左氧氟沙星/PLGA亚微粒的制备、表征和体外释药考察  

Preparation,Characterization and in vitro Drug Release of Levofloxacin/PLGA Submicroparticles

作　　者：陈文斐[1] 倪健新[1] 

机构地区：[1]温州医学院附属眼视光医院,浙江温州325027

出　　处：《中国药师》2013年第4期550-552,共3页China Pharmacist

摘　　要：目的:制备左氧氟沙星/PLGA亚微粒,并进行相关表征和体外释放行为考察。方法:采用纳米共沉淀法制备左氧氟沙星/PLGA亚微粒,采用激光粒度分析仪以及扫描电镜分别进行亚微粒粒度测定和形貌分析。同时采用紫外-可见分光光度法(UV)测定其载药量与体外药物释放行为。结果:经过激光粒度分析仪测定,所制备的左氧氟沙星/PLGA亚微粒粒径为197～230 nm,Zeta电位为-24 mv。扫描电镜观察亚微粒呈圆形/椭圆形,分布均匀。UV法测定亚微粒的载药量为6.25%～9.38%,包封产率为12.45%～46.59%。体外释放结果显示相比于商品化左氧氟沙星滴眼液,所制备的左氧氟沙星/PLGA亚微粒具有良好的缓释效果。结论:通过纳米共沉淀法成功制备粒径均一,高载药量的左氧氟沙星PLGA亚微粒,同时能实现药物的缓慢释放,减少给药次数的目的。Objective： To prepare, characterize and investigate the in vitro drug release of levofloxacin/PLGA submicroparticles. Method： Levofloxacin/PLGA submicroparticles were prepared by a nano-coprecipitation method and characterized by a scanning elec- tron microscope （SEM） and a dynamic light scattering （DLS）. The drug loading efficiency and in vitro drug release of the submicrop-articles were measured by UV. Result ： According to the results of DLS, the mean diameter of the developed levofloxacin/PLGA submi-croparticles was within the range of 197-230 nm, and the Zeta potential was about-24 my. The morphology of the developed submi-croparticles was spherical or nearly spherical with uniform size distribution. Drug release in vitro of the submicroparticles showed sus- tained release property comopared with that of the marketed levofloxacin eye drops. Conclusion： Levofloxacin/PLGA submicroparticles with uniform size distribution, high drug loading efficiency and sustained release behavior are successfully developed by the nano-copre- ci^itation method, which can reduce the administration frequency.

关 键 词：左氧氟沙星 PLGA亚微粒的制备 表征 体外释放 

分 类 号：R944.9[医药卫生—药剂学] R945[医药卫生—药学]