Cyclodextrin Complexation as a Way of Increasing the Aqueous Solubility and Stability of Carvedilol

We studied the effect of several CDs on carvedilol’s solubility and chemical stability in various aqueous media. Our present results show that it is possible to achieve a carvedilol concentration of 5 mg/mL (12.3 mM) in the presence of 5 eq of γCD or RAMEB in an aqueous medium with an acceptable aci...

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Autores principales: Rigaud, Sébastien, Mathiron, David, Moufawad, Tarek, Landy, David, Djedaini-Pilard, Florence, Marçon, Frédéric
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8620534/
https://www.ncbi.nlm.nih.gov/pubmed/34834163
http://dx.doi.org/10.3390/pharmaceutics13111746
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author Rigaud, Sébastien
Mathiron, David
Moufawad, Tarek
Landy, David
Djedaini-Pilard, Florence
Marçon, Frédéric
author_facet Rigaud, Sébastien
Mathiron, David
Moufawad, Tarek
Landy, David
Djedaini-Pilard, Florence
Marçon, Frédéric
author_sort Rigaud, Sébastien
collection PubMed
description We studied the effect of several CDs on carvedilol’s solubility and chemical stability in various aqueous media. Our present results show that it is possible to achieve a carvedilol concentration of 5 mg/mL (12.3 mM) in the presence of 5 eq of γCD or RAMEB in an aqueous medium with an acceptable acid pH (between 3.5 and 4.7). Carvedilol formed 1:1 inclusion complexes but those with RAMEB appear to be stronger (K = 317 M(−1) at 298 K) than that with γCD (K = 225 M(−1) at 298 K). The complexation of carvedilol by RAMEB significantly increased the drug’s photochemical stability in aqueous solution. These results might constitute a first step towards the development of a novel oral formulation of carvedilol.
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spelling pubmed-86205342021-11-27 Cyclodextrin Complexation as a Way of Increasing the Aqueous Solubility and Stability of Carvedilol Rigaud, Sébastien Mathiron, David Moufawad, Tarek Landy, David Djedaini-Pilard, Florence Marçon, Frédéric Pharmaceutics Article We studied the effect of several CDs on carvedilol’s solubility and chemical stability in various aqueous media. Our present results show that it is possible to achieve a carvedilol concentration of 5 mg/mL (12.3 mM) in the presence of 5 eq of γCD or RAMEB in an aqueous medium with an acceptable acid pH (between 3.5 and 4.7). Carvedilol formed 1:1 inclusion complexes but those with RAMEB appear to be stronger (K = 317 M(−1) at 298 K) than that with γCD (K = 225 M(−1) at 298 K). The complexation of carvedilol by RAMEB significantly increased the drug’s photochemical stability in aqueous solution. These results might constitute a first step towards the development of a novel oral formulation of carvedilol. MDPI 2021-10-20 /pmc/articles/PMC8620534/ /pubmed/34834163 http://dx.doi.org/10.3390/pharmaceutics13111746 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
Rigaud, Sébastien
Mathiron, David
Moufawad, Tarek
Landy, David
Djedaini-Pilard, Florence
Marçon, Frédéric
Cyclodextrin Complexation as a Way of Increasing the Aqueous Solubility and Stability of Carvedilol
title Cyclodextrin Complexation as a Way of Increasing the Aqueous Solubility and Stability of Carvedilol
title_full Cyclodextrin Complexation as a Way of Increasing the Aqueous Solubility and Stability of Carvedilol
title_fullStr Cyclodextrin Complexation as a Way of Increasing the Aqueous Solubility and Stability of Carvedilol
title_full_unstemmed Cyclodextrin Complexation as a Way of Increasing the Aqueous Solubility and Stability of Carvedilol
title_short Cyclodextrin Complexation as a Way of Increasing the Aqueous Solubility and Stability of Carvedilol
title_sort cyclodextrin complexation as a way of increasing the aqueous solubility and stability of carvedilol
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8620534/
https://www.ncbi.nlm.nih.gov/pubmed/34834163
http://dx.doi.org/10.3390/pharmaceutics13111746
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