依托泊苷聚乳酸微球的制备

Preparation of etoposide Polylactic Acid Microspheres

目的:用生物可降解材料聚乳酸制备依托泊苷微球,并对其体外释药特性进行研究。方法:采用乳化-溶剂扩散法制备依托泊苷聚乳酸微球,通过正交试验确定最佳处方工艺;采用紫外分光光度法测定微球载药量、包封率和体外药物释放,利用光学显微镜观察微球形态和粒径分布。结果:所得微球外观圆整,平均粒径为12.87μm,载药量为14.79%,药物包封率为61.09%,体外释药符合Higuchi方程。结论:依托泊苷聚乳酸微球制备工艺稳定,体外释药符合长效制剂特征。

Objective To prepare etoposide microspheres using thg biodegradable meterials-polylactic acid and to study its release characteristics in vitro.Methods The polylactic acid microspheres were prepared by emulsion-solvent diffusion method and the orthogonal test design was used to optimize the formulation and technology.The drug-loading,emcapsulation and release in vitro were determined by ultraviolet spectrophotometry and the appearance and particle size of microspheres was observed by light microscope.Results The shape of etoposide microspheres was spherical with mean particle size of 12.87 μm.The drug loading and encapsulation efficiency were 14.79% and 61.09%,respectively.The in vitro release characteristics of microspheres was found to agree with Higuchi equation.Conclusion The technology of preparation was successful and etoposide polylactic acid micropheres showed significant sustained release.