载紫杉醇的甲氧基聚乙二醇-胆固醇胶束的研究  

Study on methoxy poly ethylene glycol-cholesterol micelles carrying Paclitaxel

作　　者：甘李 余义义 徐蓓[1] 宋相容[1] 何谷[1] 何黎黎[2] 

机构地区：[1]四川大学华西医院生物治疗国家重点实验室,四川成都610041 [2]西南民族大学化学与环境保护工程学院,四川成都610041

出　　处：《华西药学杂志》2014年第6期613-615,共3页West China Journal of Pharmaceutical Sciences

基　　金：国家自然科学基金资助项目(批准号:81302729);四川大学优秀青年学者基金(编号:2013SCU04A19)

摘　　要：目的制备载紫杉醇(PTX)的甲氧基聚乙二醇-胆固醇(m PEG-Chol)胶束(PTX-PM),并考察其性质及体外抗肿瘤活性。方法采用薄膜分散法制备PTX-PM,以胶束粒径、载药量和包封率为评价指标,优化其制备工艺;并对其体外释放特性及抗肿瘤活性进行评价。结果 PTX-PM的最优处方为:PTX与m PEG-Chol比例为1∶20,粒径为19.22±1.32 nm,PDI为0.267±0.021,包封率为88.44%±1.08%;体外释放速率在p H5.5条件下较p H7.4的快;对A549和Hep G-2细胞的生长抑制活性均与游离PTX相当,对A549的抑制作用强于Hep G-2。结论 m PEG-Chol可作为包载PTX的一种新型纳米材料;PTX-PM的体外释放呈明显p H依赖性,且具有较好的体外抗肿瘤活性。OBJECTIVE To prepare methoxy poly ethylene glycol- cholesterol（ m PEG- Chol） micelles（ PTX- PM） carrying Paclitaxel（ PTX）,and investigate the properties and in vitro anti- tumor activity. METHODS PTX- PM was prepared by film dispersion method and the processing parameters were optimized according to the size and entrapment efficiency（ EE%） of micelles.The in vitro release profiles and in vitro anti- tumor activity investigation was carried out using the optimal PTX- PM. RESULTS The optimal PTX- PM,with the size of 19. 22 ± 1. 32 nm,PDI of 0. 267 ± 0. 021 and EE of 88. 44% ± 1. 08%,was prepared using PTX / m PEG- Chol with the mass ratio of 1∶20. The release of PTX has faster at p H5. 5 than at p H7. 4. PTX- PM had the similar cell growth inhibition activity on both A549 and Hep G- 2 to free PTX in vitro,between which higher efficacy was found on A549.CONCLUSION m PEG- Chol is one of novel and ideal biomaterials as PTX nano- carrier. PTX- PM presentes sustained release profiles and achieves higher anti- tumor activity.

关 键 词：紫杉醇 甲氧基聚乙二醇-胆固醇 胶束 人肺癌细胞A549 人肝癌细胞HEPG-2 

分 类 号：R94[医药卫生—药剂学]