Pluronic F127-modified liposome-containing tacrolimus-cyclodextrin inclusion complexes: improved solubility, cellular uptake and intestinal penetration
作者： Quanlei Zhu , Tao Guo , Dengning Xia , Xiuying Li , Chunliu Zhu
DOI: 10.1111/JPHP.12074
关键词: Chemistry 、 Drug 、 Liposome 、 Poloxamer 、 Solubility 、 Cyclodextrin 、 Membrane 、 Nanocarriers 、 Chromatography 、 Penetration (firestop)
摘要: Objective The aim of this study was to investigate Pluronic F127-modified liposome-containing cyclodextrin (CD) inclusion complex (FLIC) for improving the solubility, cellular uptake and intestinal penetration tacrolimus (FK 506) in gastrointestinal (GI) tract. Methods Molecular modelling performed screen optimal CD solubilization FK 506. FLIC prepared by thin-lipid film hydration with solutions followed membrane extrusion. Dilution tests were conducted simulated gastric fluids phosphate-buffered solution sodium taurocholate solubility improvement FK506. nanocarriers studied Caco-2 cells, mucous GI tract evaluated Sprague-Dawley rats. Key findings results showed that β-CD had strongest binding energy guest molecule among CDs. has an average diameter 180.8 ± 8.1 nm a spherical shape. 506 greatly improved incorporation complexes liposomes. Intestinal also significantly preparation FLIC. Conclusion With drug penetration, shows promising oral delivery system © 2013 Royal Pharmaceutical Society.
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