Supersaturated polymeric micelles for oral cyclosporine A delivery
文献类型：期刊论文
| 作者 | Yu, Hongzhen; Xia, Dengning; Zhu, Quanlei; Zhu, Chunliu ; Chen, Dan; Gan, Yong
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| 刊名 | EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
 |
| 出版日期 | 2013-11 |
| 卷号 | 85期号:3页码:1325-1336 |
| 关键词 | Supersaturated polymeric micelle Cyclosporine A Soluplus (R) Supersaturation degree Oral bioavailability Cellular uptake and transport |
| ISSN号 | 0939-6411 |
| DOI | 10.1016/j.ejpb.2013.08.003 |
| 文献子类 | Article |
| 英文摘要 | Polymeric micelles provide a promising platform for improving oral absorption of poorly soluble drugs. However., improved understanding of how drug retention within the hydrophobic micelle core can reduce drug absorption is required. We designed supersaturated polymeric micelles (Super-PMs) to increase molecularly dissolved drug concentration and gain an insight into the effect of the degree of supersaturation on oral absorption of cyclosporine A (CsA) in rats. The drug release from Super-PMs increased with an increase in initial supersaturation degrees in micelles. The cellular uptake of coumarin-6 was reduced by the retention of drug in polymer micelles. The transport flux of CsA across Caco-2 monolayer was increased with initial supersaturation degrees of 0.81-3.53 (p < 0.05). However, increase in supersaturation to 5.64 actually resulted in decreased CsA transport. The same trend was observed in a rat in vivo absorption study, in which the highest bioavailability of 134.6 +/- 24.7% (relative to a commercial product, Sandimmun Neoral (R), p < 0.01) was achieved when the supersaturation degree was 3.53. These results demonstrated that Super-PMs were a promising drug delivery system for compounds with low aqueous solubility. This study also provided an experimental proof for the hypothesis that moderately supersaturated formulations are valuable alternative to high supersaturation formulations, resulting in optimal in vivo performance, and the degree of supersaturation should be carefully controlled to optimize drug absorption. Crown Copyright (C) 2013 Published by Elsevier B.V. All rights reserved. |
| WOS关键词 | BLOCK-COPOLYMER MICELLES ; WATER-SOLUBLE DRUGS ; CACO-2 CELL MONOLAYERS ; IN-VIVO PERFORMANCE ; SOLID DISPERSION ; ADMINISTERED PACLITAXEL ; MULTIDRUG-RESISTANCE ; CREMOPHOR-EL ; VITRO ; BIOAVAILABILITY |
| 资助项目 | National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program"[2012ZX09301001-001] ; Novo Nordisk-Chinese Academy of Science Research Foundation[NNCAS-2009-10] ; National Basic Research Program of China[2009CB930300] ; National Natural Science Foundation of China[81202468] ; China Postdoctoral Science Foundation[2013M530219] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000330200800058 |
| 出版者 | ELSEVIER SCIENCE BV |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277386]  |
| 专题 | 药物制剂研究中心 |
| 通讯作者 | Gan, Yong |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yu, Hongzhen,Xia, Dengning,Zhu, Quanlei,et al. Supersaturated polymeric micelles for oral cyclosporine A delivery[J]. EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS,2013,85(3):1325-1336. |
| APA | Yu, Hongzhen,Xia, Dengning,Zhu, Quanlei,Zhu, Chunliu,Chen, Dan,&Gan, Yong.(2013).Supersaturated polymeric micelles for oral cyclosporine A delivery.EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS,85(3),1325-1336. |
| MLA | Yu, Hongzhen,et al."Supersaturated polymeric micelles for oral cyclosporine A delivery".EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS 85.3(2013):1325-1336. |
入库方式： OAI收割
来源：上海药物研究所
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