Nanoemulsion improves the oral absorption of candesartan cilexetil in rats: Performance and mechanism
文献类型：期刊论文
| 作者 | Gao, Fang2; Zhang, Zhiwen2 ; Bu, Huihui2; Huang, Yan2; Gao, Zhiwei1; Shen, Jianan2; Zhao, Chunjie3; Li, Yaping2
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| 刊名 | JOURNAL OF CONTROLLED RELEASE
 |
| 出版日期 | 2011-01-20 |
| 卷号 | 149期号:2页码:168-174 |
| 关键词 | Candesartan cilexetil Candesartan Nanoemulsion Oral absorption |
| ISSN号 | 0168-3659 |
| DOI | 10.1016/j.jconrel.2010.10.013 |
| 文献子类 | Article |
| 英文摘要 | Candesartan cilexetil (CC), an inactive prodrug of candesartan, was rapidly hydrolyzed into active candesartan during absorption in the gastrointestinal (GI) tract to achieve antihypertensive effects. However, CC exhibited incomplete intestinal absorption with low oral bioavailability due to its poor aqueous solubility. In this work, a novel CC loaded nanoemulsion (CCN) was designed to improve the intestinal absorption. CCN was prepared by a modified emulsification-solvent evaporation technique. The physicochemical characteristics of CCN were characterized, and the intestinal absorption was investigated as well. The experimental results indicated that CCN was nanometer-sized droplets (35.5 +/- 5.9 nm) with negative potential (-6.45 +/- 0.36 mV), and the absorption of CCN was significantly improved in total intestinal tract compared with free CC solution. Moreover, CCN could be internalized into the enterocytes by clathrin-mediated endocytosis pathway, and thereafter transported into systemic circulation via both portal vein and lymphatic pathway. The concentration of active candesartan in rat plasma was determined by LC-MS-MS method. The experimental results showed that the area under the concentration-time curve (AUC(0-t)) of candesartan was improved over 10-fold after CC was incorporated into CCN. The overall results implicated that the nanoemulsion was very effective for enhancing the oral absorption of insoluble CC, and CCN showed the great potential for clinical application. (c) 2010 Elsevier B.V. All rights reserved. |
| WOS关键词 | INTESTINAL LYMPHATIC TRANSPORT ; SOLID LIPID NANOPARTICLES ; FLOW BLOCKING APPROACH ; SPONTANEOUS EMULSIFICATION ; LIPOPHILIC DRUGS ; CELL-LINE ; FORMULATION ; DELIVERY ; BIOAVAILABILITY ; INTERNALIZATION |
| 资助项目 | National Basic Research Program of China[2009CB930304] ; National Basic Research Program of China[2007CB935800] ; National Natural Science Foundation of China[30925041] ; National Natural Science Foundation of China[30873169] ; National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program"[2009ZX09501-024] ; National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program"[2009ZX09301-001] ; Shanghai Nanomedicine Program[1052nm06300] |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000287115200010 |
| 出版者 | ELSEVIER SCIENCE BV |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278622]  |
| 专题 | 药物制剂研究中心 |
| 通讯作者 | Li, Yaping |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Drug Metab, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Pharmaceut, Shanghai 201203, Peoples R China; 3.Shenyang Pharmaceut Univ, Sch Pharm, Shenyang 110016, Peoples R China |
| 推荐引用方式 GB/T 7714 | Gao, Fang,Zhang, Zhiwen,Bu, Huihui,et al. Nanoemulsion improves the oral absorption of candesartan cilexetil in rats: Performance and mechanism[J]. JOURNAL OF CONTROLLED RELEASE,2011,149(2):168-174. |
| APA | Gao, Fang.,Zhang, Zhiwen.,Bu, Huihui.,Huang, Yan.,Gao, Zhiwei.,...&Li, Yaping.(2011).Nanoemulsion improves the oral absorption of candesartan cilexetil in rats: Performance and mechanism.JOURNAL OF CONTROLLED RELEASE,149(2),168-174. |
| MLA | Gao, Fang,et al."Nanoemulsion improves the oral absorption of candesartan cilexetil in rats: Performance and mechanism".JOURNAL OF CONTROLLED RELEASE 149.2(2011):168-174. |
入库方式： OAI收割
来源：上海药物研究所
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