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目的制备一种载羟基喜树碱的聚乳酸-羟基乙酸(PLGA)缓释微球,并考察其相关性能。方法采用乳化-溶剂挥发法制备羟基喜树碱PLGA微球,用扫描电子显微镜观察载药微球表面形态,测定平均粒径及跨距,高效液相色谱检测包封率、载药率及体外释放情况,改良寇氏法计算小鼠半数致死量。结果制备的载药PLGA微球呈圆球形,表面光滑,无粘连,平均粒径30.8μm,跨距0.9,包封率为85.5%、载药率4.28%,在体外28 d累积释放药物81.4%。羟基喜树碱小鼠静脉注射的半数致死量为18.4 mg/kg,肌内注射半数致死量为71.3 mg/kg,而羟基喜树碱PLGA微球肌内注射的半数致死量为138.5 mg/kg。结论乳化-溶剂挥发法制备的羟基喜树碱PLGA微球粒径适宜,包封率、载药率高,缓释效果好,毒性低,具有潜在的临床应用价值。
OBJECTIVE To prepare a polylactic-glycolic acid (PLGA) sustained-release microspheres loaded with hydroxycamptothecin and to investigate its performance. Methods Hydroxycamptothecin (PLGA) microspheres were prepared by emulsion-solvent evaporation method. The surface morphology of the loaded microspheres was observed by scanning electron microscopy. The average particle size and spans were measured. The encapsulation efficiency, drug loading rate and in vitro Release, improved Kou’s method to calculate the median lethal dose of mice. Results The prepared drug-loaded PLGA microspheres were spherical with a smooth surface and no adhesions. The average diameter was 30.8μm, the span was 0.9, the encapsulation efficiency was 85.5% and the drug loading rate was 4.28% . The median lethal dose of hydroxycamptothecin was 18.4 mg / kg for intravenous injection and 71.3 mg / kg for intramuscular injection. The half lethal dose of hydroxycamptothecin (PLGA) microspheres intramuscular injection was 138.5 mg / kg . Conclusions Hydroxycamptothecin (PLGA) microspheres prepared by emulsification-solvent evaporation method have the advantages of suitable particle size, high entrapment efficiency, high drug loading rate, good sustained-release effect and low toxicity, and have potential clinical application value.