叶酸偶联纳米紫杉醇的制备  

Preparation of folic acid coupled nano-paclitaxel drug

作　　者：佟玲霞[1] 李红霞[1] 

机构地区：[1]首都医科大学附属北京世纪坛医院妇产科,北京100038

出　　处：《首都医科大学学报》2012年第5期565-568,共4页Journal of Capital Medical University

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(Z080507030808028)~~

摘　　要：目的制备磷脂酰乙醇胺-聚乙二醇2000-叶酸(folic acid monomethoxy-polyethylene glycol 2000-distearoyl phosphatidylethanolamine,ESPE-PEG2000-FA)修饰的紫杉醇纳米脂质体并考察其性质。方法采用超声乳化-溶剂挥发法制备DSPE-PEG2000-FA胶束;采用薄膜分散-挤压法制备紫杉醇脂质体;两者共同孵育形成DSPE-PEG2000-FA修饰的紫杉醇纳米脂质体;并测定修饰前后脂质体的粒径,包封率。结果叶酸偶联纳米紫杉醇药物的粒径(140.5±10.3)nm,多分散指数0.263±0.061,与原料药物纳米紫杉醇的粒径[(121.6±12.7)nm]和多分散指数(0.262±0.031)相比,差异无统计学意义。叶酸-紫杉醇纳米脂质体药物的包封率高达97%,与原料药紫杉醇纳米脂质体的包封率99%相比,差异无统计学意义,保证了药物的纯度和有效性。。结论本研究报道了一种靶向叶酸偶联纳米紫杉醇的新剂型及制备方法。该剂型有良好的药物包封率和胶体稳定性。Objective To prepare the folic acid coupled nano-paclitaxel drug for targeted tumor therapy. Methods Nano-paclitaxel was prepared by polycarbonate membrane dispersion-extrusion. The method of ultrasonic emulsification-solvent evaporation was adopted to prepare DSPE-PEG2000-FA micelle. Co-incubation method was used to prepare DSPE-PEG2000-FA modified folic acid coupling nano- paclitaxel. The mean diameter of folic acid coupling nano-paclitaxel drugs and the encapsulation efficiency were determined by zetasizer and elution curve of drug. Results Compared with the diameter of nano-paclitaxel particle[ （ 121.6 ± 12.7 ） nm] and polydispersity index （PDI） （ 0. 262 ± 0.031 ）, the mean diameter of folic acid coupling nano-paclitaxel drugs [ （ 140.5 ± 10.3 ） nm ] and PDI （ 0. 263 ± 0. 061 ） were slightly larger, but the difference was not statistically significant （t = 2. 013; P = 0.114 ）. In contrast to the encapsulation efficiency of the crude drugs （nano-paclitaxel drugs） 99% , the encapsulation efficiency of folic acid coupling nano-paclitaxel drugs was as high as 97% with no significant decline, which ensures purity and effectiveness of the drugs. Conclusion The novel formulation of FR- targeted folic acid coupling nano-paelitaxel is reported. This formulation has good drug loading properties, drug encapsulation efficiency, and exhibits excellent colloidal stability.

关 键 词：磷脂酰乙醇胺-聚乙二醇2000-叶酸 脂质体 紫杉醇 粒径 包封率 

分 类 号：R94[医药卫生—药剂学]