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Title: | Functional Characterisation and Permeation Studies of Lyophilised Thiolated Chitosan Xerogels for Buccal Delivery of Insulin |
Authors: | Boateng, Joshua S. Mitchell, John C. Pawar, Harshavardhan Ayensu, Isaac |
Keywords: | Buccal mucosa chitosan enzyme inhibitor insulin permeation enhancement xerogel |
Issue Date: | Aug-2014 |
Publisher: | Bentham Science Publishers |
Citation: | Bentham Science Publishers |
Abstract: | Stable and mucoadhesive, lyophilised, thiolated chitosan xerogels, loaded with insulin for buccal mucosa delivery,
in place of the currently used parenteral route have been developed. The xerogels were backed with impervious ethylcellulose
laminate to ensure unidirectional release and also loaded with enzyme inhibitor to enhance insulin permeability
across the buccal mucosa. Characterisation of xerogels using 1HNMR confirmed the degree of deacetylation of the synthesised
thiolated chitosan. The amount of thiol groups immobilised on the modified chitosan was quantified by Ellman’s
reaction and molecular weight monitored by gel permeation chromatography. The stability of the secondary structure of
insulin was examined by attenuated total reflectance Fourier transform infra-red spectroscopy and circular dichroism. In
vitro and ex vivo permeation studies were undertaken by using EpiOralTM and sheep buccal membrane respectively. Insulin
released from thiolated chitosan xerogels, loaded with aprotinin (enzyme inhibitor and permeation enhancer) showed a
1.7-fold increase in permeation through EpiOralTM buccal tissue construct compared to the pure drug. However, permeation
was decreased for xerogels containing the enzyme inhibitor glutathione. Further, aprotinin containing xerogels enhanced
insulin permeation through sheep buccal membrane and demonstrated good linear correlation with the permeation
data from the EpiOralTM study. The results show the potential application of lyophilised thiolated chitosan xerogels containing
aprotinin with improved mucoadhesion, penetration enhancing and enzyme inhibition characteristics for buccal
mucosa delivery of macromolecules such as insulin. |
Description: | This article is published by Bentham Science Publishers and is also available at DOI: 10.2174/0929866521666140805124403 |
URI: | 10.2174/0929866521666140805124403 http://hdl.handle.net/123456789/15957 |
Appears in Collections: | College of Health Sciences
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