姜黄素PLGA-TPGS纳米粒在小鼠体内分布及肝靶向性研究

Body distribution and hepatic targeting of CM-PLGA-TPGS-NPs in mice

关键词:  姜黄素  纳米粒  肝靶向

Key words:  [Key words]　Curcumin  nanoparticle  liver targeting

摘要:

[摘要]　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。〖ＨＴH〗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。〖ＨＴH〗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。〖ＨＴH〗结论　CPTN对肝脏有良好的靶向作用。

Abstract:

[Abstract]　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　Intrahepatic 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 except 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.