氟尿嘧啶聚丙交酯乙交酯-聚乙二醇单甲基醚纳米粒的制备及体外释放的研究  

Study on Preparation and in Vitro Release Characteristics of 5-Fluorouracil Loaded PLGA-mPEG Nanoparticles

作　　者：纪宏宇[1,2,3] 谷宏伟[1,3] 唐景玲[3] 刘红梅[1,2,3] 于明涛[1,3] 吴琳华[1,2,3] 

机构地区：[1]哈尔滨医科大学第二附属医院药学部,哈尔滨150086 [2]黑龙江省高校重点实验室,哈尔滨150086 [3]哈尔滨医科大学药学院,哈尔滨150086

出　　处：《中国药学杂志》2011年第23期1814-1818,共5页Chinese Pharmaceutical Journal

基　　金：黑龙江省青年科学基金项目(QC2011C104);黑龙江省卫生厅科研课题(No.2009-136);哈尔滨医科大学附属第二医院院青年基金项目(QN2009-03)

摘　　要：目的制备氟尿嘧啶聚丙交酯乙交酯-聚乙二醇单甲基醚(PLGA-mPEG)纳米粒,并对其体外释放特性进行研究。方法采用纳米沉淀法制备氟尿嘧啶PLGA-mPEG纳米粒,采用高效液相色谱法进行包封率的测定。在单因素实验的基础上,通过正交实验优化处方和制备工艺。采用动态膜透析法对纳米粒子的体外释药特性进行研究。结果制备的纳米粒为较均匀的类球形粒子,平均粒径约124.3 nm,Zeta电位-20.6 mV,平均包封率为(44.72±0.38)%。体外释药实验研究表明,粒子在2 h的突释量小于30%,在突释后的48 h内药物缓慢释放。结论纳米沉淀法操作简单,制备的氟尿嘧啶PLGA-mPEG纳米粒粒径小,体外药物释放具有良好的缓释效果。OBJECTIVE To prepare 5-fluorouracil loaded PLGA-mPEG nanoparticles （5-FPN） and study its release profile in vitro. METHODS 5-FPN was prepared by nano-precipitation method. A reversed-phase high performance liquid chromatog- raphy （RP-HPLC） method was used to determine the entrapment efficiency of S-FPN. Based on the single-factor experiment, the formulation and preparation process of 5-FPN was optimized using orthogonal design. RESULTS 5-FPN had regular spherical appearance with a mean diameter of 124.3 nm and Zeta potential of - 20.6 mV, and entrapment efficiency of （44.72 _＋ 0.38 ） %. In the release in vitro, the cumulative percentage of abruptly released drug from PLGA-mPEG nanoparticles was lower than 30% in 2 h. The 5-FPN showed delayed release in 48 h after the drug dumping. CONCLUSION The nano-precipitation method is convenient. The 5-FPN prepared by nano-precipitation method has smaller particle size and possesses good sustained re- lease characteristics in vitro.

关 键 词：氟尿嘧啶 纳米粒 纳米沉淀法 体外释放 

分 类 号：R944[医药卫生—药剂学]