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Improved Mucoadhesion, Permeation and In Vitro Anticancer Potential of Synthesized Thiolated Acacia and Karaya Gum Combination: A Systematic Study

Thiolation of polymers is one of the most appropriate approaches to impart higher mechanical strength and mucoadhesion. Thiol modification of gum karaya and gum acacia was carried out by esterification with 80% thioglycolic acid. FTIR, DSC and XRD confirmed the completion of thiolation reaction. Ant...

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Autores principales: Munot, Neha, Kandekar, Ujjwala, Rikame, Chaitali, Patil, Abhinandan, Sengupta, Poulomi, Urooj, Shabana, Bilal, Anusha
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9609301/
https://www.ncbi.nlm.nih.gov/pubmed/36296425
http://dx.doi.org/10.3390/molecules27206829
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author Munot, Neha
Kandekar, Ujjwala
Rikame, Chaitali
Patil, Abhinandan
Sengupta, Poulomi
Urooj, Shabana
Bilal, Anusha
author_facet Munot, Neha
Kandekar, Ujjwala
Rikame, Chaitali
Patil, Abhinandan
Sengupta, Poulomi
Urooj, Shabana
Bilal, Anusha
author_sort Munot, Neha
collection PubMed
description Thiolation of polymers is one of the most appropriate approaches to impart higher mechanical strength and mucoadhesion. Thiol modification of gum karaya and gum acacia was carried out by esterification with 80% thioglycolic acid. FTIR, DSC and XRD confirmed the completion of thiolation reaction. Anticancer potential of developed thiomer was studied on cervical cancer cell lines (HeLa) and more than 60% of human cervical cell lines (HeLa) were inhibited at concentration of 5 µg/100 µL. Immobilized thiol groups were found to be 0.8511 mmol/g as determined by Ellman’s method. Cytotoxicity studies on L929 fibroblast cell lines indicated thiomers were biocompatible. Bilayered tablets were prepared using Ivabradine hydrochloride as the model drug and synthesized thiolated gums as mucoadhesive polymer. Tablets prepared using thiolated polymers in combination showed more swelling, mucoadhesion and residence time as compared to unmodified gums. Thiol modification controlled the release of the drug for 24 h and enhanced permeation of the drug up to 3 fold through porcine buccal mucosa as compared to tablets with unmodified gums. Thiolated polymer showed increased mucoadhesion and permeation, anticancer potential, controlled release and thus can be utilized as a novel excipient in formulation development.
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spelling pubmed-96093012022-10-28 Improved Mucoadhesion, Permeation and In Vitro Anticancer Potential of Synthesized Thiolated Acacia and Karaya Gum Combination: A Systematic Study Munot, Neha Kandekar, Ujjwala Rikame, Chaitali Patil, Abhinandan Sengupta, Poulomi Urooj, Shabana Bilal, Anusha Molecules Article Thiolation of polymers is one of the most appropriate approaches to impart higher mechanical strength and mucoadhesion. Thiol modification of gum karaya and gum acacia was carried out by esterification with 80% thioglycolic acid. FTIR, DSC and XRD confirmed the completion of thiolation reaction. Anticancer potential of developed thiomer was studied on cervical cancer cell lines (HeLa) and more than 60% of human cervical cell lines (HeLa) were inhibited at concentration of 5 µg/100 µL. Immobilized thiol groups were found to be 0.8511 mmol/g as determined by Ellman’s method. Cytotoxicity studies on L929 fibroblast cell lines indicated thiomers were biocompatible. Bilayered tablets were prepared using Ivabradine hydrochloride as the model drug and synthesized thiolated gums as mucoadhesive polymer. Tablets prepared using thiolated polymers in combination showed more swelling, mucoadhesion and residence time as compared to unmodified gums. Thiol modification controlled the release of the drug for 24 h and enhanced permeation of the drug up to 3 fold through porcine buccal mucosa as compared to tablets with unmodified gums. Thiolated polymer showed increased mucoadhesion and permeation, anticancer potential, controlled release and thus can be utilized as a novel excipient in formulation development. MDPI 2022-10-12 /pmc/articles/PMC9609301/ /pubmed/36296425 http://dx.doi.org/10.3390/molecules27206829 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Munot, Neha
Kandekar, Ujjwala
Rikame, Chaitali
Patil, Abhinandan
Sengupta, Poulomi
Urooj, Shabana
Bilal, Anusha
Improved Mucoadhesion, Permeation and In Vitro Anticancer Potential of Synthesized Thiolated Acacia and Karaya Gum Combination: A Systematic Study
title Improved Mucoadhesion, Permeation and In Vitro Anticancer Potential of Synthesized Thiolated Acacia and Karaya Gum Combination: A Systematic Study
title_full Improved Mucoadhesion, Permeation and In Vitro Anticancer Potential of Synthesized Thiolated Acacia and Karaya Gum Combination: A Systematic Study
title_fullStr Improved Mucoadhesion, Permeation and In Vitro Anticancer Potential of Synthesized Thiolated Acacia and Karaya Gum Combination: A Systematic Study
title_full_unstemmed Improved Mucoadhesion, Permeation and In Vitro Anticancer Potential of Synthesized Thiolated Acacia and Karaya Gum Combination: A Systematic Study
title_short Improved Mucoadhesion, Permeation and In Vitro Anticancer Potential of Synthesized Thiolated Acacia and Karaya Gum Combination: A Systematic Study
title_sort improved mucoadhesion, permeation and in vitro anticancer potential of synthesized thiolated acacia and karaya gum combination: a systematic study
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9609301/
https://www.ncbi.nlm.nih.gov/pubmed/36296425
http://dx.doi.org/10.3390/molecules27206829
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