Preparation and passive target of 5-fluorouracil solid lipid nanoparticles.
作者： Bin Du , Ying Yan , Ying Li , ShuYu Wang , ZhenZhong Zhang
DOI: 10.3109/10837450903246390
关键词: Solid lipid nanoparticle 、 In vivo 、 Half-life 、 Chromatography 、 High-performance liquid chromatography 、 Zeta potential 、 Pharmacokinetics 、 Distribution (pharmacology) 、 Drug 、 Chemistry
摘要: This work studied the intravenous injection formulation of solid lipid nanoparticles (SLNs) loaded with 5-fluorouracil (5-FU). The goal was to design longer drug residence in vivo and passive targeting which could improve therapeutic efficacy reduce side-effects. Based on optimized results uniform experiment, 5-FU-SLNs were prepared by multiple emulsion-ultrasonication (w/o/w). SLNs found be relatively size (182.1 +/- 25.8 nm) a negative zeta potential (-27.89 5.1 mV). average entrapment efficiency loading 74% 10%, respectively. Compared 5-FU solution (t(1/2beta), 0.593h; MRT, 0.358h) after rats, pharmacokinetic parameters exhibited retention time. 4.0628h; 3.5321h). area under curve plasma concentration-time (AUC) 1.48 times greater than that free drugs. overall (TE(C)) enhanced from 13.25-20.45% lung 11.48-23.16% kidney while spleen distribution significantly reduced as compared solution. These indicated promising agents for curing primary carcinoma.
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