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Solid lipid nanoparticles loading candesartan cilexetil enhance oral bioavailability: in vitro characteristics and absorption mechanism in rats

文献类型：期刊论文

作者Zhang, Zhiwen1; Gao, Fang1,2; Bu, Huihui1; Xiao, Jisheng1; Li, Yaping1
刊名NANOMEDICINE-NANOTECHNOLOGY BIOLOGY AND MEDICINE
出版日期2012-07
卷号8期号:5页码:740-747
关键词Solid lipid nanoparticles Candesartan Oral bioavailability Lymphatic transport
ISSN号1549-9634
DOI10.1016/j.nano.2011.08.016
文献子类Article
英文摘要Candesartan cilexetil (CC) is widely used for the treatment of hypertension and heart failure, but it shows very poor aqueous solubility and very low oral absorption. In this work, CC-loaded solid lipid nanoparticles (CLNs) were successfully developed to improve the oral bioavailability. The physicochemical properties of CLNs were characterized, and the pharmacokinetic behavior of CLNs was evaluated in rats. CLNs exhibited nanometer-sized spherical particles with high entrapment efficiency (91.33%). The absorption of CLNs in the stomach was only 2.8% of that in intestine. Moreover, CLNs could be internalized into the enterocytes and then transported into the systemic circulation via the portal circulation and intestinal lymphatic pathway. The pharmacokinetic results indicated that the oral bioavailability of candesartan was obviously improved over 12-fold after incorporation into solid lipid nanoparticles. These results demonstrated that solid lipid nanoparticles have great potential for increasing oral bioavailability of lipophilic drugs such as CC. (C) 2011 Elsevier Inc. All rights reserved.
WOS关键词INTESTINAL LYMPHATIC TRANSPORT ; FLOW BLOCKING APPROACH ; HEART-FAILURE ; LIPOPHILIC DRUGS ; CACO-2 CELLS ; HYPERTENSION ; DELIVERY ; PHARMACOKINETICS ; FORMULATIONS ; EFFICACY
资助项目National Basic Research Program of China[2009CB930304] ; National Basic Research Program of China[2010CB934000] ; National Natural Science Foundation of China[30925041] ; National Natural Science Foundation of China[30901866] ; Shanghai Nanomedicine Program[1052nm06300] ; Shanghai Rising-Star Program[11QA1407900]
WOS研究方向Science & Technology - Other Topics ; Research & Experimental Medicine
语种英语
WOS记录号WOS:000305704800022
出版者ELSEVIER SCIENCE BV
源URL[http://119.78.100.183/handle/2S10ELR8/278030]  
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.Shenyang Pharmaceut Univ, Sch Pharm, Shenyang, Peoples R China
推荐引用方式
GB/T 7714		 Zhang, Zhiwen,Gao, Fang,Bu, Huihui,et al. Solid lipid nanoparticles loading candesartan cilexetil enhance oral bioavailability: in vitro characteristics and absorption mechanism in rats[J]. NANOMEDICINE-NANOTECHNOLOGY BIOLOGY AND MEDICINE,2012,8(5):740-747.
APA Zhang, Zhiwen,Gao, Fang,Bu, Huihui,Xiao, Jisheng,&Li, Yaping.(2012).Solid lipid nanoparticles loading candesartan cilexetil enhance oral bioavailability: in vitro characteristics and absorption mechanism in rats.NANOMEDICINE-NANOTECHNOLOGY BIOLOGY AND MEDICINE,8(5),740-747.
MLA Zhang, Zhiwen,et al."Solid lipid nanoparticles loading candesartan cilexetil enhance oral bioavailability: in vitro characteristics and absorption mechanism in rats".NANOMEDICINE-NANOTECHNOLOGY BIOLOGY AND MEDICINE 8.5(2012):740-747.

入库方式： OAI收割

来源：上海药物研究所

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