Fe_2O_3-Glu纳米颗粒在小鼠体内的代谢动力学研究

The Pharmacokinetics Study of Nanoparticles of Fe_2O_3 Coated with Glutamic Acid

[目的]探讨Fe2O3-Glu纳米颗粒在小鼠体内的代谢动力学过程。[方法]采用湿化学共沉淀法制备以59Fe为示踪剂的Fe2O3-Glu纳米颗粒,将5.12mg/kg体重的Fe2O3-Glu纳米颗粒注入小鼠尾静脉,然后在不同时间采取眼眶后静脉丛血,用放射性核素示踪法检测其在体内的组织分布及代谢动力学过程。[结果]静脉注射后,小鼠体内血药浓度时间曲线为双室模型,方程式为C=29.09e-4.29t+1.13e-0.009673t,T1/2,α=0.16h,T1/2,β=71.65h。Fe2O3-Glu纳米颗粒在各主要器官中均有分布,以肝脏、脾脏中分布最多。其中,1h时肝脏中放射性百分比为48.93%(ID/g),占整体放射性的80.60%。Fe2O3-Glu纳米颗粒在不同组织脏器中达到浓度高峰的时间不同。[结论]Fe2O3-Glu纳米颗粒的体内过程符合双室模型;Fe2O3-Glu纳米颗粒能通过血脑屏障、血睾屏障和血眼屏障;肝脏、脾脏可能为其在体内作用的靶器官。

[ Objective ] To explore the pharmacokinetics of nanoparticles of Fe2O3 coated with glutamic acid （ nano-Fe2O3- Glu ）. [ Methods ] ^59Fe was used as a tracer to investigate the pharmacokinetics of nano-Fe2O3-Glu given via tail vein in mice. [ Results ] The time-concentration curve of nano-Fe2O3-Glu was fit mainly to a two-compartment model in mice. The equation was C=29.09e^-429t＋1.13e^0.009673t, T1/2α=0.16 h, T1/2β=71.65 h. Nano-Fe2O3-Glu was found to be distributed widely in various organs in vivo, and the concentration in liver and spleen was higher than that in other organs, cpm/cpm in liver was 48.93%（ ID/g ） at one hour after injection, the cpm0 in liver was 80.60% of total cpm in mice. Moreover, the time of peak concentration in various organs was different. [ Conclusion ] The characteristics of pharmacokinetics are accordant to a two-compartment model. NanoFe2O3-Glu can permeate the blood barriers of brain, eyes and genitals, and its target organs may be liver and spleen.