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Preactivated thiomers for vaginal drug delivery vehicles

Paper ID Volume ID Publish Year Pages File Format Full-Text
6373 488 2013 8 PDF Available
Title
Preactivated thiomers for vaginal drug delivery vehicles
Abstract

It was the purpose of this study to design and evaluate a chitosan derivative as mucoadhesive excipient for vaginal drug delivery systems. The chemical modification of chitosan was achieved by conjugation of thioglycolic acid (TGA) resulting in 1594 μmol thiol groups per gram of polymer followed by the linkage of mercaptonicotinic acid (MNA) to the immobilized thiol groups via disulfide bonding leading to 702 μmol ligand per gram of preactivated polymer. The mucoadhesive properties of these polymers within newly designed vaginal formulations (Chitosan–TGA and Chitosan–TGA–MNA) and commercially available vaginal formulations (Candibene®, Daktarin®, Dalacin®, GynoPevaryl®) were tested over a time period of 24 h via a mucoadhesion test system simulating vaginal conditions, tensile studies and mucus polymer interaction studies via viscosity measurements. Within the vaginal test system simulating vaginal in situ conditions, a 1.5-fold increase in mucoadhesion could be observed for preactivated thiomer formulations after 24 h in comparison to commercially available formulations. Similar results were achieved for tensile studies, as the chitosan–TGA–MNA containing formulation resulted in a 4.9-fold increase in total work of adhesion (TWA) in comparison to Candibene which showed the highest TWA value of all tested commercial formulations. Also in terms of rheology investigations of mucus/formulation mixtures, a 5.8-fold increase in dynamic viscosity for chitosan–TGA–MNA containing mixtures could be observed in comparison to the mucus-free control. In contrast, commercially available formulations achieved a maximum enhancement of 1.9-fold. These outcomes confirm that the newly developed polymer is a promising tool for vaginal drug delivery likely providing a prolonged vaginal residence time due to its comparatively high mucoadhesive properties.

Keywords
Thiol; Chitosan; Mucosal adhesion; Vaginal drug delivery
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Publisher
Database: Elsevier - ScienceDirect
Journal: Biomaterials - Volume 34, Issue 32, October 2013, Pages 7811–7818
Authors
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Subjects
Physical Sciences and Engineering Chemical Engineering Bioengineering
Get Full-Text Now
Don't Miss Today's Special Offer
Price was $35.95
You save - $31
Price after discount Only $4.95
100% Money Back Guarantee
Full-text PDF Download
Online Support
Any Questions? feel free to contact us