SPG膜乳化法制备粒径均一可控的载蛋白缓释微球

Preparation of protein loaded microspheres with uniform and controllable particle sizes by SPG membrane emulsification

目的:研究一种制备粒径均一可控的载蛋白缓释微球的新工艺,探究微球粒径、载体材料、形态结构与微球载药释药性能的关系。方法:以牛血清白蛋白(BSA)为模型药物,PLGA和PEG-PLGA作为载体材料,采用SPG膜乳化法,通过调整不同孔径(3,5,7,12μm)的SPG膜制备不同粒径的微球。考察微球粒径、包封率、释放行为、表面/内部形态等性质,并对微球微观结构相关的参数如孔径、平面孔隙率等进行定量分析。结果:微球的粒径与SPG膜孔径呈正相关关系,且相关系数>0.9。随着微球粒径的增大,载药量和包封率也呈现增大的趋势,突释减轻。PLGA和PEG-PLGA微球的内部结构随微球粒径增加的变化差异较大。结论:获得较为满意的制备载蛋白微球的新工艺,微球形态圆整,粒径均一可控。

OBJECTIVE To prepare protein sustained release microspheres with uniform and controllable particle sizes by a new method, then explore the relationship between microspheres particle size, carrier materials, morphological structure and the drug release characteristics. METHODS SPG membranes with different apertures （3,5,7,12μm） were chosen to prepare sustain released microspheres of different particle sizes by SPG membrane emulsification. Bovine serum albumin （BSA） was used as the model drug and PLGA/PEG-PLGA as the carrier material. The particle size, entrapment efficiency, release behavior and surface/internal morphology were investigated, and the microstructures related parameters such as pore size and plane porosity were quantitatively analyzed. RESULTS The particle size of microspheres was positively correlated with the pore size of SPG membrane, and the correlation coefficient was 〉0. 9. With the increase of particle size, the drug loading and entrapment efficiencies also showed increasing trends, and the burst release was decreased. The internal structures of PLGA and PEG-PLGA microspheres varied greatly with increase of microsphere particle size. CONCLUSION This new method can prepare protein loaded microsphere with rounded surface and more uniform particle size.