去甲斑蝥素壳聚糖纳米粒在小鼠体内分布及肝靶向作用

目的:研究去甲斑蝥素壳聚糖纳米粒(NCD-NP)在小鼠体内的分布及肝靶向性.方法:利用离子交联法制备去甲斑蝥素壳聚糖纳米粒后,经小鼠尾静脉给药,采用HPLC法检测去甲斑蝥素在小鼠血浆、心、肝、脾、肺、肾中的浓度随时间的变化,与去甲斑蝥素溶液(NCD-SOL)组进行比较.并以靶向指数TI=(AUC)NCD-NP/(AUC)NCD-SOL来判断NCD-NP对主要器官的靶向性.结果:NCD-NP组在肝脏中组织浓度明显高于NCD-SOL组,肝、脾的靶向指数大于1,而在其他器官靶向指数小于1.结论:去甲斑蝥素纳米粒可通过网状内皮系统吞噬作用实现肝脏被动靶向,能够提高药物疗效,降低全身毒副作用.

Study on the distribution and liver targeting of norcantharidin nanoparticles in mice

OBJECTIVETo study the distribution character and liver targeting trend of norcantharidin chitosan nanoparticles(NCD-NP) in mice. METHODSNCD-NP was prepared by ionic crosslinkage. The concentrations of norcantharidin in mice plasma, heart, liver, spleen, lung and kidney were determined respectively by HPLC after intravenous injection administration of narcantharidin solution (NCD-SOL) or NCD-NP. Targetability to each organ was evaluated by targeting index (TI), which equal to (AUC)_(NCD-NP)/(AUC)_(NCD-SOL). RESULTSThe tissue concentration of norcantharidin in liver was significantly higher in NCD-NP group than in NCD-SOL group. TI showed that nanoparticles have the targeting ability to liver and spleen while have not targeting trend to the other organs. CONCLUSIONNCD-NP can be intercepted by reticoendothelial system (RES) to display passive liver targeting. So NCD-NP can improve curative effect and reduce toxicity of NCD.