| Enhanced oral absorption of paclitaxel in N-deoxycholic acid-N, O-hydroxyethyl chitosan micellar system. | |
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MedLine Citation:
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PMID: 20845453 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The overall goal of this study was to develop a micellar system of paclitaxel (PTX) to enhance its oral absorption. An amphiphilic chitosan derivative, N-deoxycholic acid-N, O-hydroxyethyl chitosan (DHC), was synthesized and characterized by FTIR, (1)H NMR, elemental analysis, and X-ray diffraction (XRD) techniques. The degree of substitution (DS) of hydroxyethyl group and deoxycholic acid group ranged from 89.5-114.5% and 1.11-8.17%, respectively. The critical micelle concentration (CMC) values of DHC decreased from 0.26 to 0.16 mg/mL as the DS of deoxycholic acid group increased. PTX was successfully loaded in DHC micelles with a high drug loading (31.68 ± 0.14%) and entrapment efficiency (77.57 ± 0.51%). The particle size of PTX-loaded DHC micelles ranged from 203.35 ± 2.19 to 236.70 ± 3.40 nm as the DS of deoxycholic acid group increased. After orally administration of PTX-loaded DHC micelles, the bioavailability was threefold compared with that of an orally dosed Taxol®. The single-pass intestinal perfusion studies (SPIP) showed that the intestinal absorption of micelles was via endocytosis involving a saturable process and a p-glycoprotein (P-gp)-independent way. All these indicated that the DHC micelles might be a promising tool for oral delivery of poorly water-soluble drugs. |
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Authors:
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Hong Li; Meirong Huo; Jianping Zhou; Yindi Dai; Yaping Deng; Xiangjie Shi; Jumah Masoud |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Journal of pharmaceutical sciences Volume: 99 ISSN: 1520-6017 ISO Abbreviation: J Pharm Sci Publication Date: 2010 Nov |
Date Detail:
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Created Date: 2010-09-16 Completed Date: 2011-01-13 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 2985195R Medline TA: J Pharm Sci Country: United States |
Other Details:
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Languages: eng Pagination: 4543-53 Citation Subset: IM |
Copyright Information:
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© 2010 Wiley-Liss, Inc. and the American Pharmacists Association |
Affiliation:
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Faculty of Pharmacy, Department of Pharmaceutics, China Pharmaceutical University, Nanjing 210009, China. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Administration, Oral Animals Antineoplastic Agents, Phytogenic / administration & dosage*, pharmacokinetics* Chitosan / chemistry* Deoxycholic Acid / chemistry* Drug Carriers / chemistry Intestinal Absorption Micelles P-Glycoprotein / metabolism Paclitaxel / administration & dosage*, pharmacokinetics* Rats Rats, Sprague-Dawley |
| Chemical | |
Reg. No./Substance:
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0/Antineoplastic Agents, Phytogenic; 0/Drug Carriers; 0/Micelles; 0/P-Glycoprotein; 33069-62-4/Paclitaxel; 83-44-3/Deoxycholic Acid; 9012-76-4/Chitosan |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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