Document Detail

In vitro permeability enhancement in intestinal epithelial cells (Caco-2) monolayer of water soluble quaternary ammonium chitosan derivatives.
MedLine Citation:
PMID:  20333490     Owner:  NLM     Status:  MEDLINE    
The aim of this study was to investigate the effects of a type of hydrophobic moiety, extent of N-substitution (ES), and degree of quaternization (DQ) of chitosan (CS) on the transepithelial electrical resistance and permeability of Caco-2 cells monolayer, using fluorescein isothiocyanate dextran 4,400 (FD-4) as the model compound for paracellular tight junction transport. CS was substituted with hydrophobic moiety, an aliphatic aldehyde (n-octyl) or aromatic aldehyde (benzyl), for the improved hydrophobic interaction with cell membrane, and they were quaternized with Quat-188 to render CS soluble. The factors affecting the epithelial permeability have been evaluated in the intestinal cell monolayers, Caco-2 cells. Cytotoxicity was evaluated by using the trypan blue and MTT viability assay. The results revealed that at pH 7.4 CSQ appeared to increase cell permeability in dose-dependent manner, and this effect was relatively reversible at the lower doses of 0.05-1.25 mM. The higher DQ and ES caused the higher permeability of FD-4. Cytotoxicity of CSQ was concentration, %DQ, and %ES dependent. Substitution with hydrophobic moiety caused decreasing in permeability of FD-4 and cytotoxicity by benzyl group had more effect than octyl group. These studies demonstrated that these novel modified chitosan derivatives had potential for using as absorption enhancers.
Jariya Kowapradit; Praneet Opanasopit; Tanasait Ngawhirunpat; Auayporn Apirakaramwong; Theerasak Rojanarata; Uracha Ruktanonchai; Warayuth Sajomsang
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2010-03-24
Journal Detail:
Title:  AAPS PharmSciTech     Volume:  11     ISSN:  1530-9932     ISO Abbreviation:  AAPS PharmSciTech     Publication Date:  2010 Jun 
Date Detail:
Created Date:  2010-06-18     Completed Date:  2010-10-08     Revised Date:  2013-05-29    
Medline Journal Info:
Nlm Unique ID:  100960111     Medline TA:  AAPS PharmSciTech     Country:  United States    
Other Details:
Languages:  eng     Pagination:  497-508     Citation Subset:  IM    
Faculty of Pharmacy, Silpakorn University, Nakhon Pathom, Thailand.
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MeSH Terms
Caco-2 Cells
Cell Membrane / chemistry*
Cell Membrane Permeability*
Chitosan / chemistry*
Drug Carriers / chemistry*
Quaternary Ammonium Compounds / chemistry*
Reg. No./Substance:
0/Drug Carriers; 0/Quaternary Ammonium Compounds; 9012-76-4/Chitosan

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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