负载利福平的Pluronic L61-PBSu纳米粒的制备及性能研究  

Preparation and Properties of Rifampicin-loaded Pluronic L61-PBSu Nanoparticles

作　　者：徐新[1,2] 李琰 王庆毓 李玉红 茹国美[3] 董坚[1] 

机构地区：[1]绍兴文理学院化学化工学院,浙江绍兴312000 [2]浙江医药股份有限公司,浙江绍兴312000 [3]绍兴市人民医院医学研究中心,浙江绍兴312000

出　　处：《中国药学杂志》2017年第21期1924-1929,共6页Chinese Pharmaceutical Journal

基　　金：国家自然科学基金资助项目(21674063);浙江省自然科学基金资助项目(LY12E03001)

摘　　要：目的研究Pluronic L61修饰的聚丁二酸丁二醇酯(PBSu)载药纳米粒的制备及体外释放,并评价纳米粒的细胞毒性,为可生物降解PBSu材料在给药体系中的应用开辟途径。方法通过乳化法制备L61-PBSu纳米粒,以利福平为模型药物,研究L61-PBSu纳米粒负载药物的体外释放,并对药物释放进行动力学分析,采用MTT染色法评价L61-PBSu纳米粒对人卵巢癌细胞(OVCAR-3)的细胞毒性。结果纳米粒大小均匀,载药后平均粒径在(140±7)nm。纳米粒能对药物进行有效包封,包封率64.98%。累积释放率为90%时,体外释放时间达到27 h,药物释放机制遵循非Fick传输机制。纳米粒对OVCAR-3细胞毒性小,L61修饰后具有更低的细胞毒性。结论 L61-PBSu纳米粒制备简单,生物相容性好,对难溶性药物的缓释效果好,是一种有前景的被动靶向载体新平台。OBJECTIVE To study the preparation of pluronie-modified biodegradable poly（butylene succinate） （PBSu） nanopar- ticles（NPs） and evaluate the release kinetics of the drug-loaded PBSu NPs and the cytotoxicity of the NPs, so as to provide a new plat- form for the application of biodegradable PBSu in drug delivery. METHODS Pluronic L61-modified PBSu NPs were prepared by e- mulsification method, and the morphology of the NPs was observed by transmission electron microscopy. The in vitro release kinetics of the rifampicin-loaded L61-PBSu NPs at 37 ~C was studied. The cytotoxicity of the L61-PBSu NPs against human ovarian cancer cells （OVCAR-3） was evaluated by MTT assay. RESULTS The drug-loaded NPs had a unimodal distribution with an average size of （ 140 -＋ 7 ） ran. The drug encapsulation efficiency attained 64.98%. The release time reached 27 h when the cumulative release per- centage was 90%. The release kinetics followed non-Fickian mechanism. The NPs demonstrated very low cytotoxicity against OVCAR- 3 caneer cells. Modification by L61 improved bioeompatibility. CONCLUSION The Pluronic-modified PBSu NPs are easy to pre- pare, biocompatible, and show great promise as a new passive targeting platform for controlled release of insoluble drugs.

关 键 词：纳米粒 利福平 释放动力学 细胞毒性 可生物降解 

分 类 号：R944[医药卫生—药剂学]