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Methacrylated chitosan as a polymer with enhanced mucoadhesive properties for transmucosal drug delivery

Lookup NU author(s): Dr Wing Man LauORCiD

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This work is licensed under a Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License (CC BY-NC-ND).


Abstract

© 2018 Elsevier B.V. Chitosan is a cationic polysaccharide that exhibits mucoadhesive properties which allow it to adhere to mucosal tissues. In this work, we explored chemical modification of chitosan through its reaction with methacrylic anhydride to synthesise methacrylated derivative with the aim to improve its mucoadhesive properties. The reaction products were characterised using 1H NMR, FTIR and UV–Vis spectroscopy. 1H NMR and ninhydrin test were used to quantify the degree of methacrylation of chitosan. Turbidimetric analysis of the effect of pH on aqueous solubility of the polymers revealed that the highly methacrylated derivative remained turbid and its turbidity did not change from pH 3 to 9. However, solutions of native chitosan and its derivative with low methacrylation remained transparent at pH 6.5 and exhibited a rapid increase in turbidity at pH > 6.5. The mucoadhesive properties of chitosan and its methacrylated derivatives were evaluated using flow-through method combined with fluorescent microscopy with fluorescein sodium as a model drug. The retention of these polymers was evaluated on porcine bladder mucosa in vitro. The methacrylated derivatives exhibited greater ability to retain fluorescein sodium on the bladder mucosa compared to the parent chitosan. Toxicological studies using MTT assay with UMUC3 bladder cells show no significant differences in toxicity between chitosan and its methacrylated derivatives suggesting good biocompatibility of these novel mucoadhesive polymers.


Publication metadata

Author(s): Kolawole OM, Lau WM, Khutoryanskiy VV

Publication type: Article

Publication status: Published

Journal: International Journal of Pharmaceutics

Year: 2018

Volume: 550

Issue: 1-2

Pages: 123-129

Print publication date: 25/10/2018

Online publication date: 18/08/2018

Acceptance date: 17/08/2018

Date deposited: 03/09/2018

ISSN (print): 0378-5173

ISSN (electronic): 1873-3476

Publisher: Elsevier B.V.

URL: https://doi.org/10.1016/j.ijpharm.2018.08.034

DOI: 10.1016/j.ijpharm.2018.08.034


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