盐酸表柔比星-聚乳酸-羟基乙酸共聚物纳米粒的制备  

Study on Preparation of Epirubicin Hydrochloride Loaded Poly(L-Lactic-co-Glycolic Acid) Nanoparticles and the Effects in Vitro

作　　者：宋晶晶[1] 李慧[2] 傅红兴[2] 纪建松[3] 

机构地区：[1]温州医学院,325000 [2]温州医学院药学院,325035 [3]浙江省丽水市中心医院,323000

出　　处：《医药导报》2012年第6期779-782,共4页Herald of Medicine

基　　金：卫生部科研基金(WKJ2009-2-035)

摘　　要：目的制备盐酸表柔比星-聚乳酸-羟基乙酸(PLGA)共聚物纳米粒,对其进行质量评价。方法采用乳化-溶剂挥发法制备盐酸表柔比星纳米粒;对主要处方因素如PLGA用量、外水相中聚山梨酯-80用量、泊洛沙姆188和聚山梨酯-80比例进行正交设计,以药物的包封率、载药量和药物利用率等为考察指标。结果采用优化后处方制得的纳米粒药物包封率为(32.6±1.2)%,载药量为(7.2±0.5)%,药物利用率为(51.6±3.4)%,纳米粒平均粒径166.6 nm,药物可持续160 h释放。结论该方法制备盐酸表柔比星纳米粒工艺简单,无需使用聚乙烯醇,药物释放缓慢。Objective To prepare epirubicin hydrochloride-loaded poly L-lactic-co-glyeolic acid （PLGA） nanoparticles and investigate the characteristics. Methods The epirubicin hydrochloride-loaded PLGA nanoparticles were prepared by double emulsion-solvent evaporation method. The main effective factors such as the amount of PLGA, Tween-80 in external water phase, and the ratio of poloxamer 188 to Tween-80 were orthogonally designed. Drug entrapment efficiency, drug loading rate and drug utilization were determined. Results By using the optimal formulation, the drug encapsulation efficiency of the nanoparticles was （32.6± 1.2）% ; the drug loading was （7.2±0.5）% ; the drug utilization was （51.6±3.4）% ; the mean size of the nanoparticles was 166.6 nm; the drug release continued 160 hours. Conclusion Epirubicin hydrochloride-loaded PLGA nanoparticles are prepared successfully and simply without use of polyviol and display sustained drug release properties.

关 键 词：表柔比星 盐酸 聚乳酸-羟基乙酸共聚物 纳米粒 

分 类 号：R979.1[医药卫生—药品] TQ460.1[医药卫生—药学]