大黄素聚乳酸微球的制备及体外释药行为研究

Preparation of Emodin Loaded Polylactic Acid Microspheres and the Drug Release Study

目的制备包裹大黄素的聚乳酸微球并进行表征,研究其体外释放曲线。方法采用W/O/W溶剂蒸发法制备包裹大黄素的聚乳酸微球,并对微球的表面形态、粒径、载药量与包封率等质量指标进行考察,透析袋法考察体外释药行为,拟合动力学模型。结果包载大黄素的聚乳酸微球外观圆整,呈球形,粒径为(4.87±0.1)μm,载药量为(31.37±1.41)%,包封率为(92.18±0.39)%,体外释放时间10d,释放量(86.93±3.78)%,对其体外释药曲线进行拟合,大黄素聚乳酸微球释药符合Ritger-Peppas方程,其拟合方程为lnQ=0.3759lnt-2.0691(R^2=0.959)。结论制备的包裹大黄素的聚乳酸微球,粒径分布均匀,具有较好的稳定性,并能缓慢释放药物。

Objective To prepare and characterize the emodin loaded polylactic acid microsphere and investigate its release in vitro.Methods The emodin loaded polylactic acid microsphere were prepared using the W/O/W double-emulsion and solvent-evaporation method,the surface morphology,particle size,drug loading and entrapment efficiency of the microspheres were investigated,the drug release behavior in vitro was investigated by dialysis bag method,and the kinetic model was fitted.Results Emodin loaded polylactic acid microsphere were round and spherical in appearance,the particle size was(4.87±0.1)μm,the drug load was(31.37±1.41)%,the entrapment efficiency was(92.18±0.39)%,in vitro release time was 10 days,the release rate is(86.93±3.78)%.On the basis of the variance analysis of the fitting equation,the emodin microspheres fit the Ritger-peppas equation best.Conclusion Emodin loaded polylactic acid microspheres have uniform particle size distribution,good stability and slow drug release.