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Losartan Interactions with 2-Hydroxypropyl-β-CD

Losartan potassium salt (LSR) is a well-known antihypertensive drug with proven beneficial effects on human health. Its formulation with the non-toxic 2-hydroxypropyl-β-cyclodextrin (2-HP-β-CD) could improve its pharmacological profile. Thus, its molecular interactions are studied using a combinatio...

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Autores principales: Palli, Vasiliki, Leonis, Georgios, Zoupanou, Nikoletta, Georgiou, Nikitas, Chountoulesi, Maria, Naziris, Nikolaos, Tzeli, Demeter, Demetzos, Costas, Valsami, Georgia, Marousis, Konstantinos D., Spyroulias, Georgios A., Mavromoustakos, Thomas
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9027256/
https://www.ncbi.nlm.nih.gov/pubmed/35458617
http://dx.doi.org/10.3390/molecules27082421
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author Palli, Vasiliki
Leonis, Georgios
Zoupanou, Nikoletta
Georgiou, Nikitas
Chountoulesi, Maria
Naziris, Nikolaos
Tzeli, Demeter
Demetzos, Costas
Valsami, Georgia
Marousis, Konstantinos D.
Spyroulias, Georgios A.
Mavromoustakos, Thomas
author_facet Palli, Vasiliki
Leonis, Georgios
Zoupanou, Nikoletta
Georgiou, Nikitas
Chountoulesi, Maria
Naziris, Nikolaos
Tzeli, Demeter
Demetzos, Costas
Valsami, Georgia
Marousis, Konstantinos D.
Spyroulias, Georgios A.
Mavromoustakos, Thomas
author_sort Palli, Vasiliki
collection PubMed
description Losartan potassium salt (LSR) is a well-known antihypertensive drug with proven beneficial effects on human health. Its formulation with the non-toxic 2-hydroxypropyl-β-cyclodextrin (2-HP-β-CD) could improve its pharmacological profile. Thus, its molecular interactions are studied using a combination of Differential Scanning Calorimetry (DSC), Nuclear Magnetic Resonance (NMR) and Molecular Dynamics (MD). First, its complexation is shown through Differential Scanning Calorimetry as lyophilization provided distinct thermal properties in comparison to the mixture. The complexation is further proved by utilizing the chemical shift changes in the complexation and T1 values. Furthermore, the reversible favorable complexation was shown by MD calculations. Such physical chemical properties provide evidence that this formulation must be further explored through biological experiments.
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spelling pubmed-90272562022-04-23 Losartan Interactions with 2-Hydroxypropyl-β-CD Palli, Vasiliki Leonis, Georgios Zoupanou, Nikoletta Georgiou, Nikitas Chountoulesi, Maria Naziris, Nikolaos Tzeli, Demeter Demetzos, Costas Valsami, Georgia Marousis, Konstantinos D. Spyroulias, Georgios A. Mavromoustakos, Thomas Molecules Article Losartan potassium salt (LSR) is a well-known antihypertensive drug with proven beneficial effects on human health. Its formulation with the non-toxic 2-hydroxypropyl-β-cyclodextrin (2-HP-β-CD) could improve its pharmacological profile. Thus, its molecular interactions are studied using a combination of Differential Scanning Calorimetry (DSC), Nuclear Magnetic Resonance (NMR) and Molecular Dynamics (MD). First, its complexation is shown through Differential Scanning Calorimetry as lyophilization provided distinct thermal properties in comparison to the mixture. The complexation is further proved by utilizing the chemical shift changes in the complexation and T1 values. Furthermore, the reversible favorable complexation was shown by MD calculations. Such physical chemical properties provide evidence that this formulation must be further explored through biological experiments. MDPI 2022-04-08 /pmc/articles/PMC9027256/ /pubmed/35458617 http://dx.doi.org/10.3390/molecules27082421 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
Palli, Vasiliki
Leonis, Georgios
Zoupanou, Nikoletta
Georgiou, Nikitas
Chountoulesi, Maria
Naziris, Nikolaos
Tzeli, Demeter
Demetzos, Costas
Valsami, Georgia
Marousis, Konstantinos D.
Spyroulias, Georgios A.
Mavromoustakos, Thomas
Losartan Interactions with 2-Hydroxypropyl-β-CD
title Losartan Interactions with 2-Hydroxypropyl-β-CD
title_full Losartan Interactions with 2-Hydroxypropyl-β-CD
title_fullStr Losartan Interactions with 2-Hydroxypropyl-β-CD
title_full_unstemmed Losartan Interactions with 2-Hydroxypropyl-β-CD
title_short Losartan Interactions with 2-Hydroxypropyl-β-CD
title_sort losartan interactions with 2-hydroxypropyl-β-cd
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9027256/
https://www.ncbi.nlm.nih.gov/pubmed/35458617
http://dx.doi.org/10.3390/molecules27082421
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