初乳搅拌速率对复乳法制备载蛋白微球性质的影响  

Effect of Homogenization Speed on Morphology and Release of Protein Loaded PLGA Microspheres Made by WOW Method

作　　者：黄小舟[1] 成晓岚[1] 罗宇燕[1] 郭喆霏[1] 钟晨[2] 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）》2015年第3期119-124,共6页Acta Scientiarum Naturalium Universitatis Sunyatseni

基　　金：广东省重大专项科技计划资助项目(2011A080504003)

摘　　要：采用复乳法制备载牛血清白蛋白的聚乳酸聚乙醇酸(PLGA)微球,研究初乳搅拌速率(5 000、10 000和15 000 r/min)对微球性质的影响。以包封率、载药量、粒径等为指标,评价其理化性质;扫描电镜观察微球内外形态,并通过图像分析软件计算其结构参数;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;荧光摄取实验考察孔洞与微球表面连通情况;并考察微球体外释药行为及降解过程中微球的内外形态变化。随着搅拌速率的增加,微球表面及内部孔洞增加,内部孔洞孔径减小,微球释药及降解速率减慢,但对微球粒径及截面孔隙率无显著影响。10 000 r/min组,微球包封率有最大值,1 d的突释率最低,且有最低的表面孔洞连通率;5 000 r/min和15 000 r/min组,微球突释率较高。不同初乳搅拌速率所得微球的内外形态在载蛋白的PLGA微球的释放中发挥重要作用。Poly（ lactic-co-glycolic acid）（ PLGA） microspheres loaded bovine serum albumin were prepared by WOW double emulsion method. The influence of homogenization speed during primary emulsion（ 5 000,10 000,15 000 r/min） on the physicochemical properties was investigated. Encapsulation efficiency,drug loading and particle size were used to evaluate the physicochemical properties of the microspheres. The surface and internal morphology of the microspheres was investigated by scanning electron microscopy（ SEM）. The structure parameters were analyzed by image analysis software. Confocal laser scanning microscopy was utilized to observe protein distribution within the skeletons of the microspheres.Finally,the connectivity of the microspheres was examined by the uptake experiments. Moreover,the release behaviors and the surface and internal structural evolution were also systematically studied. When the homogenization speed increased,the number of surface and internal pores increased,pore size of internal pores decreased. Besides,higher homogenization speed may result in slower drug release and degradation of the microspheres. But it caused no significant difference in the particle size and cross-sectioned porosity. In 10 000 r / min group,the microspheres showed highest encapsulation efficiency and lowest burst release rate in the first day and lowest surface pore connectivity. While in 5 000 r / min and15 000 r / min group,microspheres released faster,with a higher burst release. The microspheres prepared at different homogenization speed showed different surface and internal morphology,which play a significant role in in vitro release behaviors.

关 键 词：微球 显微结构 缓释 聚乳酸聚乙醇酸 初乳搅拌速率 

分 类 号：R927.2[医药卫生—药学]