粒细胞-巨噬细胞集落刺激因子微球制剂的体外释放研究

目的：开发一种粒细胞-巨噬细胞集落刺激因子（GM—CSF）长效缓释微球剂型。方法：采用S／O／hO法制备了包裹粒细胞一巨噬细胞集落刺激因子多糖玻璃体颗粒的PLGA微球，考察了微球的表面形态、粒径分布等，并且运用ELISA方法考察了微球的体外释放效果。结果：本方法制备的粒细胞-巨噬细胞集落刺激因子微球光滑圆整，粒径分布均匀，体外可以缓释达32天，累积释放率接近90％。结论：本方法制备的粒细胞-巨噬细胞集落刺激因子微球能有效地保护蛋白活性，同时实现长效缓释的目标，是一种可行的蛋白缓释方案。

Study on the Vitro Release of GM-CSF Microspheres

Objective： An effective long-acting sustained-release preparation of GM-CSF was developed. Methods： GM-CSF dex- tran glassy particles were prepared by a unique method of aqueous-aqueous ＂emulsion＂, and then the GM-CSF-loaded dextran glassy particles were encapsulated into PLGA microspheres by the method of solid-in-oil-in- hydrophilic oil （S/O/hO） emulsion-evaporation technique. The microspheres were characterized by SEM and size distribution. In vitro release profiles of GM-CSF loaded microspheres were plotted by Human GM-CSF Quantikine ELISA Kit. Results： The GM-CSF-loaded microspheres possessed spherical shape and smooth surface. The size distribution demonstrated that average spherical diameter of GM-CSF microspheres was equal to 25.427 μm. The accumulated release in vitro was 87% after 32 days. Conclusions： This method effectively protected the bioactivity of GM-CSF and microspheres exhibited an ideal sustained release behavior.