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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 study the preparation method of hydroxycamptothecin-loaded poly (lactic acid) microspheres and study its in vitro release properties. Methods: Polylactic acid microspheres loaded with hydroxycamptothecin were prepared by the modified emulsion-solvent evaporation method with PLA as the membrane-forming material and the preparation process was optimized. The drug-loaded microspheres were characterized and the drug-loaded microspheres In vitro release test. Results: The size of microspheres was 1 ~ 7μm and the size was uniform. The encapsulation efficiency of drug-loaded microspheres was 62.2% at the concentration of 10mg.mL-1 and the drug loading was 1.69% Higuchi equation. CONCLUSION: Hydroxycamptothecin microspheres with high entrapment efficiency can be prepared by emulsion-solvent evaporation method with PLA as the membrane-forming material, which is expected to reduce the dose of hydroxycamptothecin, reduce adverse reactions and improve the targeting Sexual goals.