Hydroxyethyl cellulose functionalised with maleimide groups as a new excipient with enhanced mucoadhesive properties

Buang, F., Fu, M., Chatzifragkou, A. ORCID: https://orcid.org/0000-0002-9255-7871, Amin, M. C. I. M. and Khutoryanskiy, V. V. ORCID: https://orcid.org/0000-0002-7221-2630 (2023) Hydroxyethyl cellulose functionalised with maleimide groups as a new excipient with enhanced mucoadhesive properties. International Journal of Pharmaceutics, 642. 123113. ISSN 0378-5173 doi: 10.1016/j.ijpharm.2023.123113

Abstract/Summary

Hydroxyethylcellulose (HEC) is a non-ionic water-soluble polymer with poor mucoadhesive properties. The mucoadhesive properties of hydroxyethylcellulose can be improved by modifying it through conjugation with molecules containing maleimide groups. Maleimide groups interact with the thiol groups present in cysteine domains in the mucin via Michael addition reaction under physiological conditions to form a strong mucoadhesive bond. This will prolong the residence time of a dosage form containing this modified polymer and drug on mucosal surfaces. In this study HEC was modified by reaction with 4-bromophenyl maleimide in varying molar ratios and the successful synthesis was confirmed using 1H NMR and FTIR spectroscopies. The safety of the newly synthesised polymer derivatives was assessed with in vivo planaria assays and in vitro MTT assay utilising Caco-2 cell line. The synthesized maleimide-functionalised HEC solutions were sprayed onto blank tablets to develop a model dosage form. The physical properties and mucoadhesive behavior of these tablets were evaluated using a tensile test with sheep buccal mucosa. The maleimide-functionalised HEC exhibited superior mucoadhesive properties compared to unmodified HEC.

Item Type	Article
URI	https://reading-clone.eprints-hosting.org/id/eprint/112255
Item Type	Article
Refereed	Yes
Divisions	Life Sciences > School of Chemistry, Food and Pharmacy > School of Pharmacy > Pharmaceutics Research Group Life Sciences > School of Chemistry, Food and Pharmacy > Department of Food and Nutritional Sciences > Food Research Group
Publisher	Elsevier
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