Effect of Salt Forms of
Chitosan on In Vitro Permeability Enhancement in
Intestinal Epithelial Cells (Caco-2)
Thisirak Woraphatphadung, Jariya Kowapradit, Tanasait
Ngawhirunpat, Theerasak Rojanarata and Praneet
Opanasopit*
Pharmaceutical Development of
Green Innovations Group (PDGIG), Faculty of Pharmacy,
Silpakorn University, Nakhon Pathom 73000, Thailand
*For
correspondence: Email:
praneet@su.ac.th
Tel: +66-34-255800; Fax: +66-34-250941
Received: 18 October 2012
Revised accepted: 28 June
2013
Tropical Journal of
Pharmaceutical Research, August 2013;
12(4): 495-501
http://dx.doi.org/10.4314/tjpr.v12i4.8
Abstract
Purpose: To investigate the effect
of chitosan (CS) salt forms and pH condition on the
transepithelial electrical resistance (TEER) of Caco-2
cell monolayer for enhanced permeability.
Methods: Solutions (2 %w/v) of four
different salt forms of CS-aspartate (CS-A), CS-ethylene
diamine tetraacetate (CS-EDTA), CS-hydroxybenzotriazole
(CS-HOBt) and CS-thiamine pyrophosphate (CS-TPP) - were
prepared and tested on TEER using fluorescein
isothiocyanate dextran 4,400 (FD-4) as the permeant
across Caco-2 cell monolayer in both pH 6.2 and 7.4
(physiological pH) environment.
Results: The results show that
CS-salt solutions, at pH of 6.2, increased cell
permeability in a dose-dependent manner and caused
relatively reversible effects only at low doses of 0.001
- 0.010 %w/v. At CS-salt solution concentration of 0.01
%w/v, accumulation of FD-4 in the acceptor compartment
was in the rank order: CS-EDTA > CS-TPP > CS-A > CS-HOBt.
All CS-salt solutions significantly (p < 0.05) increased
the transport of FD-4. On the other hand, at pH 7.4,
only CS-EDTA at a concentration of 0.5 %w/v enhanced the
transport of FD-4. CS-EDTA was also the most toxic CS
salt.
Conclusion: The salt forms of CS are
capable of enhancing the transport of FD-4 across Caco-2
cell monolayer, with CS-EDTA the most promising of them.
Keywords: Chitosan salts,
Fluorescein isothiocyanate dextran, Transport,
Absorption enhancer, Caco-2 cells.
