The characteristics and mechanism of simvastatin loaded lipid nanoparticles to increase oral bioavailability in rats
文献类型：期刊论文
| 作者 | Zhang, Zhiwen2 ; Bu, Huihui2; Gao, Zhiwei2; Huang, Yan2; Gao, Fang1,2; Li, Yaping2
|
| 刊名 | INTERNATIONAL JOURNAL OF PHARMACEUTICS
 |
| 出版日期 | 2010-07-15 |
| 卷号 | 394期号:1-2页码:147-153 |
| 关键词 | Simvastatin Simvastatin acid Lipid nanoparticles Intestinal absorption Bioavailability |
| ISSN号 | 0378-5173 |
| DOI | 10.1016/j.ijpharm.2010.04.039 |
| 文献子类 | Article |
| 英文摘要 | Simvastatin (SV), a cholesterol-lowering agent, has been widely used in the treatment of hypercholesterolemia, dyslipidemia and coronary heart disease, but SV shows the low oral bioavailability due to its poor aqueous solubility and extensive metabolism by cytochrome-3A system in intestinal guts and liver. In this work. SV loaded lipid nanoparticles (SLNs) with different components were designed to enhance its oral bioavailability, and the plasma concentration of SV and its active metabolite (simvastatin acid, SVA) was determined by LC-MS-MS method. The experimental results showed that SLNs were spherical nano-sized particles with high encapsulation efficiency (>95%). The in situ intestinal absorption indicated that the absorption of SLNs was greatly improved compared with that of free SV, and the absorption was changed with the site of the intestinal segments. SLNs could be uptaken into the enterocytes through both clathrin and caveolae mediated endocytosis pathways. The oral bioavailability of SV after its incorporation into the lipid nanoparticles was improved by 3.37-fold for SLNs I and 2.55-fold for SLNs II compared with that from free SV in rats, and that of the SVA was significantly enhanced as well. As a result, lipid nanoparticles could be a promising delivery system to enhance the oral bioavailability of simvastatin. (C) 2010 Elsevier B.V. All rights reserved. |
| WOS关键词 | DRUG-DELIVERY SYSTEMS ; POORLY SOLUBLE DRUGS ; IN-VITRO ; FORMULATION ; ABSORPTION ; EXCIPIENTS ; CYTOCHROME-P450 ; ENHANCEMENT ; STRATEGIES |
| 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 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[0852nm05700] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000279720400017 |
| 出版者 | ELSEVIER SCIENCE BV |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278834]  |
| 专题 | 药物制剂研究中心 |
| 通讯作者 | Li, Yaping |
| 作者单位 | 1.Shenyang Pharmaceut Univ, Sch Pharm, Shenyang 110016, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Drug Delivery Syst, Shanghai 201203, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Zhang, Zhiwen,Bu, Huihui,Gao, Zhiwei,et al. The characteristics and mechanism of simvastatin loaded lipid nanoparticles to increase oral bioavailability in rats[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2010,394(1-2):147-153. |
| APA | Zhang, Zhiwen,Bu, Huihui,Gao, Zhiwei,Huang, Yan,Gao, Fang,&Li, Yaping.(2010).The characteristics and mechanism of simvastatin loaded lipid nanoparticles to increase oral bioavailability in rats.INTERNATIONAL JOURNAL OF PHARMACEUTICS,394(1-2),147-153. |
| MLA | Zhang, Zhiwen,et al."The characteristics and mechanism of simvastatin loaded lipid nanoparticles to increase oral bioavailability in rats".INTERNATIONAL JOURNAL OF PHARMACEUTICS 394.1-2(2010):147-153. |
入库方式： OAI收割
来源：上海药物研究所
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