复乳法及其改良法制备的干扰素PLGA微球载药释药特性的对比  

To Compare the Drug-Loading Characteristics and Release Behavior of Interferon PLGA Microspheres Prepared by Normal and Modified Double-Emulsion Methods

作　　者：罗宇燕[1] 麦海燕[1] 黎呐[2] 金启星[1] 黄小舟[1] 张永明[1] 

机构地区：[1]中山大学附属第三医院,广东广州510630 [2]中山大学药学院,广东广州510006

出　　处：《中山大学学报（自然科学版）》2014年第3期110-114,共5页Acta Scientiarum Naturalium Universitatis Sunyatseni

基　　金：广东省重大科技专项资助项目(2011A08054003)

摘　　要：改良法在复乳法基础上结合了海藻酸钠与Ca2+螯合形成缓释凝胶的原理。分别用上述两法制备蛋白药物干扰素α-1b的聚乳酸聚乙醇酸(PLGA)微球,以包封率、载药量等为指标,评价其理化性质;扫描电镜观察微球内外形态,软件计算其结构参数;用表面蛋白染色、激光共聚焦显微镜观察蛋白在微球表面及骨架内的分布情况;考察微球体外释药行为。与复乳法相比,改良法所得微球有较高的包封率和载药量(61.85%,0.724 3%),表面孔洞少、孔隙率低;内部孔洞大而少,孔隙率无显著差异;蛋白更多地分布在微球内部孔洞壁上而非表面;突释显著降低,缓释时间延长至20 d以上,30 d累积释药约70%。表明改良法所得微球载药释药性能较好,释药符合缓释制剂标准。The modified method integrated the principal that sodium alginate produces ionic interaction with calcium ion to form a kind of sustained-release gel into the double-emulsion method. Interferon α1b （IFN α-1b） poly （lactic-co-glycolic） （PLGA） microspheres were prepared by the above two methods. Encapsulation efficiency, drug loading, yield and average size were used to evaluate the physicochemical properties of microspheres; Scanning electron microscope was taken to observe the outlook and internal morphology of microspheres, while the structure parameters were analyzed by the image analysis software Image J; Staining surface protein method and confocal laser scanning microscope were utilized respective- ly to observe protein distribution on the surface and inside the microsphere skeletons; Finally, the micro- spheres in vitro release pattern was studied. Compared with microspheres made by the double-emulsion method, the ones made by modified method were of the following characteristics： high encapsulation effi- ciency and drug loading （61.85 % , 0. 7243 % ） ; less pores on the surface with lower surface porosity; less but bigger pores inside the micorspheres, with cross-sectioned porosity equal to the double-emulsionmethod ; less proteins distributed on the surface, while more in the inner hole wall of the microspheres; The cumulated release percent was about 70 % in 30 d, with apparently less burst-release and sustained- release period over 20 d. The result shows that IFN-PLGA microspheres produced by modified method were of better drug-loading and release properties

关 键 词：缓释微球 聚乳酸聚乙醇酸 干扰素 改良复乳法 激光共聚焦 

分 类 号：R927.2[医药卫生—药学]