Document Detail

Enhanced oral absorption of paclitaxel in N-deoxycholic acid-N, O-hydroxyethyl chitosan micellar system.
MedLine Citation:
PMID:  20845453     Owner:  NLM     Status:  MEDLINE    
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.
Hong Li; Meirong Huo; Jianping Zhou; Yindi Dai; Yaping Deng; Xiangjie Shi; Jumah Masoud
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of pharmaceutical sciences     Volume:  99     ISSN:  1520-6017     ISO Abbreviation:  J Pharm Sci     Publication Date:  2010 Nov 
Date Detail:
Created Date:  2010-09-16     Completed Date:  2011-01-13     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  2985195R     Medline TA:  J Pharm Sci     Country:  United States    
Other Details:
Languages:  eng     Pagination:  4543-53     Citation Subset:  IM    
Copyright Information:
© 2010 Wiley-Liss, Inc. and the American Pharmacists Association
Faculty of Pharmacy, Department of Pharmaceutics, China Pharmaceutical University, Nanjing 210009, China.
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MeSH Terms
Administration, Oral
Antineoplastic Agents, Phytogenic / administration & dosage*,  pharmacokinetics*
Chitosan / chemistry*
Deoxycholic Acid / chemistry*
Drug Carriers / chemistry
Intestinal Absorption
P-Glycoprotein / metabolism
Paclitaxel / administration & dosage*,  pharmacokinetics*
Rats, Sprague-Dawley
Reg. No./Substance:
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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