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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。
The praziquantel solid lipid nanoparticles (1-SLN) were prepared by emulsification-ultrasonic dispersion method and the long-circulating solid lipid nanoparticles were prepared by the same method with distearoylphosphatidylethanolamine-polyethylene glycol 2000 (1-LCN). The particle size, entrapment efficiency, thickness of intrinsic hydration layer and the cumulative release rate of 24 h in vitro were investigated. The results were (95.57 ± 1.27) and (77.79 ± 1.01) nm, (72.7 ± 2.7) nm, % And (68.2 ± 3.5)%, (1.56 ± 0.32) and (7.03 ± 0.39) nm, and (77.7 ± 3.5)% and (87.4 ± 4.2)%, respectively. The phagocytosis rates of macrophages in vitro were (10.21 ± 2.85)% and (1.62 ± 0.41)%, respectively. The half-life and AUC of 1-LCN compared with 1-SLN and 1 solution significantly increased after rabbits ear vein injection, suggesting that they have a long circulation effect.