4.6 Article

Synthesis and Characterization of Thiolated Gum Ghatti as a Novel Excipient: Development of Compression-Coated Mucoadhesive Tablets of Domperidone

Journal

ACS OMEGA
Volume 6, Issue 24, Pages 15844-15854

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acsomega.1c01328

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The research aimed to synthesize and characterize a novel mucoadhesive carbohydrate polymer for formulating mucoadhesive tablets of domperidone, demonstrating potential applications in drug delivery systems.
Mucoadhesive polymers represent a major part of site-specific and localized retention strategies in oral drug delivery. The present research was designed to synthesize and characterize a novel mucoadhesive carbohydrate polymer (thiolated gum ghatti; TGG), which was employed to formulate mucoadhesive tablets of domperidone using an industrially viable compression coating technique. Thiolation of gum ghatti was achieved by the ester formation (esterification) between the hydroxyl group and the carboxyl group of gum ghatti and thioglycolic acid. TGG was characterized by various physicochemical techniques such as FTIR, XRD, SEM, and DSC. In rheological studies, the observed viscosities of pure gum mucin were 45.45 and 71.75 mPa.s and those of the thiolated gum were 78.7 and 112.58 mPa.s, respectively, in water and simulated gastric fluid. A significant increase in viscosity for thiolated gum may be attributed to increased macromolecular interactions responsible for enhanced mucoadhesive potential of thiolated gum. In silico studies corroborate the role of mucin gum interaction and energetic stabilization for enhanced mucoadhesion properties of thiolated gum. Ex vivo mucoadhesion strength of gum ghatti- and TGG-coated tablets was found to be ranging between 45.77 +/- 1.49 and 88.16 +/- 1.75 and 115.32 +/- 2.36 and 184.65 +/- 2.07 mN, respectively. In an acute oral toxicity study, TGG did not show any toxicity on the vital organs of the Wistar rat and proved to be a safe polymer. TGG may be regarded as a promising polymer for developing different mucoadhesive drug delivery systems.

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