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Pluronic F127-modified liposome-containing tacrolimus-cyclodextrin inclusion complexes: Improved solubility, cellular uptake and intestinal penetration
Zhu Q.1; Guo T.1; Xia D.1; Li X.1; Zhu C.1; Li H.1; Ouyang D.2; Zhang J.1; Gan Y.1
2013-08-01
Source PublicationJournal of Pharmacy and Pharmacology
ISSN00223573 20427158
Volume65Issue:8Pages:1107-1117
Abstract

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 of tacrolimus (FK 506) in the gastrointestinal (GI) tract. Methods Molecular modelling was performed to screen the optimal CD for the solubilization of FK 506. FLIC was prepared by thin-lipid film hydration with the inclusion complex solutions followed by membrane extrusion. Dilution tests were conducted in simulated gastric fluids and phosphate-buffered solution of sodium taurocholate to investigate the solubility improvement of FK506. The cellular uptake of nanocarriers was studied in Caco-2 cells, and intestinal mucous membrane penetration in the GI tract was evaluated in Sprague-Dawley rats. Key findings The results showed that β-CD had the strongest binding energy with the guest molecule among the CDs. The prepared FLIC has an average diameter of 180.8 ± 8.1 nm with a spherical shape. The solubility and cellular uptake of FK 506 was greatly improved by the incorporation of CD complexes in the Pluronic F127-modified liposomes. Intestinal mucous membrane penetration was also significantly improved by the preparation of FLIC. Conclusion With improved drug solubility and intestinal mucous membrane penetration, FLIC shows a promising oral delivery system for FK 506. © 2013 Royal Pharmaceutical Society.

KeywordCellular Uptake Cyclodextrin Inclusion Complex Molecular Modelling Pluronic F127-modified Liposomes Solubility Tacrolimus
DOI10.1111/jphp.12074
URLView the original
Indexed BySCI
Language英语
WOS Research AreaPharmacology & Pharmacy
WOS SubjectPharmacology & Pharmacy
WOS IDWOS:000321504500002
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Cited Times [WOS]:22   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Affiliation1.Shanghai Institute of Materia Medica, Chinese Academy of Sciences
2.Aston University
Recommended Citation
GB/T 7714
Zhu Q.,Guo T.,Xia D.,et al. Pluronic F127-modified liposome-containing tacrolimus-cyclodextrin inclusion complexes: Improved solubility, cellular uptake and intestinal penetration[J]. Journal of Pharmacy and Pharmacology,2013,65(8):1107-1117.
APA Zhu Q..,Guo T..,Xia D..,Li X..,Zhu C..,...&Gan Y..(2013).Pluronic F127-modified liposome-containing tacrolimus-cyclodextrin inclusion complexes: Improved solubility, cellular uptake and intestinal penetration.Journal of Pharmacy and Pharmacology,65(8),1107-1117.
MLA Zhu Q.,et al."Pluronic F127-modified liposome-containing tacrolimus-cyclodextrin inclusion complexes: Improved solubility, cellular uptake and intestinal penetration".Journal of Pharmacy and Pharmacology 65.8(2013):1107-1117.
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