奥沙利铂长循环脂质体的制备及其在小鼠体内的药效学研究  

Preparation of oxaliplatin long circulating liposomes and their pharmacodynamics in mice

作　　者：李哲[1] 马海英[1] 

机构地区：[1]中国医科大学附属第四医院药学部,沈阳110032

出　　处：《药学服务与研究》2015年第1期27-30,共4页Pharmaceutical Care and Research

基　　金：辽宁省科学技术计划项目(2011225020)

摘　　要：目的:制备奥沙利铂长循环脂质体,考察其在小鼠体内的药效学。方法:采用乙醇注入法制备奥沙利铂长循环脂质体,观察其形态,测定粒径分布和包封率。以S180荷瘤小鼠为模型,生理盐水为对照,测定奥沙利铂溶液和奥沙利铂长循环脂质体的抑瘤率,考察肿瘤生长情况以及小鼠生存情况。分别测定小鼠的白细胞计数、脾脏指数和胸腺指数,以考察对免疫器官的影响。结果:奥沙利铂长循环脂质体平均粒径为(112.2±0.3)nm,包封率为(59.93±0.67)%(n=3)。与奥沙利铂溶液相比,奥沙利铂长循环脂质体的抑瘤率明显提高[(30.4±1.9)%vs(85.8±2.3)%,P<0.05]。奥沙利铂脂质体组小鼠的白细胞计数、脾脏指数和胸腺指数与生理盐水组相比,无显著性差异(P>0.05),肿瘤体积增长缓慢,小鼠生长状态良好。结论:奥沙利铂长循环脂质体有显著的抑瘤作用,并减少了奥沙利铂的免疫系统毒性。Objective：To prepare oxaliplatin long circulating liposomes and study their pharmacodynamics in mice.Methods：The oxaliplatin long circulating liposomes were prepared by ethanol injection and morphology was observed,the grain size and entrapment efficiency were determined.Tumor inhibition rates,tumor growth situation,survival situation of mice administered with oxaliplatin solution and long circulating liposomes were investigated with S180tumor-bearing mouse as animal models and physiological saline as control.The count of white blood cells,spleen index and thymus index in mice were determined to evaluate the toxicity of oxaliplatin to immune organs.Results：The average grain size of oxaliplatin long circulating liposomes were（112.2±0.3）nm,and the entrapment efficiency was（59.93±0.67）%（n=3）.Compared with oxaliplatin solution,tumor inhibition rate of oxaliplatin long circulating liposomes was obviously increased [（30.4±1.9）% vs（85.8±2.3）%,P〈0.05].There were no significant differences in the count of white blood cells,spleen index and thymus index,as compared with those of the physiological saline group（P〉0.05）.Tumor volume in the mice administered with oxaliplatin long circulating liposomes increased rather slowly,and the mice all survived.Conclusion：Oxaliplatin long circulating liposomes seemed to have significant inhibitory effects on tumors and could reduce oxaliplatin toxicity to the immune system.

关 键 词：奥沙利铂 长循环脂质体 药效学 小鼠 

分 类 号：R979.1[医药卫生—药品] R944.9[医药卫生—药学]