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Amorphization and modified release of ibuprofen by post-synthetic and solvent-free loading into tailored silica aerogels
Promising active pharmaceutical ingredients (APIs) often exhibit poor aqueous solubility and thus a low bioavailability that substantially limits their pharmaceutical application. Hence, efficient formulations are required for an effective translation into highly efficient drug products. One strateg...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Taylor & Francis
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9291651/ https://www.ncbi.nlm.nih.gov/pubmed/35838584 http://dx.doi.org/10.1080/10717544.2022.2092237 |
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author | Zarinwall, Ajmal Maurer, Viktor Pierick, Jennifer Oldhues, Victor Marcus Porsiel, Julian Cedric Finke, Jan Henrik Garnweitner, Georg |
author_facet | Zarinwall, Ajmal Maurer, Viktor Pierick, Jennifer Oldhues, Victor Marcus Porsiel, Julian Cedric Finke, Jan Henrik Garnweitner, Georg |
author_sort | Zarinwall, Ajmal |
collection | PubMed |
description | Promising active pharmaceutical ingredients (APIs) often exhibit poor aqueous solubility and thus a low bioavailability that substantially limits their pharmaceutical application. Hence, efficient formulations are required for an effective translation into highly efficient drug products. One strategy is the preservation of an amorphous state of the API within a carrier matrix, which leads to enhanced dissolution. In this work, mesoporous silica aerogels (SA) were utilized as a carrier matrix for the amorphization of the poorly water-soluble model drug ibuprofen. Loading of tailored SA was performed post-synthetically and solvent-free, either by co-milling or via the melting method. Thorough analyses of these processes demonstrated the influence of macrostructural changes during the drying and grinding process on the microstructural properties of the SA. Furthermore, interfacial SA-drug interaction properties were selectively tuned by attaching terminal hydrophilic amino- or hydrophobic methyl groups to the surface of the gel. We demonstrate that not only the chemical surface properties of the SA, but also formulation-related parameters, such as the carrier-to-drug ratio, as well as process-related parameters, such as the drug loading method, decisively influence the ibuprofen adsorption efficiency. In addition, the drug-loaded SA formulations exhibited a remarkable physical stability over a period of 6 months. Furthermore, the release behavior is shown to change considerably with different surface properties of the SA matrix. Hence, the reported results demonstrate that utilizing specifically processed and modified SA offers a compelling technique for enhancement of the bioavailability of poorly-water soluble APIs and a versatile adjustment of their release profile. |
format | Online Article Text |
id | pubmed-9291651 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | Taylor & Francis |
record_format | MEDLINE/PubMed |
spelling | pubmed-92916512022-07-19 Amorphization and modified release of ibuprofen by post-synthetic and solvent-free loading into tailored silica aerogels Zarinwall, Ajmal Maurer, Viktor Pierick, Jennifer Oldhues, Victor Marcus Porsiel, Julian Cedric Finke, Jan Henrik Garnweitner, Georg Drug Deliv Research Article Promising active pharmaceutical ingredients (APIs) often exhibit poor aqueous solubility and thus a low bioavailability that substantially limits their pharmaceutical application. Hence, efficient formulations are required for an effective translation into highly efficient drug products. One strategy is the preservation of an amorphous state of the API within a carrier matrix, which leads to enhanced dissolution. In this work, mesoporous silica aerogels (SA) were utilized as a carrier matrix for the amorphization of the poorly water-soluble model drug ibuprofen. Loading of tailored SA was performed post-synthetically and solvent-free, either by co-milling or via the melting method. Thorough analyses of these processes demonstrated the influence of macrostructural changes during the drying and grinding process on the microstructural properties of the SA. Furthermore, interfacial SA-drug interaction properties were selectively tuned by attaching terminal hydrophilic amino- or hydrophobic methyl groups to the surface of the gel. We demonstrate that not only the chemical surface properties of the SA, but also formulation-related parameters, such as the carrier-to-drug ratio, as well as process-related parameters, such as the drug loading method, decisively influence the ibuprofen adsorption efficiency. In addition, the drug-loaded SA formulations exhibited a remarkable physical stability over a period of 6 months. Furthermore, the release behavior is shown to change considerably with different surface properties of the SA matrix. Hence, the reported results demonstrate that utilizing specifically processed and modified SA offers a compelling technique for enhancement of the bioavailability of poorly-water soluble APIs and a versatile adjustment of their release profile. Taylor & Francis 2022-07-15 /pmc/articles/PMC9291651/ /pubmed/35838584 http://dx.doi.org/10.1080/10717544.2022.2092237 Text en © 2022 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. https://creativecommons.org/licenses/by/4.0/This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) ), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Research Article Zarinwall, Ajmal Maurer, Viktor Pierick, Jennifer Oldhues, Victor Marcus Porsiel, Julian Cedric Finke, Jan Henrik Garnweitner, Georg Amorphization and modified release of ibuprofen by post-synthetic and solvent-free loading into tailored silica aerogels |
title | Amorphization and modified release of ibuprofen by post-synthetic and solvent-free loading into tailored silica aerogels |
title_full | Amorphization and modified release of ibuprofen by post-synthetic and solvent-free loading into tailored silica aerogels |
title_fullStr | Amorphization and modified release of ibuprofen by post-synthetic and solvent-free loading into tailored silica aerogels |
title_full_unstemmed | Amorphization and modified release of ibuprofen by post-synthetic and solvent-free loading into tailored silica aerogels |
title_short | Amorphization and modified release of ibuprofen by post-synthetic and solvent-free loading into tailored silica aerogels |
title_sort | amorphization and modified release of ibuprofen by post-synthetic and solvent-free loading into tailored silica aerogels |
topic | Research Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9291651/ https://www.ncbi.nlm.nih.gov/pubmed/35838584 http://dx.doi.org/10.1080/10717544.2022.2092237 |
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