荧光分光光度法检测半乳糖化白蛋白磁性阿霉素纳米粒在大鼠体内分布的研究

目的观察由半乳糖化白蛋白磁性纳米粒运载的阿霉素经舌静脉给药后在大鼠体内的的分布状况.方法全部大鼠随机分为四组,经舌静脉,按分组分别注射相应药物,剂量均为阿霉素2.5 mg/kg体重.取全血、心、肺、肝、脾、肾.全血制成血浆,器官组织制成匀浆,盐酸乙醇法提取阿霉素,用荧光光度计测量.结果静脉注射同等剂量、不同剂型的阿霉素药物后,阿霉素在器官中的蓄积程度从高到低:肝:D靶肝＞D非靶肝、C＞B＞A;心脏、肾、血浆:A＞B＞D、C;脾:B＞A、C、D;肺:B＞A＞C、D.磁性阿霉素白蛋白纳米粒注入体内后,在心、肺、肝、脾、肾中的药物浓度在15～30min达峰值,而半乳糖化后,阿霉素的药物峰值提前到5 min或之前.外加磁场和未加磁场的半乳糖化白蛋白磁性阿霉素纳米粒组的药物靶向指数和药物选择指数是均高于磁性白蛋白纳米粒.结论磁性阿霉素白蛋白纳米粒经半乳糖化后,可显著增强阿霉素对肝脏的靶向性,并显著降低心、肺、脾、肾、血浆肝外器官的组织阿霉素浓度.利用外加磁场,可提高阿霉素在肝脏特定部位蓄积的能力.因此,静脉注射半乳糖化白蛋白磁性阿霉素纳米粒是可行的.

Distribution of adriamycin contained by galactosed albumin magnetic nanoparticles in rats

Objective: to investigate distribution of adriamycin contained by galactosed albumin magnetic nanoparticles injected by lingual vein in rats. Methods: All animals were divided into four groups. The drugs were administrated into corresponding rats at a dosage of adriamycin 2.5 mg/kg body weight. Before drugs were injected intravenously. Blood samples were made into plasm, organic tissues were rinsed for homogenate. Adriamycin was picked up by hydrochlore-ethanol method, which level was measured by fluorescence photometer. Results: Adriamycin level of targeted liver tissue in D group was the highest in all groups, and not only singnificantly higher than that of untargeted in D group, but also that in A, B, C group (P<0.05); But adriamycin level was not significantly different between targeted liver tissue in D group and liver tissue in C group(P>0.05). Adriamycin level of plasm, heart, lung, kidney was not significantly different between C and D group(P>0.05), but significantly lower than that in A and B group (P<0.05). Adriamycin level of spleen in B group was the highest in all groups, but that was not significantly different in A?C and D group (P>0.05). drug targeting index and drug selective index in C and D group were those in A and B group. Conclusions: After adriamycin contained by galactosed albumin magnetic nanoparticle was administrated intravenously, adriamycin can be targetedly deliver to liver, and adriamycin level in plasm, heart, lung, kidney, spleen was significantly lowered in extra-hepatic organ, external magnetic field can significantly increase adriamycin level in specific site of liver tissue. So it was feasible that adriamycin contained by galactosed magnetic albumin nanoparticles was administrated intravenously.