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目的 检测阿霉素毫微粒 (NADM)经肝动脉灌注后 ,在大鼠体内的药物分布 ,并与游离阿霉素 (FADM)相比较 .方法 以 α-聚氰基丙烯酸正丁酯为载体材料 ,制备NADM;SD纯系大鼠 2 4只 ,随机分为两组 ,每组 1 2只动物 ,经肝动脉分别注入 NADM与 FADM,药物剂量 2 mg·kg- 1 ,药物浓度 1 .0 g· L- 1 .每组于给药后 1 ,5 ,1 5 h各处死 4只大鼠 ,分别提取血浆、肝、心、脾、肺、肾样品 ,以反相高效液相色谱荧光检测法 (RP- HPL C)测定药物浓度 .结果 与FADM组相比 ,1 ,5 ,1 5 h时 NADM组大鼠肝、脾中阿霉素浓度显著增高 ,而血浆、肺、肾中阿霉素浓度降低 .心脏药物浓度给药后 1 h,5 h FADM组高于 NADM组 ,1 5 h时低于NADM组 .结论 NADM肝动脉给药后改变了阿霉素的体内分布特征 ,对肝、脾表现出明显的靶向性 ,而血、心、肺、肾中的药物分布减少 .
Objective To investigate the drug distribution of doxorubicin nanoparticles (NADM) after hepatic artery perfusion in rats and compare with free doxorubicin (FADM) .Methods The α-polycyanoacrylate , NADM was prepared. 24 SD SD rats were randomly divided into two groups, 12 animals in each group. The animals were injected with NADM and FADM via hepatic artery respectively. The drug dose was 2 mg · kg-1 and the drug concentration was 1.0 g · L-1. Each group was sacrificed at 1, 5, 15 h after injection, and 4 rats were sacrificed. Samples of plasma, liver, heart, spleen, lung and kidney were collected and analyzed by reverse-phase high performance liquid chromatography (RP-HPL C) .Results Compared with FADM group, the concentrations of doxorubicin in liver and spleen of rats in NADM group were significantly increased at 1, 5 and 15 h, while those in plasma, lung and kidney The concentrations of cardiac drug were lower in the FADM group than in the NADM group at 1 h and 5 h and lower than those in the NADM group at 15 h after the administration of cardiac drug.Conclusion The distribution of doxorubicin in vivo changes after hepatic artery administration of NADM, Spleen showed significant targeting, and blood, heart, lung, kidney drug distribution decreased.