摘要
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 and characterize the poly(lactic--co-glycolic acid )(PLGA) microspheres containing 10- hydroxycamptothecin (PMCH). Methods PMCH were prepared by emulsion-solvent evaporation method, the morphology was examined by scanning electron microscope, the encapsulation efficiency, drug loading rate and in vitro release were measured by high- performance liquid chromatography, and the median lethal dose on mice was calculated by modified Cole's method. Results Theprepared PMCH were spherical in shape with a mean size of 30.8 μm, encapsulation efficiency of 85.5 %, drug loading rate of 4.28 %. The cumulative release of hydroxyeamptothecin from microspheres was 81.4 % within 28-day. The median lethal dose of 10- hydroxycamptothecin on mice was 18.4 mg/kg by intravenous injection, 71.3 mg/kg by intramuscular injection, and 138.5 mg/kg whenusing PMCH intramuscular injection. Conclusion It is demonstrated that PLGA microspheres containing lO-hydroxycamptothecin were successfully prepared by emulsion-solvent evaporation method with optimal particle size, high drug loading rate and encapsulation efficiency, suitable release kinetics, and low toxicity, which would possess potential clinical application value.
出处
《生物医学工程与临床》
CAS
2012年第2期114-117,共4页
Biomedical Engineering and Clinical Medicine
基金
福建医科大学青年骨干教师基金
关键词
羟基喜树碱
聚乳酸-羟基乙酸
缓释材料
微球
lO-hydroxycamptothecin
poly(lactic-co-glycolic acid)
sustained-release material
microspheres