吡喹酮长循环固体脂质纳米粒的制备及体内外质量评价  

Preparation and in vitro-in vivo Evaluation of Long-circulating Solid Lipid Nanoparticles Loaded with Praziquantel

作　　者：邹永华[1] 丁劲松[1] 郑志难[1] 张龙贵[2] 马宁[2] 

机构地区：[1]中南大学药学院,湖南长沙410013 [2]长沙医学院,湖南长沙410219

出　　处：《中国医药工业杂志》2012年第6期438-442,共5页Chinese Journal of Pharmaceuticals

基　　金：湖南省教育厅(09A011)重点项目

摘　　要：采用乳化-超声分散法制备了吡喹酮固体脂质纳米粒(1-SLN),并以二硬脂酰磷脂酰乙醇胺-聚乙二醇2000为材料同法制备了长循环固体脂质纳米粒(1-LCN)。考察了1-SLN和1-LCN粒径、包封率、固有水化层厚度和体外24 h累积释放率,结果分别为(95.57±1.27)和(77.79±1.01)nm、(72.7±2.7)%和(68.2±3.5)%、(1.56±0.32)和(7.03±0.39)nm,以及(77.7±3.5)%和(87.4±4.2)%。两者的体外巨噬细胞吞噬率分别为(10.21±2.85)%、(1.62±0.41)%。经家兔耳缘静脉注射后,1-LCN较1-SLN和1溶液的半衰期和AUC显著增加,提示其具有长循环效果。Praziquantel solid lipid nanoparticles（1-SLN） and its long-circulating solid lipid nanoparticles（1-LCN） with distearoyl phosphoethanolamine-polyethylene glycol 2000（DSPE-PEG 2000） as the material were prepared by emulsification-ultrasonic dispersion method.The particle size,encapsulation efficiency,fixed aqueous layer thickness and cumulative release rate at 24 h of 1-SLN and 1-LCN were（95.57±1.27） and（77.79±1.01）nm,（72.7±2.7）% and（68.2±3.5）%,（1.56±0.32） and（7.03±0.39）nm,（77.7±3.5）% and（87.4±4.2）%,respectively.The in vitro phagocytize rate of 1-SLN and 1-LCN by peritoneal macrophages were（10.21±2.85）% and（1.62±0.41）%,respectively.The pharmacokinetic behavior in rabbits of 1 solution,1-SLN and 1-LCN after？ear intravenous administration were investigated.The results showed that the half-life and AUC of 1-LCN group were significantly increased compared with the solution and SLN groups.It indicated that the nanoparticles modified with DSPE-PEG 2000 had a long-circulation property.

关 键 词：吡喹酮 长循环固体脂质纳米粒 制备 评价 吞噬率 

分 类 号：R944.9[医药卫生—药剂学]