A high-drug-loading self-assembled nanoemulsion enhances the oral absorption of probucol in rats
文献类型：期刊论文
| 作者 | Zhang, Zhiwen1 ; Huang, Jian2; Jiang, Shijun3; Liu, Zeying3; Gu, Wangwen1; Yu, Haijun1; Li, Yaping1
|
| 刊名 | JOURNAL OF PHARMACEUTICAL SCIENCES
 |
| 出版日期 | 2013-04 |
| 卷号 | 102期号:4页码:1301-1306 |
| 关键词 | nanoemulsion self-assembly bioavailability poorly water-soluble drug probucol intestinal absorption pharmacokinetics calorimetry (DSC) oral drug delivery |
| ISSN号 | 0022-3549 |
| DOI | 10.1002/jps.23460 |
| 文献子类 | Article |
| 英文摘要 | The purpose of this study was to develop a high-drug-loading nanoemulsion by self-assembly to improve the oral absorption of high dosing poorly water-soluble drugs. Probucol was selected as a model drug and the probucol-loaded self-assembled nanoemulsion (PSN) was prepared and characterized. Moreover, the intestinal absorption and in vivo pharmacokinetic behavior of PSN were evaluated in rats after oral administration. The experimental results indicated that PSN was nanometer-sized droplets with the mean diameter of 40.32 +/- 0.31 nm and polydispersity index of 0.184 +/- 0.005. The aqueous solubility of probucol was remarkably increased after its incorporation into PSN. Compared with free drug suspension, the intestinal absorption of PSN was not significantly increased in duodenum, but obviously enhanced 3.62- and 13.1-fold in jejunum and ileum, respectively. In particular, the in vivo pharmacokinetic results indicated that the oral bioavailability of probucol was greatly improved 8.97-fold by PSN. Thereby, the high-drug-loading self-assembled nanoemulsion was very effective in enhancing the oral absorption of high-dosing poorly water-soluble drugs. (c) 2013 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 102:13011306, 2013 |
| WOS关键词 | SOLID LIPID NANOPARTICLES ; IN-VITRO CHARACTERISTICS ; DELIVERY SYSTEMS ; LIPOPHILIC DRUGS ; BIOAVAILABILITY ; OPTIMIZATION ; FORMULATIONS ; PARAMETERS ; MECHANISM ; DESIGN |
| 资助项目 | National Basic Research Program of China[2009CB930304] ; National Basic Research Program of China[2013CB932503] ; National Basic Research Program of China[2013CB932704] ; Shanghai Rising-Star Program[11QA1407900] ; SA-SIBS Scholarship Program[00000000] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000315723700014 |
| 出版者 | WILEY |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277683]  |
| 专题 | 药物制剂研究中心 |
| 通讯作者 | Li, Yaping |
| 作者单位 | 1.Chinese Acad Sci, Ctr Pharmaceut, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; 2.Jiangsu Univ, Sch Pharm, Zhenjiang 212013, Peoples R China; 3.E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhang, Zhiwen,Huang, Jian,Jiang, Shijun,et al. A high-drug-loading self-assembled nanoemulsion enhances the oral absorption of probucol in rats[J]. JOURNAL OF PHARMACEUTICAL SCIENCES,2013,102(4):1301-1306. |
| APA | Zhang, Zhiwen.,Huang, Jian.,Jiang, Shijun.,Liu, Zeying.,Gu, Wangwen.,...&Li, Yaping.(2013).A high-drug-loading self-assembled nanoemulsion enhances the oral absorption of probucol in rats.JOURNAL OF PHARMACEUTICAL SCIENCES,102(4),1301-1306. |
| MLA | Zhang, Zhiwen,et al."A high-drug-loading self-assembled nanoemulsion enhances the oral absorption of probucol in rats".JOURNAL OF PHARMACEUTICAL SCIENCES 102.4(2013):1301-1306. |
入库方式： OAI收割
来源：上海药物研究所
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