摘要
采用逆相蒸发-挤出法制备奥沙利铂聚乙二醇(PEG)修饰脂质体,处方中蛋黄卵磷脂E80-胆固醇-聚乙二醇修饰二硬脂酰磷脂酰乙醇胺(PEG 2000-DSPE)重量比为100∶25∶34,药脂比为1∶10。所得制品平均粒径为140 nm,包封率97.5%。采用HPLC法测定大鼠血浆中的奥沙利铂,考察奥沙利铂PEG修饰脂质体静注给予大鼠的药动学情况,并与奥沙利铂溶液相比较。结果显示,奥沙利铂PEG修饰脂质体组的cmax和AUC均显著大于溶液组(P<0.05);平均滞留时间(MRT)比溶液组延长了约20倍。说明奥沙利铂PEG修饰脂质体能延长药物在大鼠体内的循环时间。
Oxaliplatin PEGylated liposomes were prepared by reverse phase evaporation-extrusion method. The liposomal membranes consisted of egg yolk lecithin E80, cholesterin and polyethylene glycol 2000-distearoylphosphatidylethanolamine (PEG 2000-DSPE) with weight ratio of 100 : 25 : 34. And drug-to-lipid ratio was 1 : 10. The average particle size of the product was about 140 nm with the encapsulation efficiency of 97.5 %. The concentration of oxaliplatin in rat plasma was determined by HPLC. The pharmacokinetics of oxaliplatin PEGylated liposomes in rats after iv administration was investigated with oxaliplatin solution as the control. The results showed that the c and A UC of the liposomes group were significantly higher than those of the solution group (P〈0.05). Compared with the solution group, the mean residence time (MRT) of liposomes group was increased by about 20 times. It indicated that the oxaliplatin PEGylated liposomes could prolong the circulation time in rats.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2012年第11期913-916,926,共5页
Chinese Journal of Pharmaceuticals
基金
2010年度上海市科技启明星(B类)(10QB1404100)
2009年上海市自然科学基金项目(09ZR1430900)