骆驼蓬生物碱壳聚糖纳米粒在小鼠体内的组织分布

Preparation of Peganum. Harmala Alkaloids Chitosan Nanoparticle and Tissue Distribution of It in Mice

目的：研究骆驼蓬生物碱壳聚糖纳米粒在小鼠体内的组织分布情况。方法：采用离子交联法制备骆驼蓬生物碱壳聚糖纳米粒。80只KM小鼠随机均分为溶液（骆驼蓬生物碱壳聚糖溶液,10 mg/kg）组与纳米粒（骆驼蓬生物碱壳聚糖纳米粒,10 mg/kg）组,尾静脉注射给药,于给药0.083、0.17、0.5、1、1.5、2、4、8 h时取样,以高效液相色谱法测定小鼠不同时间脑、心、肝、脾、肺、肾的药物质量浓度,并计算制剂的靶向性参数。结果：制备的骆驼蓬生物碱壳聚糖纳米粒粒度分布范围为63-231 nm,纳米粒外观形态饱满、表面光滑、分散性良好,无粘连现象。小鼠脑的相对摄取率为2.46,脑组织峰浓度比值为2.38;靶向效应最大值为2.845,靶向效应最小值为1.337。结论：骆驼蓬生物碱壳聚糖纳米粒在小鼠体内具有较明显脑靶向性。

OBJECTIVE：To study tissue distribution of P. Harmala alkaloids chitosan nanoparticle in mice. METHODS：The P. Harmala alkaloids chitosan nanoparticle was prepared by ionic crosslinking method. 80 KM mice were randomly divided into solution group（P. harmala alkaloids,10 mg/kg） and nanoparticle group（P. harmala alkaloids chitosan nanoparticle,10 mg/kg）.They were given medicines via caudal vein. The samples were collected 0.083,0.17,0.5,1,1.5,2,4 and 8 h after medication.HPLC method was performed to determine the concentrations of drug in brain,heart,liver,spleen,lung and kidney. The target parameters of drug were calculated. RESULTS：The particle size of P. harmala alkaloids chitosan nanoparticle were 63-231 nm,and the nanoparticle was full in shape,smooth in appearance and good in dispersity without adhesions. The relative uptake rate of P.Harmala alkaloids chitosan nanoparticle was 2.46 in brain of mice;maximum value of target response was 2.845 and the minimum value was 1.337. The peak value ratio of drug concentration was 2.38 in brain. The indicators of other organs were in low level.CONCLUSIONS：P. Harmala alkaloids chitosan nanoparticle has obvious brain target effect in mice.