SPG膜乳化法制备槲皮素缓释微球的工艺优化与表征及体外释放研究

Optimization,Characterization,and in vitro Release of Quercetin Sustained-release Microspheres Prepared by SPG Membrane Emulsification

目的以槲皮素作为模型药物,制备聚乳酸-羟基乙酸共聚物(PLGA)缓释微球,考察其粒径及其分布、形态、包封率、载药量和体外释药性质。方法采用SPG膜乳化法制备微球,单因素法初步优化制备处方;粒径分析仪检测微球的粒径及其分布;光学显微镜观察微球形态;通过紫外分光光度法测定微球的包封率和载药量;利用直接释药法和超速离心法结合对槲皮素微球的体外释放行为进行考察。结果制备的槲皮素微球形态圆整,粒径为(0.623±0.04)μm;包封率91.61%;载药量6.97%;体外释放平缓,无突释效应。结论经处方优化制备的槲皮素微球表面形态圆整,其粒径均一,包封率高,体外释药平缓,工艺重现性好。

Objective To prepare sustained-release microspheres of poly(lactic-co-glycolic acid)copolymer(PLGA)using quercetin as a model drug,and to investigate its particle sizes and its distribution,morphology,encapsulation efficiency,drug loading,and in vitro release properties.Methods SPG membrane emulsification method was used to prepare microspheres,and a single factor method was used to optimize the formulation.Particle size analyzer was used to detect the particle sizes and distribution of the microspheres.Optical microscopy was used to observe the morphology of the microspheres.The encapsulation efficiency and drug loading of the microspheres were determined by UV spectrophotometry.The in vitro release behavior of quercetin microspheres was investigated by a direct release method and ultracentrifugation.Results The surface of the prepared quercetin microspheres was smooth and round,and the size was small(0.623±0.05)μm;the encapsulation efficiency was high in 91.61%,and the drug loading was 6.97%;the in vitro release was gentle with no burst release effect.Conclusion The surface morphology of quercetin microspheres prepared by formulation optimization was round.Its particle size was uniform,and the encapsulation efficiency was high.The release was gentle in vitro,and the process reproducibility was good.