Pluronic F127-modified liposome-containing tacrolimus-cyclodextrin inclusion complexes: improved solubility, cellular uptake and intestinal penetration

Quanlei Zhu, Tao Guo, Dengning Xia, Xiuying Li, Chunliu Zhu, Haiyan Li, Defang Ouyang, Jiwen Zhang, Yong Gan*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

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.

Original languageEnglish
Pages (from-to)1107-1117
Number of pages11
JournalJournal of Pharmacy and Pharmacology
Volume65
Issue number8
Early online date15 May 2013
DOIs
Publication statusPublished - Aug 2013

Keywords

  • cellular uptake
  • cyclodextrin inclusion complex
  • molecular modelling
  • Pluronic F127-modified liposomes
  • solubility
  • tacrolimus

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