胰高血糖素样肽-2/聚乳酸-羟基乙酸微球的制备及其体外释药性质研究

Preparation and in Vitro Release Property of Glucagon-like Peptide-2/PLGA Microspheres

目的:制备胰高血糖素样肽-2(GLP-2)/聚乳酸-羟基乙酸(PLGA)微球,并对其体外释药特性进行研究。方法:通过L(93)4正交试验设计优选微球最佳制备工艺条件,采用复乳-溶剂挥发法制备GLP-2/PLGA微球,并对制备工艺的重现性、所制微球的性质及体外释药性能进行考察。结果:优选的GLP-2/PLGA微球的最佳制备工艺稳定、重现性好;微球形态圆整,粒度分布均匀,平均粒径为14.49μm,载药量为13.48%,包封率为36.97%,微球在6 d内释药缓慢而均匀。结论:建立的制备工艺条件稳定、可行,所制微球初步达到了预期的试验目的。

OBJECTIVE： To prepare Glucagon-like peptide-2（GLP-2）/poly（lactide-co-glycolide acid）（PLGA） microsphere,and to study in vitro drug release property of the microsphere.METHODS： L9（34） orthogonal experiment design was introduced to optimize the preparation process of microsphere.GLP-2/PLGA microsphere was prepared by double emulsion（W/O/W） solvent evaporation method.Reproducibility of preparation process,in vitro release property and physical characteristics of microsphere were investigated.RESULTS： Optimized preparation process of GLP-2/PLGA microsphere was stable and reproducible.Microsphere showed even and regular appearance with mean particle size of 14.49 μm.The drug-loading rate was 13.48% and encapsulation efficiency was 36.97%.The drug release behavior was slow and regular in 6 days.CONCLUSION： The optimized preparation process is stable and practical.Prepared microspheres meet the expected experiment purpose.