目的:研究载羟基喜树碱的聚乳酸微球的制备方法并考察其体外释药性质。方法:以PlA为成膜材料,采用改良乳化-溶剂挥发法,制备载羟基喜树碱的聚乳酸微球并优化制备工艺;对载药微球进行表征;超声介导下进行载药微球的体外释药试验。结果:微球粒径在1~7μM,大小均一;羟基喜树碱浓度在10Mg.Ml-1下,载药微球包封率为62.2%,载药量为1.69%;药物体外释药符合HIguCHI方程。结论:采用乳化-溶剂挥发法,以PlA为成膜材料可制得具有较高包封率的羟基喜树碱微球,有望实现降低羟基喜树碱给药量、减少不良反应,提高靶向性的目标。Objective:To prepare hydroxycamptothecin(HCPT)-loaded PLA microspheres and study the release of HCPT in vitro.Methods:To optimize the preparation process,the HCPT-loaded PLA microspheres were prepared by using an improved solvent evaporation method;drug-loaded microspheres was characterized;in vitro drug release experiments were carried out under ultrasound.Results:The sizes of drug loaded PLA microspheres were homogeneous and between 1--7 μm;the concentration of HCPT was 10 mg·mL-1,the drug encapsulation efficiency was 62.2%,and the drug-loading amounts was 1.69%;the release in vitro complied with Higuchi equation.Conclusion:The improved solvent evaporation method with PLA as the film-forming material can increase the encapsulation efficiency of HCPT-loaded microspheres,thus the reduction of dosage and improvement of toxic effects of HCPT would be expected.Targeting effect may be improved.福建省卫生厅青年科研项目(2009-2-79
