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

[Image: see text] 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 form...

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Autores principales: Puri, Vivek, Sharma, Ameya, Kumar, Pradeep, Singh, Inderbir, Huanbutta, Kampanart
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2021
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8223422/
https://www.ncbi.nlm.nih.gov/pubmed/34179628
http://dx.doi.org/10.1021/acsomega.1c01328
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author Puri, Vivek
Sharma, Ameya
Kumar, Pradeep
Singh, Inderbir
Huanbutta, Kampanart
author_facet Puri, Vivek
Sharma, Ameya
Kumar, Pradeep
Singh, Inderbir
Huanbutta, Kampanart
author_sort Puri, Vivek
collection PubMed
description [Image: see text] 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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spelling pubmed-82234222021-06-25 Synthesis and Characterization of Thiolated Gum Ghatti as a Novel Excipient: Development of Compression-Coated Mucoadhesive Tablets of Domperidone Puri, Vivek Sharma, Ameya Kumar, Pradeep Singh, Inderbir Huanbutta, Kampanart ACS Omega [Image: see text] 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. American Chemical Society 2021-06-10 /pmc/articles/PMC8223422/ /pubmed/34179628 http://dx.doi.org/10.1021/acsomega.1c01328 Text en © 2021 The Authors. Published by American Chemical Society Permits non-commercial access and re-use, provided that author attribution and integrity are maintained; but does not permit creation of adaptations or other derivative works (https://creativecommons.org/licenses/by-nc-nd/4.0/).
spellingShingle Puri, Vivek
Sharma, Ameya
Kumar, Pradeep
Singh, Inderbir
Huanbutta, Kampanart
Synthesis and Characterization of Thiolated Gum Ghatti as a Novel Excipient: Development of Compression-Coated Mucoadhesive Tablets of Domperidone
title Synthesis and Characterization of Thiolated Gum Ghatti as a Novel Excipient: Development of Compression-Coated Mucoadhesive Tablets of Domperidone
title_full Synthesis and Characterization of Thiolated Gum Ghatti as a Novel Excipient: Development of Compression-Coated Mucoadhesive Tablets of Domperidone
title_fullStr Synthesis and Characterization of Thiolated Gum Ghatti as a Novel Excipient: Development of Compression-Coated Mucoadhesive Tablets of Domperidone
title_full_unstemmed Synthesis and Characterization of Thiolated Gum Ghatti as a Novel Excipient: Development of Compression-Coated Mucoadhesive Tablets of Domperidone
title_short Synthesis and Characterization of Thiolated Gum Ghatti as a Novel Excipient: Development of Compression-Coated Mucoadhesive Tablets of Domperidone
title_sort synthesis and characterization of thiolated gum ghatti as a novel excipient: development of compression-coated mucoadhesive tablets of domperidone
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8223422/
https://www.ncbi.nlm.nih.gov/pubmed/34179628
http://dx.doi.org/10.1021/acsomega.1c01328
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