| Solid lipid nanoparticles loading candesartan cilexetil enhance oral bioavailability: in vitro characteristics and absorption mechanism in rats. | |
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MedLine Citation:
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PMID: 21930110 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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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 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 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 (SLNs). These results indicated that SLNs demonstrated great potential for increasing oral delivery of lipophilic drugs such as CC. |
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Authors:
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Fang Gao; Huihui Bu; Zhiwen Zhang; Jisheng Xiao; Yaping Li |
Publication Detail:
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Type: JOURNAL ARTICLE Date: 2011-9-16 |
Journal Detail:
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Title: Nanomedicine : nanotechnology, biology, and medicine Volume: - ISSN: 1549-9642 ISO Abbreviation: - Publication Date: 2011 Sep |
Date Detail:
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Created Date: 2011-9-20 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 101233142 Medline TA: Nanomedicine Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Copyright Information:
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Copyright © 2011. Published by Elsevier Inc. |
Affiliation:
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Center of Pharmaceutics, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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