Related Experiment Video
Updated: May 9, 2026

Encapsulation of Cancer Therapeutic Agent Dacarbazine Using Nanostructured Lipid Carrier
Published on: April 26, 2016
Pluronic F127-modified liposome-containing tacrolimus-cyclodextrin inclusion complexes: improved solubility, cellular
Quanlei Zhu1, Tao Guo, Dengning Xia
1Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China.
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.
Related Concept Videos
Bioavailability Enhancement: Drug Permeability Enhancement
Bioavailability Enhancement: Drug Stability Enhancement and GI Retention
Site-Targeted Drug Delivery Systems: Polymeric Carriers
Bioavailability Enhancement: Drug Solubility Enhancement
Modified-Release Drug Delivery Systems: Site-Targeted
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

