维甲酸脂质体在小鼠体内的药物动力学及组织分布

目的考察2种全反式维甲酸(ATRA)脂质体静脉给药后在小鼠体内的药物动力学和组织分布。方法分别采用不饱和豆磷脂(SPC),以及SPC与聚乙二醇-磷脂酰乙醇胺(PEG-PE)以一定比例混合的混合物为膜材,利用乙醇注入法制备全反式维甲酸普通脂质体和长循环脂质体,静脉注射后采用HPLC法测定小鼠血浆及各组织中的药物浓度。结果普通脂质体和长循环脂质体的AUC分别是以游离药物给药组的2.58倍和5.00倍,t1/2分别由2.66 h延长至3.74 h和6.39 h,脂质体在肝中分布显著增加。结论2种ATRA脂质体能够延缓药物释放,增强药物靶向性。

Pharmacokinetics and tissue distribution study of ATRA liposome in mice

Objective To evaluate the pharmacokinetics and tissue distribution of ATRA in mice after intravenous administration of the two ATRA liposomes.Methods ATRA liposomes formulated with either unsaturated SPC or SPC and PEG-PE mixture were prepared using ethanol injection method.The plasma concentration and tissue distribution of the drug was determined by HPLC.Results The AUC of ATRA liposome(ATRA-L) and long circle liposome(ATRA-PEGL)were 2.58-fold and 5.00-fold higher than that of the ATRA solution.the t1/2 of ATRA-L and ATRA-PEGL were 3.74 h and 6.39 h,the liver distribution of ATRA-L were remarkably increased compared that of 2.66 h for ATRA solution.Conclusions The two ATRA liposomes exhibit a longer circulation time and better tissue targeting.