mechanism of folic acid coupling nano-paclitaxel drugs in targeting treatment of ovarian cancer in vitro. Methods：The folic acid coupling nano-pachtaxel drugs were prepared by the co-incubation method. The targeted therapy of the drug was examined by using fluorescence microscope and flow cytometric analysis （FCM）. The drug effects on SKOV3 cells and SKOV3/TAX cells in vitro were examined by drawing cell growth curve and using MTT method, FCM, electron microscopy. Results： （ 1 ） The particle size and encapsulation efficiency of folic acid coupling nano-paclitaxel drugs were （140.5± 10.3 ）nm and 97% respectively. （2）Folic acid coupling nano-paclitaxel drugs may actively targeting the folic acid receptor, enable to deliver the nanoscale drugs directively into cancer cells. The effective of drug depended on the incubating time and drug concentration. （3） The effects of folic acid coupling nano-paclitaxel drugs on SKOV3 cells and SKOV3/TAX cells were significantly better than nano-paclitaxel. The resistance index of SKOV3/TAX cells was decreased in the course of treatment. Conclusions： Folic acid coupling nano-paclitaxel drugs may actively targeting the folic acid receptor, enable to deliver the nanoscale drugs directively into cancer cells, which could increase the therapeutic effect of the drug largely. The anti-tumor efficiency of the novel FR-targeted nanoseale drug is better than traditional preparations.

关 键 词：叶酸偶联纳米紫杉醇 叶酸受体 靶向治疗 

分 类 号：R737.33[医药卫生—肿瘤]