半乳糖白蛋白磁性阿霉素纳米粒在正常大鼠体内的靶向性分布的研究

Study on targeting distribution of Gal-HSA magnetic nanoparticles containing adriamycin in normal rats

目的 观察半乳糖白蛋白磁性阿霉素纳米粒(Gal-MADM)在正常肝脏中的靶向性,并观察Gal-MADM在全身各脏器的分布特征。方法 使用放射示踪技术,用125I标记纳米粒。肝动脉注射,分别于注药后5、15、30、60、120min处死,立即取肝、肾、心、肺、小肠、脾、及周围血作γ计数。用同样的方法进行白蛋白磁性阿霉素纳米粒(MADM)在大鼠体内分布实验。结果 Gal-MADM和MADM肝摄取分别在注射后5 min后最高,分别为15 054.4 CPM／g和6 186.7 CPM／g,各时相前者的肝摄取率均为同时刻后者的2-3倍。在肝、肾、心、肺、小肠、脾、及周围血的分布两药差异有高度显著性(P<0.05)。结论Gal-MADM在正常肝组织中有明显的主动靶向性,Gal-MADM主要分布肝脏,其它的脏器含量少。

Objective To observe the hepatic targeting of Gal-HSA magnetic nanoparticles containing adriamycin and its effect of magnetic field application on targeting distribution in vivo. Methods Abdominal exposure was carried out through a midline abdominal incision. A cannula was inserted into the hepatic artery. Using radioactive tracer technique, Gal-HSA magnetic nanoparticles containing adriamycin and human serum albumin magnetic nanoparticles containing adriamycin were labelled with 125I.125I Gal-HSA magnetic nanoparticles containing adriamycin and 125I human serum albumin magnetic nanoparticles containing adriamycin were injected into hepatic artery (equivalent dose of free adriamycin 0.5 mg/kg). At 5,15, 30, 60, 120 min after hepatic artery injection, the rats were sacrificed. The liver, kidney, heart, lung, small intestine, spleen and blood were analyzed for 125I-counts. Results Gal-HSA magnetic nanoparticles containing adriamycin and human serum albumin magnetic nanoparticles containing adriamycin reached the maximal uptake quantity in liver after 5 min (15 054.4 CPM/g and 6 186.7 CPM/ g respectively). Uptake quantity of Gal-HSA magnetic nanoparticles containing adriamycin was 2-3 times as high as that of human serum albumin magnetic nanoparticles containing adriamycin. There was remarkable difference in the distribution of the two drugs in liver, kidney, lung, spleen, heart, small intestine and blood (P < 0.05). Conclusion Gal-HSA magnetic nanoparticles containing adriamycin in normal rat liver had remarkable hepatic targeting and good magnetic targeting. Gal-HSA magnetic nanoparticles containing adriamycin injected mainly distributed in liver.