摘要
目的:研究毛兰素固体脂质纳米粒(erianin solid lipid nanoparticles,ER-SLN)在大鼠中的药动学行为以及在小鼠体内的组织分布。方法:制备ER-SLN,大鼠静脉注射毛兰素混悬液(free ER)及ER-SLN,小鼠静脉注射free ER及ER-SLN,HPLC法测定各组织(血浆、心、肝、脾、肺、肾、脑)中的毛兰素含量,对测得的数据应用统计学软件进行统计分析。结果:静脉注射后ER-SLN在大鼠体内的AUC_(0-t)、MRT_(0-t)、t_(1/2)分别是free ER组的2.14,1.85,1.46倍;组织分布学考察表明ER-SLN在肝脏中的相对摄取率(Re)最高(1.37),同时ER-SLN在各组织中的靶向效率(Te)均大于1,对肝脏的选择性明显强于free ER。结论:毛兰素制备成纳米粒后能明显延长药物在大鼠体内的平均驻留时间(MRT),增大AUC和C_(max)值,提高生物利用度,同时在小鼠肝脏中能有效富集,减慢在肝脏中的清除速率,具有较明显的肝被动靶向性。
OBJECTIVE To investigate the pharmacokinetic behavior in rats and tissue distribution in mice of solid lipid nanoparticles of erianin(ER-SLN).METHODS ER-SLN was prepared,erianin suspension(free ER)and ER-SLN were injected into rats intravenously,and also into mice intravenously.With HPLC method,ER contents in various tissues(blood plasma,heart,liver,spleen,lung,kidney,brain)were determined,and the obtained data were analyzed statistically with statistic software.RESULTS After intravenous injection,AUC0-t,MRT0-t and MRT t1/2 of ER-SLN were 2.14,1.85 and 1.46 times that of free ER.The study on tissue distribution showed that the relative extraction rate(Re)of the ER-SLN in the liver was the highest(1.37).At the same time,the target efficiency(Te)of ER-SLN in each tissue was greater than 1,and the selectivity of ER-SLN for the liver was significantly stronger than that of the free erianin.CONCLUSION Erianin preparation of SLN can significantly prolong its mean retention time(MRT)in rats,increase the AUC0-t and Cmax values,and improve its bioavailability.Meanwhile,it can accumulate in the liver of mice effectively,retard its clearance rate in the liver,and so has significant passive target for the liver.
作者
张艺雯
陈相旭
徐文强
宋宗辉
王玲洁
于波涛
ZHANG Yi-wen;CHEN Xiang-xu;XU Wen-qiang;SONG Zong-hui;WANG Ling-jie;YU Bo-tao(Department of Pharmacy,The General Hospital of Western Theater Command,Sichuan Chengdu 610083,China;College of Medicine,Southwest Jiaotong University,Sichuan Chengdu 610031,China)
出处
《中国医院药学杂志》
CAS
北大核心
2019年第10期1042-1045,共4页
Chinese Journal of Hospital Pharmacy
基金
成都药学会赞邦药学科研基金(编号:201704)
关键词
毛兰素
固体脂质
纳米粒
药动学
组织分布学
erianin
solid lipid
nanoparticles
pharmacokinetics
tissue distribution