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Thiol functionalized polymethacrylic acid-based hydrogel microparticles for oral insulin delivery

Paper ID Volume ID Publish Year Pages File Format Full-Text
2270 107 2010 9 PDF Available
Title
Thiol functionalized polymethacrylic acid-based hydrogel microparticles for oral insulin delivery
Abstract

In the present study thiol functionalized polymethacrylic acid–polyethylene glycol–chitosan (PCP)-based hydrogel microparticles were utilized to develop an oral insulin delivery system. Thiol modification was achieved by grafting cysteine to the activated surface carboxyl groups of PCP hydrogels (Cys-PCP). Swelling and insulin loading/release experiments were conducted on these particles. The ability of these particles to inhibit protease enzymes was evaluated under in vitro experimental conditions. Insulin transport experiments were performed on Caco-2 cell monolayers and excised intestinal tissue with an Ussing chamber set-up. Finally, the efficacy of insulin-loaded particles in reducing the blood glucose level in streptozotocin-induced diabetic rats was investigated. Thiolated hydrogel microparticles showed less swelling and had a lower insulin encapsulation efficiency as compared with unmodified PCP particles. PCP and Cys-PCP microparticles were able to inhibit protease enzymes under in vitro conditions. Thiolation was an effective strategy to improve insulin absorption across Caco-2 cell monolayers, however, the effect was reduced in the experiments using excised rat intestinal tissue. Nevertheless, functionalized microparticles were more effective in eliciting a pharmacological response in diabetic animal, as compared with unmodified PCP microparticles. From these studies thiolation of hydrogel microparticles seems to be a promising approach to improve oral delivery of proteins/peptides.

Keywords
Oral insulin; Hydrogel; Microparticles; Thiolation; Mucoadhesion
First Page Preview
Thiol functionalized polymethacrylic acid-based hydrogel microparticles for oral insulin delivery
Publisher
Database: Elsevier - ScienceDirect
Journal: Acta Biomaterialia - Volume 6, Issue 8, August 2010, Pages 3072–3080
Authors
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Subjects
Physical Sciences and Engineering Chemical Engineering Bioengineering