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Molecular Dynamics and Physical Stability of Ibuprofen in Binary Mixtures with an Acetylated Derivative of Maltose
[Image: see text] In this paper, we explore the strategy increasingly used to improve the bioavailability of poorly water-soluble crystalline drugs by formulating their amorphous solid dispersions. We focus on the potential application of a low molecular weight excipient octaacetyl-maltose (acMAL) t...
Autores principales: | , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
American Chemical
Society
2020
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7467776/ https://www.ncbi.nlm.nih.gov/pubmed/32584584 http://dx.doi.org/10.1021/acs.molpharmaceut.0c00517 |
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author | Grzybowska, Katarzyna Grzybowski, Andrzej Knapik-Kowalczuk, Justyna Chmiel, Krzysztof Woyna-Orlewicz, Krzysztof Szafraniec-Szczęsny, Joanna Antosik-Rogóż, Agata Jachowicz, Renata Kowalska-Szojda, Katarzyna Lodowski, Piotr Paluch, Marian |
author_facet | Grzybowska, Katarzyna Grzybowski, Andrzej Knapik-Kowalczuk, Justyna Chmiel, Krzysztof Woyna-Orlewicz, Krzysztof Szafraniec-Szczęsny, Joanna Antosik-Rogóż, Agata Jachowicz, Renata Kowalska-Szojda, Katarzyna Lodowski, Piotr Paluch, Marian |
author_sort | Grzybowska, Katarzyna |
collection | PubMed |
description | [Image: see text] In this paper, we explore the strategy increasingly used to improve the bioavailability of poorly water-soluble crystalline drugs by formulating their amorphous solid dispersions. We focus on the potential application of a low molecular weight excipient octaacetyl-maltose (acMAL) to prepare physically stable amorphous solid dispersions with ibuprofen (IBU) aimed at enhancing water solubility of the drug compared to that of its crystalline counterpart. We thoroughly investigate global and local molecular dynamics, thermal properties, and physical stability of the IBU+acMAL binary systems by using broadband dielectric spectroscopy and differential scanning calorimetry as well as test their water solubility and dissolution rate. The obtained results are extensively discussed by analyzing several factors considered to affect the physical stability of amorphous systems, including those related to the global mobility, such as plasticization/antiplasticization effects, the activation energy, fragility parameter, and the number of dynamically correlated molecules as well as specific intermolecular interactions like hydrogen bonds, supporting the latter by density functional theory calculations. The observations made for the IBU+acMAL binary systems and drawn recommendations give a better insight into our understanding of molecular mechanisms governing the physical stability of amorphous solid dispersions. |
format | Online Article Text |
id | pubmed-7467776 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | American Chemical
Society |
record_format | MEDLINE/PubMed |
spelling | pubmed-74677762020-09-03 Molecular Dynamics and Physical Stability of Ibuprofen in Binary Mixtures with an Acetylated Derivative of Maltose Grzybowska, Katarzyna Grzybowski, Andrzej Knapik-Kowalczuk, Justyna Chmiel, Krzysztof Woyna-Orlewicz, Krzysztof Szafraniec-Szczęsny, Joanna Antosik-Rogóż, Agata Jachowicz, Renata Kowalska-Szojda, Katarzyna Lodowski, Piotr Paluch, Marian Mol Pharm [Image: see text] In this paper, we explore the strategy increasingly used to improve the bioavailability of poorly water-soluble crystalline drugs by formulating their amorphous solid dispersions. We focus on the potential application of a low molecular weight excipient octaacetyl-maltose (acMAL) to prepare physically stable amorphous solid dispersions with ibuprofen (IBU) aimed at enhancing water solubility of the drug compared to that of its crystalline counterpart. We thoroughly investigate global and local molecular dynamics, thermal properties, and physical stability of the IBU+acMAL binary systems by using broadband dielectric spectroscopy and differential scanning calorimetry as well as test their water solubility and dissolution rate. The obtained results are extensively discussed by analyzing several factors considered to affect the physical stability of amorphous systems, including those related to the global mobility, such as plasticization/antiplasticization effects, the activation energy, fragility parameter, and the number of dynamically correlated molecules as well as specific intermolecular interactions like hydrogen bonds, supporting the latter by density functional theory calculations. The observations made for the IBU+acMAL binary systems and drawn recommendations give a better insight into our understanding of molecular mechanisms governing the physical stability of amorphous solid dispersions. American Chemical Society 2020-06-25 2020-08-03 /pmc/articles/PMC7467776/ /pubmed/32584584 http://dx.doi.org/10.1021/acs.molpharmaceut.0c00517 Text en Copyright © 2020 American Chemical Society This is an open access article published under a Creative Commons Attribution (CC-BY) License (http://pubs.acs.org/page/policy/authorchoice_ccby_termsofuse.html) , which permits unrestricted use, distribution and reproduction in any medium, provided the author and source are cited. |
spellingShingle | Grzybowska, Katarzyna Grzybowski, Andrzej Knapik-Kowalczuk, Justyna Chmiel, Krzysztof Woyna-Orlewicz, Krzysztof Szafraniec-Szczęsny, Joanna Antosik-Rogóż, Agata Jachowicz, Renata Kowalska-Szojda, Katarzyna Lodowski, Piotr Paluch, Marian Molecular Dynamics and Physical Stability of Ibuprofen in Binary Mixtures with an Acetylated Derivative of Maltose |
title | Molecular
Dynamics and Physical Stability of Ibuprofen
in Binary Mixtures with an Acetylated Derivative of Maltose |
title_full | Molecular
Dynamics and Physical Stability of Ibuprofen
in Binary Mixtures with an Acetylated Derivative of Maltose |
title_fullStr | Molecular
Dynamics and Physical Stability of Ibuprofen
in Binary Mixtures with an Acetylated Derivative of Maltose |
title_full_unstemmed | Molecular
Dynamics and Physical Stability of Ibuprofen
in Binary Mixtures with an Acetylated Derivative of Maltose |
title_short | Molecular
Dynamics and Physical Stability of Ibuprofen
in Binary Mixtures with an Acetylated Derivative of Maltose |
title_sort | molecular
dynamics and physical stability of ibuprofen
in binary mixtures with an acetylated derivative of maltose |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7467776/ https://www.ncbi.nlm.nih.gov/pubmed/32584584 http://dx.doi.org/10.1021/acs.molpharmaceut.0c00517 |
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