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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...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2021
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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. |
format | Online Article Text |
id | pubmed-8401298 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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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