目的：研究姜黄素PLGA－TPGS纳米粒（ Curcumin－loaded PLGA－TPGS Nanoparticles，CPTN）在小鼠体内的分布及对肝脏的靶向性。方法经小鼠尾静脉注射CPTN和姜黄素溶液（ Curcumin solutions，CS），采用反相高效液相色谱法测定不同时间时姜黄素在小鼠血浆、肝、心、脾、肺、肾中的浓度。用靶向指数（ targeting index，TI）、选择性指数（selective index，SI）、相对靶向效率（relative targeting efficiency，Re）和靶向效率（targeting efficiency，Te）4个指标全面评价CPTN对肝脏的靶向性。结果 CPTN组1、2、4 h时肝内药物浓度远高于血浆、脾、肺（P＜0．05）和心、肾（P＜0．01），药物持续作用时间明显长于CS组；TI和SI值均＞1（SI在0．08 h和0．5 h除外），CPTN在肝中的AUC是CS在肝中AUC的31．6倍，且CPTN组的Te值均＞3。结论 CPTN对肝脏有良好的靶向作用。%Objective To study the distribution of Curcumin-loaded polylactic-co-glycolic acid-D-α-tocopherol polyethylene glycol 1000 succinate nanoparticles ( CPTN) and the liver targeting in mice.Methods The mice were given CPTN and Curcumin solutions ( CS) by tail vein injection.The concentration changes of Curcumin in plasma,liver,heart, spleen,lung,kidney of mice were determined at different time by reverse phase-high performance liquid chromatography ( RP-HPLC) ,and evaluated using TI,SI,Re and Te four index to evaluate the hepatic targeting of CPTN.Results Intrahe-patic drug concentration of CPTN at 1, 2, 4 h was higher than that of plasma, spleen, lung (P<0.05) and heart, kidney ( P<0.01) respectively, and longer drug duration than CS.TI and SI were both greater than 1 at the different intervals ex-cept for SI at 0.08 h and 0.5 h.Re of CPTN in liver was 31.6 folds than that of CS in liver, and Te of CPTN group>3. Conclusion CPTN has good targeting property in vivo for the liver.
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