HPLC研究以白蛋白微球为载体的氟尿嘧啶鼠体内分布

Study on the distribution of fluorouracil delivered via albumin microsp heres in mice by HPLC

目的 研究以白蛋白微球为载体的氟尿嘧啶鼠体内分布。方法 氟尿嘧啶包封于白蛋白微球 ,并经小鼠尾静脉给药后 ,采用HPLC离子抑制技术 ,测定氟尿嘧啶在小鼠血浆、心、肝、肺、肾、脾、脑中的浓度。结果 以白蛋白微球为载体 ,氟尿嘧啶可主要分布于肝 ,给药 1 5min ,肝中聚集达最大 ,为给药剂量的 67.1 5 % ,小鼠单核巨噬系统经空白微球饱和后 ,肝中分布显著减少 (P <0 .0 1 )。结论 氟尿嘧啶包封于白蛋白微球后可实现肝脏被动靶向 ,所建HPLC用于氟尿嘧啶体内分布研究结果良好。

OBJECTIVE: To study the distribution of fluorouracil delivered via albumin microspheres in mice. METHOD: After intravenous injection in mice, the concentrations of 5-fluorouracil in mice plasma, heart, liver, lung, kidney, spleen and brain were determined respectively by HPLC. RESULTS: The distribution of 5-fluorouracil in liver was significantly higher than that in any other organs. At 15 min, the uptake of liver reached a maximum, about 67.15% of the dose. While pretreatment with nonentrapped microspheres, the accumulation of 5-fluorouracil in liver was decreased (P<0.01). CONCLUSION: 5-fluorouracil bounded to albumin microspheres showed passive targeting no liver. The established HPLC method can be used for 5-fluorouracil biodistribution study.