Gellan gum and its methacrylated derivatives as in situ gelling mucoadhesive formulations of pilocarpine: In vitro and in vivo studies

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Agibayeva, L. E., Kaldybekov, D. B., Porfiryeva, N. N., Garipova, V. R., Mangazbayeva, R. A., Moustafine, R. I., Semina, I. I., Mun, G. A., Kudaibergenov, S. E. and Khutoryanskiy, V. V. orcid id iconORCID: https://orcid.org/0000-0002-7221-2630 (2020) Gellan gum and its methacrylated derivatives as in situ gelling mucoadhesive formulations of pilocarpine: In vitro and in vivo studies. International Journal of Pharmaceutics, 577. 119093. ISSN 0378-5173 doi: 10.1016/j.ijpharm.2020.119093

Abstract/Summary

Gellan gum was chemically modified by the reaction with methacrylic anhydride to produce derivatives with 6, 14 and 49% methacrylation. The structure and substitution degrees of these derivatives were confirmed by 1H NMR- and FTIR-spectroscopy. These derivatives are more hydrophobic compared to pristine gellan and form turbid solutions in water. In vitro study performed with formulations of sodium fluorescein containing gellan gum and its methacrylated derivatives indicated that methacrylation enhances their retention on bovine conjunctival mucosa. In vivo experiments with the formulations of pilocarpine hydrochloride containing gellan gum and methacrylated derivatives have demonstrated that all polymers enhance the drug effect significantly, but best performance is observed for the polysaccharide with 6% methacrylation.

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Item Type Article
URI https://reading-clone.eprints-hosting.org/id/eprint/89013
Identification Number/DOI 10.1016/j.ijpharm.2020.119093
Refereed Yes
Divisions Interdisciplinary centres and themes > Chemical Analysis Facility (CAF) > NMR (CAF)
Life Sciences > School of Chemistry, Food and Pharmacy > School of Pharmacy > Pharmaceutics Research Group
Publisher Elsevier
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