熊果酸磷脂纳米注射剂在小鼠体内的分布研究

Study on the Distribution of Ursolic Acid Phospholipid Nanoparticle Injection in Mice

目的:考察熊果酸磷脂纳米(UA-PL-NP)注射剂在小鼠体内的组织分布。方法:取昆明小鼠尾静脉注射UA-PL-NP后,分别于给药后5min、1h和4h收集血浆和各组织,采用反相高效液相(RP-HPLC)法检测各组织中熊果酸(UA)药物浓度。结果:(1)UA-PL-NP给药后UA主要分布于肝和胃肠组织(。2)主要分布组织的药物浓度呈现随给药剂量增加而线性增加的趋势(。3)胃、肠组织药物浓度于停药后迅速下降,至停药4h后浓度下降至极低水平;而肝组织药物浓度于停药后不断升高,停药后4h仍维持较高浓度([52.15±18.61)mg·kg-1]。结论:UA-PL-NP给药初期迅速分布于肝、胃、肠等组织,停药后胃肠组织药物释放入血后经再分布达平衡,使UA较长时间高度浓聚于肝组织,具有肝靶向分布特征。

Objective： To investigate the distribution of Ursolic Acid Phospholipid Nanoparticles （UA-PL-NP） in mice. Methods： Kunming mice were injected UA-PL-NA through caudal veins, and the plasma and the main tissues of these mice were collected at 5 min, 1 h and 4 h after injection, respectively. RP-HPLC method was used to determine the concentrations of UA in the plasma and the main tissues. Results： （1） UA mainly distributed in liver and gastrointestinal tissues. （2） A linear increase was noted with increasing concentrations of UA in the main tissues. （3） UA concentration decreased rapidly in gastrointestinal tissue, and only an extremely low concentration was remained at 4 h after injection. UA concentration in liver increased constantly after injection, and even at 4 h after injection, it maintained a high level [（52.15±18.61） mg· kg^-1]. Conclusion： UA-PL-NP distributes quickly in liver and gastrointestinal tissues on the early stage of injection. After administration, UA concentration in gastrointestinal tissues releases into blood and the redistribution reaches balance. In this way, a highconcentration of UA maintains in liver tissue. UA-PL-NP has a good hepatic targeting distribution characteristic in mice.