膜乳化法制备单分散性载羟基喜树碱缓释微球

Uniform microspheres loaded with hydroxycamptothecin （HCPT） by employing shirasu porous glass emulsification technique

目的 研究利用微孔膜乳化法制备载抗癌药10-羟基喜树碱（IqCPT）缓释微球的可行性。方法 以HCPT为模型药物，聚乳酸（PEA）为载体，以膜乳化法制备载药微球，并研究制剂的表面形态、载药率、包封率和缓释效果等性质。结果 膜乳化法制备的载HCPT聚乳酸微球，粒径可控制在1-10μm之间。表面圆整，稳定性、单分散性良好，载药率和包封率最高分别可达32．7％和81．7％，24h体外累积释放量为17．3％。结论 膜乳化法制备的载HCPT微球制剂均匀分散，具有明显缓释效果，是制备缓释微球制剂的较好方法。

Objective To investigate the feasibility of employing shirasu porous glass（SPG） emulsification technique to prepare microspheres loaded with antitumor drug hydroxycamptothecin（HCPT）. Methods polylacticacid（PLA） microspheres loaded with model drug HCPT were prepared by shirasu porous glass （SPG） emulsification technique. The preparation was characterized by observing its surface shape, drug loading/drug encapsulation efficiency and drug releasing capability. Results The diameters of the microspheres could be controlled between 1- 10μm. The preparation was stable and narrowly dispersed and had perfect surface circularity. The drug loading and drug encapsulation efficiency could reach 32.7% and 81.7%, respectively. The accumulated drug release rate in 24 hours was 17.3%. Conclusion HCPT loaded microspheres prepared by SPG emulsification technique are uniformly dispersed and demonstrated ideal sustained drug release. SPG emulsification technique should be a good method to obtain microspberes for sustained drug release.