【作者】 韩钢； 俞振伟； 马珂；

【Author】 HAN Gang,YU Zhen-wei,MA Ke(Sir Run Run Shaw Hospital,College of medicine,Zhejiang University,Hangzhou 310016)

【机构】 浙江大学医学院附属邵逸夫医院；

【摘要】 目的:制备氧氟沙星脂质体以增加细菌对药物的敏感性,并对其进行体外评价。方法:以磷脂和胆固醇为材料,以pH梯度法制备氧氟沙星脂质体;考察pH值,水浴温度和时间对脂质体包封率的影响。测定脂质体的粒径并进行电镜观察;以生理盐水为介质考察脂质体的体外释放;使用纸片扩散法和稀释法测定氧氟沙星脂质体和溶液对金黄色葡萄球菌的抑菌效果。结果:当pH值为7.0,水浴温度为50℃,水浴时间为5min时,脂质体的包封率最高,为82.40%。氧氟沙星脂质体的平均粒径为174nm,电镜下形态良好。脂质体在体外具有缓慢释放氧氟沙星的性质。氧氟沙星脂质体和溶液以纸片扩散法测定的抑菌圈直径相同,而以稀释法测定的最低抑菌浓度分别为0.39μg·mL-1和0.78μg·mL-1。结论:pH梯度法可制备包封率较高的氧氟沙星脂质体;氧氟沙星装载于脂质体后可增加对金黄色葡萄球菌的敏感性。更多还原

【Abstract】 Objective:To prepare ofloxacin liposome for increasing bacteria sensitivity,and to evaluate its in vitro property.Methods:Ofloxacin liposome was prepared by pH gradient method using phospholipid and cholesterol as material.The effect of pH value,warming temperature and time on encapsulation efficiency was investigated.The particle size of liposome was determined and the morphology was investigated by transmission electric microscope(TEM).The in vitro release experiment was carried using physiological saline as media.The bacteriostatic property against Staphylococcus aureus was investigated using disc diffusion test and dilution test.Results:The maximum encapsulation efficiency which was 82.40% could be achieved when pH value was 7.0,warming temperature was 50 ℃ and warming time was 5 min.The average particle size of liposome was 174 nm,and the ofloxacin liposome had shown good morphology under TEM.The liposome could release ofloxacin in a sustained manner in vitro.The liposome and solution of ofloxacin had shown the same inhibition zone in disc diffusion test,while the minimal inhibitory concentration determined by dilution test was 0.39 μg.mL-1 and 0.78 μg.mL-1,separately.Conclusion:Ofloxacin liposome with high encapsulation efficiency could be prepared by pH gradient method,and the bacteriostatic effect against Staphylococcus aureus of ofloxacin could be heightened by incorporating into liposome.更多还原