Effect of cell-penetrating peptide-coated nanostructured lipid carriers on the oral absorption of tripterine
作者： Ling Yuan , Zhen-hai Zhang , Cao Wei , Lei Zhou , Qingqing Wu
DOI: 10.2147/IJN.S34991
关键词: Jejunum 、 Bioavailability 、 Controlled release 、 Cytotoxicity 、 Materials science 、 MTT assay 、 Pharmacology 、 Zeta potential 、 Dialysis tubing 、 Pharmacokinetics
摘要: PURPOSE To develop nanostructured-lipid carriers (NLCs) coated with cell-penetrating peptides (CPP) for improving the oral bioavailability of tripterine. METHODS We prepared CPP-coated tripterine-loaded NLCs (CT-NLCs) by using a solvent evaporation method, and determined their physical properties. In vitro drug release was dialysis bag diffusion technique, intestinal toxicity evaluated performing MTT assay Caco-2 cells. vivo absorption studied in an situ rat perfusion model, examined beagles. RESULTS The average particle size, zeta potential, encapsulation efficiency optimized CT-NLCs were 126.7 ± 9.2 nm, 28.7 3.4 mV, 72.64% 1.37%, respectively. showed controlled profile had significantly lower cytotoxicity than tripterine solution (P < 0.05). levels from duodenum jejunum markedly higher without CPP coating (T-NLCs), solution. Pharmacokinetic study that maximum concentration greater T-NLCs suspension, time to as well T-NLCs, longer suspension. relative compared suspension 484.75% 149.91% CONCLUSION is dramatically increased CT-NLCs. Therefore, seem be promising carrier delivery
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