水飞蓟宾脂质纳米粒的制备与鼠体内分布研究

Study on the preparation and bio-distribution of silybin lipid nanospheres

目的:探索水飞蓟宾脂质纳米粒的制备工艺,同时考察其形态、大小及鼠体内分布。方法:采用薄膜乳化高压均质技术制备的水飞蓟宾脂质纳米粒,高效液相色谱法测定小鼠灌胃给药后血及肝、脾、肺、肾、脑、心、胃中的水飞蓟宾。结果:水飞蓟宾脂质纳米粒扫描电镜多呈圆形,光子相关光谱测得其平均粒径为148.9 nm,多分散性指数为0.17,体内分布研究结果表明,与市售制剂相比,脂质纳米粒可显著减少水飞蓟宾在胃中的滞留,增加其在血及肝中的分布,肝靶向指数为1.81。结论:本法所制脂质纳米粒口服给药后可增加水飞蓟宾的肝位蓄积,无疑有助于肝炎的临床治疗。

Objective： To prepare silybin lipid nanospheres（SLN） and to evaluate the properties of morphology, particle size and the silybin distribution in mice. Method： Silybin lipid nanospheres were prepared by thin film emulsion-high pressure homogenization technique. Concentrations of silybin in mice blood, liver, spleen, lung, kidney, brain, heart, stomach after oral administration were determined by high performance liquid chromatography. Result： Scanning electron mierograph showed that most of the SLN were spherical. The average diameter from photon correlation spectrometer was 148.9 nm with the polydispersity 0.17. Body distribution data indicated that SLN could increase the distribution of silybin in blood and liver, decrease the amount of silybin in stomach as compared with the preparation on market, and the drug targeting index （DTI） in liver was 1.81. Conclusion： SLN can increase the uptake of silybin in liver after oral administration, which must benefit the hepatitis treatment.