Enhanced digestion inhibition and mucus penetration of F127-modified self-nanoemulsions for improved oral delivery
文献类型：期刊论文
| 作者 | Song, Wenyi2,3; Yang, Yuting2,3; Yu, Miaorong3; Zhu, Quanlei1,3; Damaneh, Mohammadali Soleimani1,4; Zhong, Haijun2; Gan, Yong1,3
|
| 刊名 | ASIAN JOURNAL OF PHARMACEUTICAL SCIENCES
 |
| 出版日期 | 2018-07 |
| 卷号 | 13期号:4页码:326-335 |
| 关键词 | Self-nanoemulsifying system (SNEs) Oral absorption Enzymatic degradation Mucus penetration Pluronic (R) F127 |
| ISSN号 | 1818-0876 |
| DOI | 10.1016/j.ajps.2018.03.001 |
| 文献子类 | Article |
| 英文摘要 | Self-nanoemulsifying systems (SNEs) have excellent ability to improve the solubility of poorly water-soluble drugs (PWSD). However, SNEs are likely to be degraded in gastrointestinal (GIT) when their surface is recognized by lipase/co-lipase enzyme complex, resulting in rapid release and precipitation of encapsulated drugs. The precipitates are then captured and removed by intestinal mucus, reducing the delivery efficacy of SNEs. Herein, the amphiphilic polymer Pluronic (R) F127 was incorporated into long and short-chain triglycerides (LCT, SCT) based SNEs to diminish the recognition and therefore minimized their degradation by enzymes and clearance by mucus. The SNEs were characterized in terms of particle size, zeta potential and stability. Ex vivo multiple particles tracking studies were performed by adding particle solution into fresh rat mucus. Cellular uptake of SNEs were conducted by using E12 cells, the absorption and distribution in small intestine were also studied after oral administration in male Sprague-Dawley (SD) rats. The in vitro digestion rate of SNEs were found to be in following order SCT-SNE > SCT-F127-SNE > LCT-SNE > LCT-F127-SNE. Moreover, the LCT-F127-SNE was found to be most effective in enhancing cellular uptake, resulting in 3.5-fold, 2.1-fold and 1.7-fold higher than that of SCT-SNE, LCT-SNE and SCT-F127-SNE, respectively. After incubating the SNE with E12 cells, the LCT-F127-SNE exhibited the highest amount regarding both mucus penetration and cellular uptake, with an uptake amount number (via bicinchoninic acid (BCA) analysis) of 3.5-fold, 2.1-fold and 1.7fold higher than that of SCT-SNE, LCT-SNE and SCT-F127-SNE, respectively. The in vivo results revealed that orally administered LCT-F127-SNE could significantly increase the bioavailability of Cyclosporine A (CsA), which was approximately 2.43-fold, 1.33-fold and 1.80-fold higher than that of SCT-SNE, SCT-F127-SNE and LCT-SNE, respectively. We address in this work that F127-modified SNEs have potentials to improve oral drug absorption by significantly reducing gastrointestinal enzymatic degradation and simultaneously enhancing mucus penetration. (c) 2018 Shenyang Pharmaceutical University. Published by Elsevier B.V. This is an open access article under the CC BY-NC-ND license. (http://creativecommons.org/licenses/by-nc-nd/4.0/) |
| WOS关键词 | LIPID-BASED FORMULATIONS ; MULTIPLE-PARTICLE TRACKING ; IN-VITRO ; ABSORPTION BARRIER ; DIFFUSION BARRIER ; CYCLOSPORINE-A ; MEDIUM-CHAIN ; NANOPARTICLES ; DRUG ; BIOAVAILABILITY |
| 资助项目 | National Natural Science Foundation of China[81373356] ; National Natural Science Foundation of China[81573378] ; National Natural Science Foundation of China[81703436] ; Science and Technology Innovation Action Plan for Basic Research of Shanghai 2014[14JC1493200] ; Shanghai Sailing Program 2017[CASIMM0120153020] ; Shanghai Sailing Program 2017[17YF1423500] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000441188300004 |
| 出版者 | HONG KONG ASIAMED PUBLISH HOUSE |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279672]  |
| 专题 | 药物制剂研究中心 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Zhong, Haijun; Gan, Yong |
| 作者单位 | 1.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China; 2.Nanchang Univ, Dept Pharm, Med Coll, 461 Bayi Rd, Nanchang 330066, Jiangxi, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, 501 Haike Rd, Shanghai 201203, Peoples R China; 4.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Song, Wenyi,Yang, Yuting,Yu, Miaorong,et al. Enhanced digestion inhibition and mucus penetration of F127-modified self-nanoemulsions for improved oral delivery[J]. ASIAN JOURNAL OF PHARMACEUTICAL SCIENCES,2018,13(4):326-335. |
| APA | Song, Wenyi.,Yang, Yuting.,Yu, Miaorong.,Zhu, Quanlei.,Damaneh, Mohammadali Soleimani.,...&Gan, Yong.(2018).Enhanced digestion inhibition and mucus penetration of F127-modified self-nanoemulsions for improved oral delivery.ASIAN JOURNAL OF PHARMACEUTICAL SCIENCES,13(4),326-335. |
| MLA | Song, Wenyi,et al."Enhanced digestion inhibition and mucus penetration of F127-modified self-nanoemulsions for improved oral delivery".ASIAN JOURNAL OF PHARMACEUTICAL SCIENCES 13.4(2018):326-335. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。