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Author Sajeesh, S. ♦ Bouchemal, K. ♦ Sharma, C. P. ♦ Vauthier, C.
Source Sree Chitra Tirunal Institute for Medical Sciences & Technology
Content type Text
Publisher European Journal of Pharmaceutics and Biopharmaceutics
File Format PDF
Language English
Subject Domain (in DDC) Technology ♦ Medicine & health ♦ Pharmacology and therapeutics
Subject Domain (in MeSH) Therapeutics ♦ Analytical, Diagnostic and Therapeutic Techniques and Equipment
Subject Keyword Drug Delivery
Abstract Aim of the present work was to develop novel thiol-functionalized hydrogel microparticles based on poly(methacrylic acid)-chitosan-poly(ethylene glycol) (PCP) for oral drug delivery applications.PCP microparticles were prepared by a modified ionic gelation process in aqueous medium. Thiol modification of surface carboxylic acid groups of PCP micro particles was carried out by Coupling L-Cysteine with a water-soluble carbodiimide. Ellman's method was adopted to quantify the sulfhydryl groups. and dynamic light-scattering technique was used to measure the average particle size. Cytotoxicity of the modified particles was evaluated on Caco 2 cells by MTT assay. Effect of thiol modification on permeability of paracellular marker fluorescence dextran (FD4) was evaluated on Caco 2 cell monolayers and freshly excised rat intestinal tissue with an Ussing chamber set-up. Mucoadhesion experiments were carried out by an ex vivo bioadhesion method with excised rat intestinal tissue.The average size of the PCP microparticles was increased after thiol modification. Thiolated microparticles significantly improved the paracellular permeability of FD4 across Caco 2 cell monolayers, with no sign of toxicity. However, the efficacy of thiolated system remained low when permeation experiments were carried out across excised intestinal membrane. This was attributed to the high adhesion of the thiolated particles on the gut mucosa. Nevertheless, it can be concluded that surface thiolation is an interesting strategy to improve paracellular permeability of hydrophilic macromolecules. (C) 2009 Elsevier B.V. All rights reserved.
Education Level UG and PG
Learning Resource Type Article
Educational Framework Medical Council of India (MCI)
Volume Number 74
Issue Number 2
Page Count 10
Starting Page 209
Ending Page 218