拉莫三嗪胶束的制备及其靶向性能考察  

Preparation and Targeting Capacity of Lamotrigine-loaded Pluronic Mixed Micelles

作　　者：孟鑫[1,2] 李佳佳[3] 刘建盛[4] 吴玉林[2] 沈腾[1] 

机构地区：[1]复旦大学药学院药剂学教研室,智能化递药教育部重点实验室,上海201203 [2]中国药科大学药学院生理学教研室,江苏南京211198 [3]上海交通大学医学院附属仁济医院,上海200127 [4]上海交通大学附属第六人民医院神经内科,上海200233

出　　处：《中国医药工业杂志》2016年第5期565-569,共5页Chinese Journal of Pharmaceuticals

基　　金：国家自然科学基金面上项目(81072594)

摘　　要：以Pluronic P123与F127(质量比2∶1)为载体,采用薄膜水化法制备包载抗癫痫药拉莫三嗪(lamotrigine,1)的混合胶束(PF胶束)并表征。结果显示PF混合胶束包封率为92.39%、载药量为4.88%、平均粒径为21.32 nm。与P123胶束相比,PF混合胶束显著改善了体系稳定性。细胞激光共聚焦图像显示,与游离罗丹明123(一种P-糖蛋白底物,2)相比,PF胶束可显著促进脑微血管内皮细胞对2的摄取。结果预示包载1的PF混合胶束有望成为治疗难治性癫痫的新型药物载体。Lamotrigine （1）-loaded polymer micelles, named PF micelles, were prepared by thin-film hydration method with the mixture of Pluronic P123 and F127 （2 ： 1, w/w） as the carriers. The physicochemical properties of PF micelles were characterized. The results showed that encapsulation efficiency and drug loading of PF micelles were 92.39% and 4.88% with the average diameter of 21.32 nm. And the PF micelles were much more kinetically stable in aqueous environment than P 123 micelles. Rhodamine 123 （2）, a P-glycoprotein substrate, was used to evaluate the effects of PF micelles on cellular uptake of fluorescence by brain capillary endothelial cells （BCECs）. The results of confocal laser scanning microscopy showed that 2-loaded PF micelles exhibited a significant increase in cellular uptake in BCECs compared with free 2. These results indicated that l-loaded PF mixed micelles were promising vehicles for brain targeted delivery, which might have implications in the treatment of intractable epilepsy.

关 键 词：拉莫三嗪 抗癫痫药 PLURONIC 胶束 纳米载体 靶向性能 

分 类 号：R944.9[医药卫生—药剂学]