シクロデキストリン論文データベース検索システム

論文名	Pluronic F127-modified liposome-containing tacrolimus-cyclodextrin inclusion complexes: improved solubility, cellular uptake and intestinal penetration.
著者	Quanlei Zhu Tao Guo Dengning Xia Xiuying Li Chunliu Zhu Haiyan Li Defang Ouyang Jiwen Zhang Yong Gan
キーワード
出版年月	1970年1月
発表先	J Pharm Pharmacol. 2013 Aug;65(8):1107-17.
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論文概要（和文）	プルロニックF127修飾リポソーム含有タクロリムス-シクロデキストリン包接複合体：溶解性、細胞取り込みおよび腸管浸透の改善。
論文概要（英文）	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.