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Chitosan as Valuable Excipient for Oral and Topical Carvedilol Delivery Systems

Chitosan is a valued excipient due to its biocompatibility properties and increasing solubility of poorly water-soluble drugs. The research presented in this paper concerns the preparation of binary combinations of chitosan (deacetylated chitin) with carvedilol (beta-blocker) to develop a formulatio...

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Autores principales: Sip, Szymon, Paczkowska-Walendowska, Magdalena, Rosiak, Natalia, Miklaszewski, Andrzej, Grabańska-Martyńska, Katarzyna, Samarzewska, Karolina, Cielecka-Piontek, Judyta
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8401298/
https://www.ncbi.nlm.nih.gov/pubmed/34451809
http://dx.doi.org/10.3390/ph14080712
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author Sip, Szymon
Paczkowska-Walendowska, Magdalena
Rosiak, Natalia
Miklaszewski, Andrzej
Grabańska-Martyńska, Katarzyna
Samarzewska, Karolina
Cielecka-Piontek, Judyta
author_facet Sip, Szymon
Paczkowska-Walendowska, Magdalena
Rosiak, Natalia
Miklaszewski, Andrzej
Grabańska-Martyńska, Katarzyna
Samarzewska, Karolina
Cielecka-Piontek, Judyta
author_sort Sip, Szymon
collection PubMed
description Chitosan is a valued excipient due to its biocompatibility properties and increasing solubility of poorly water-soluble drugs. The research presented in this paper concerns the preparation of binary combinations of chitosan (deacetylated chitin) with carvedilol (beta-blocker) to develop a formulation with a modified carvedilol release profile. As part of the research, six physical mixtures of chitosan with carvedilol were obtained and identified by spectral (PXRD, FT-IR, and Raman), thermal (DSC), and microscopic (SEM) methods. The next stage of the research estimated the profile changes and the dissolution rate for carvedilol in the obtained drug delivery systems; the reference sample was pure carvedilol. The studies were conducted at pH = 1.2 and 6.8, simulating the gastrointestinal tract conditions. Quantitative changes of carvedilol were determined using the developed isocratic UHPLC-DAD method. Established apparent permeability coefficients proved the changes in carvedilol’s permeability after introducing a drug delivery system through membranes simulating the gastrointestinal tract and skin walls. A bioadhesive potential of carvedilol–chitosan systems was confirmed using the in vitro model. The conducted research and the obtained results indicate a significant potential of using chitosan as an excipient in modern oral or epidermal drug delivery systems of carvedilol.
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spelling pubmed-84012982021-08-29 Chitosan as Valuable Excipient for Oral and Topical Carvedilol Delivery Systems Sip, Szymon Paczkowska-Walendowska, Magdalena Rosiak, Natalia Miklaszewski, Andrzej Grabańska-Martyńska, Katarzyna Samarzewska, Karolina Cielecka-Piontek, Judyta Pharmaceuticals (Basel) Article Chitosan is a valued excipient due to its biocompatibility properties and increasing solubility of poorly water-soluble drugs. The research presented in this paper concerns the preparation of binary combinations of chitosan (deacetylated chitin) with carvedilol (beta-blocker) to develop a formulation with a modified carvedilol release profile. As part of the research, six physical mixtures of chitosan with carvedilol were obtained and identified by spectral (PXRD, FT-IR, and Raman), thermal (DSC), and microscopic (SEM) methods. The next stage of the research estimated the profile changes and the dissolution rate for carvedilol in the obtained drug delivery systems; the reference sample was pure carvedilol. The studies were conducted at pH = 1.2 and 6.8, simulating the gastrointestinal tract conditions. Quantitative changes of carvedilol were determined using the developed isocratic UHPLC-DAD method. Established apparent permeability coefficients proved the changes in carvedilol’s permeability after introducing a drug delivery system through membranes simulating the gastrointestinal tract and skin walls. A bioadhesive potential of carvedilol–chitosan systems was confirmed using the in vitro model. The conducted research and the obtained results indicate a significant potential of using chitosan as an excipient in modern oral or epidermal drug delivery systems of carvedilol. MDPI 2021-07-23 /pmc/articles/PMC8401298/ /pubmed/34451809 http://dx.doi.org/10.3390/ph14080712 Text en © 2021 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
Sip, Szymon
Paczkowska-Walendowska, Magdalena
Rosiak, Natalia
Miklaszewski, Andrzej
Grabańska-Martyńska, Katarzyna
Samarzewska, Karolina
Cielecka-Piontek, Judyta
Chitosan as Valuable Excipient for Oral and Topical Carvedilol Delivery Systems
title Chitosan as Valuable Excipient for Oral and Topical Carvedilol Delivery Systems
title_full Chitosan as Valuable Excipient for Oral and Topical Carvedilol Delivery Systems
title_fullStr Chitosan as Valuable Excipient for Oral and Topical Carvedilol Delivery Systems
title_full_unstemmed Chitosan as Valuable Excipient for Oral and Topical Carvedilol Delivery Systems
title_short Chitosan as Valuable Excipient for Oral and Topical Carvedilol Delivery Systems
title_sort chitosan as valuable excipient for oral and topical carvedilol delivery systems
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8401298/
https://www.ncbi.nlm.nih.gov/pubmed/34451809
http://dx.doi.org/10.3390/ph14080712
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