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

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

[Display omitted] 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 hydrophobi...

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Bibliographic Details
Published in:International journal of pharmaceutics Vol. 577; p. 119093
Main Authors: Agibayeva, Laura E., Kaldybekov, Daulet B., Porfiryeva, Natalia N., Garipova, Venera R., Mangazbayeva, Rauash A., Moustafine, Rouslan I., Semina, Irina I., Mun, Grigoriy A., Kudaibergenov, Sarkyt E., Khutoryanskiy, Vitaliy V.
Format: Journal Article
Language:English
Published: Netherlands Elsevier B.V 15-03-2020
Subjects:
Gellan gum
Glaucoma
In situ gelling
Methacrylation
Mucoadhesion
Ocular drug delivery
Pilocarpine
Wash out50
Glaucoma
Methacrylation
Gellan gum
Wash out50
In situ gelling
Pilocarpine
Mucoadhesion
Ocular drug delivery
Wash out
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Summary:[Display omitted] 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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content type line 23
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2020.119093