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Bile salts enhance the intestinal absorption of lipophilic drug loaded lipid nanocarriers: Mechanism and effect in rats

文献类型：期刊论文

作者Zhang, Zhiwen2; Gao, Fang2; Jiang, Shijun1; Chen, Lingli2; Liu, Zeying1; Yu, Haijun2; Li, Yaping2
刊名INTERNATIONAL JOURNAL OF PHARMACEUTICS
出版日期2013-08-16
卷号452期号:1-2页码:374-381
关键词Bile salts Lipid nanocarriers Lipophilic drugs Intestinal absorption Caco-2 cells Lymphatic transport
ISSN号0378-5173
DOI10.1016/j.ijpharm.2013.05.021
文献子类Article
英文摘要The purpose of this study was to elucidate the effect and possible mechanism of bile salts on the intestinal absorption of lipophilic drug loaded lipid nanocarriers in rats. Effects of sodium cholate (SC) on the characteristics, intestinal absorption, cellular uptake in Caco-2 cell monolayers and intestinal lymphatic transport of candesartan cilexetil loaded lipid nanocarriers (CLN) were investigated to clarify the possible mechanism. The intestinal absorption of candesartan from CLN was evidently improved over 16-fold compared with free drug suspension, and further significantly enhanced 1.79-fold after the addition of SC. The cellular uptake of CLN in Caco-2 cell monolayers at 37 degrees C and its colocalization with endoplasmic reticulum were obviously increased in the presence of SC. Moreover, the intestinal lymphatic transport of CLN was obviously enhanced by SC. These results implicated that bile salts could improve the cellular uptake of CLN in Caco-2 cell monolayers via the active processes and promote the intestinal absorption of CLN through the intestinal lymphatic pathway. Therefore, bile salts could be an important physiological factor affecting the intestinal absorption of lipophilic drugs loaded lipid nanocarriers. (C) 2013 Elsevier B. V. All rights reserved.
WOS关键词IN-VITRO CHARACTERISTICS ; FLOW BLOCKING APPROACH ; ORAL DELIVERY ; LYMPHATIC TRANSPORT ; NANOPARTICLES ; BIOAVAILABILITY ; SYSTEMS ; PHOSPHATIDYLCHOLINE ; SOLUBILIZATION ; FORMULATION
资助项目National Basic Research Program of China[2009CB930304] ; National Basic Research Program of China[2013CB932704] ; Shanghai Rising-Star Program[11QA1407900] ; SA-SIBS Scholarship Program[00000000]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000321496200044
出版者ELSEVIER SCIENCE BV
源URL[http://119.78.100.183/handle/2S10ELR8/277504]  
专题药物制剂研究中心
通讯作者Li, Yaping
作者单位1.E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China
2.Chinese Acad Sci, Ctr Pharmaceut, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China;
推荐引用方式
GB/T 7714		 Zhang, Zhiwen,Gao, Fang,Jiang, Shijun,et al. Bile salts enhance the intestinal absorption of lipophilic drug loaded lipid nanocarriers: Mechanism and effect in rats[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2013,452(1-2):374-381.
APA Zhang, Zhiwen.,Gao, Fang.,Jiang, Shijun.,Chen, Lingli.,Liu, Zeying.,...&Li, Yaping.(2013).Bile salts enhance the intestinal absorption of lipophilic drug loaded lipid nanocarriers: Mechanism and effect in rats.INTERNATIONAL JOURNAL OF PHARMACEUTICS,452(1-2),374-381.
MLA Zhang, Zhiwen,et al."Bile salts enhance the intestinal absorption of lipophilic drug loaded lipid nanocarriers: Mechanism and effect in rats".INTERNATIONAL JOURNAL OF PHARMACEUTICS 452.1-2(2013):374-381.

入库方式： OAI收割

来源：上海药物研究所

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