Pluronic F127-modified liposome-containing tacrolimus-cyclodextrin inclusion complexes: improved solubility, cellular uptake and intestinal penetration
文献类型：期刊论文
| 作者 | Zhu, Quanlei1; Guo, Tao1; Xia, Dengning1; Li, Xiuying1; Zhu, Chunliu1 ; Li, Haiyan1; Ouyang, Defang2; Zhang, Jiwen1; Gan, Yong1
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| 刊名 | JOURNAL OF PHARMACY AND PHARMACOLOGY
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| 出版日期 | 2013-08 |
| 卷号 | 65期号:8页码:1107-1117 |
| 关键词 | cellular uptake cyclodextrin inclusion complex molecular modelling Pluronic F127-modified liposomes solubility tacrolimus |
| ISSN号 | 0022-3573 |
| DOI | 10.1111/jphp.12074 |
| 文献子类 | Article |
| 英文摘要 | 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 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 beta-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. |
| WOS关键词 | ENHANCED ORAL BIOAVAILABILITY ; IN-VITRO CHARACTERIZATION ; DRUG-DELIVERY SYSTEMS ; PHARMACEUTICAL APPLICATIONS ; BILE-SALT ; ABSORPTION ; PHARMACOKINETICS ; NANOPARTICLES ; ENCAPSULATION ; ITRACONAZOLE |
| 资助项目 | National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program"[2012ZX09301001-001] ; National Basic Research Program of China[2009CB930300] ; National Natural Science Foundation of China[81102389] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000321504500002 |
| 出版者 | WILEY-BLACKWELL |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277528]  |
| 专题 | 药物制剂研究中心 |
| 通讯作者 | Gan, Yong |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; 2.Aston Univ, Sch Life & Hlth Sci, Birmingham B4 7ET, W Midlands, England |
| 推荐引用方式 GB/T 7714 | Zhu, Quanlei,Guo, Tao,Xia, Dengning,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, Quanlei.,Guo, Tao.,Xia, Dengning.,Li, Xiuying.,Zhu, Chunliu.,...&Gan, Yong.(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, Quanlei,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. |
入库方式： OAI收割
来源：上海药物研究所
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