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Polymer Microparticles Prolong Delivery of the 15-PGDH Inhibitor SW033291
As the prevalence of age-related fibrotic diseases continues to increase, novel antifibrotic therapies are emerging to address clinical needs. However, many novel therapeutics for managing chronic fibrosis are small-molecule drugs that require frequent dosing to attain effective concentrations. Alth...
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/PMC8779392/ https://www.ncbi.nlm.nih.gov/pubmed/35056981 http://dx.doi.org/10.3390/pharmaceutics14010085 |
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author | Dogan, Alan B. Rohner, Nathan A. Smith, Julianne N. P. Kilgore, Jessica A. Williams, Noelle S. Markowitz, Sanford D. von Recum, Horst A. Desai, Amar B. |
author_facet | Dogan, Alan B. Rohner, Nathan A. Smith, Julianne N. P. Kilgore, Jessica A. Williams, Noelle S. Markowitz, Sanford D. von Recum, Horst A. Desai, Amar B. |
author_sort | Dogan, Alan B. |
collection | PubMed |
description | As the prevalence of age-related fibrotic diseases continues to increase, novel antifibrotic therapies are emerging to address clinical needs. However, many novel therapeutics for managing chronic fibrosis are small-molecule drugs that require frequent dosing to attain effective concentrations. Although bolus parenteral administrations have become standard clinical practice, an extended delivery platform would achieve steady-state concentrations over a longer time period with fewer administrations. This study lays the foundation for the development of a sustained release platform for the delivery of (+)SW033291, a potent, small-molecule inhibitor of the 15-hydroxyprostaglandin dehydrogenase (15-PGDH) enzyme, which has previously demonstrated efficacy in a murine model of pulmonary fibrosis. Herein, we leverage fine-tuned cyclodextrin microparticles—specifically, β-CD microparticles (β-CD MPs)—to extend the delivery of the 15-PGDH inhibitor, (+)SW033291, to over one week. |
format | Online Article Text |
id | pubmed-8779392 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-87793922022-01-22 Polymer Microparticles Prolong Delivery of the 15-PGDH Inhibitor SW033291 Dogan, Alan B. Rohner, Nathan A. Smith, Julianne N. P. Kilgore, Jessica A. Williams, Noelle S. Markowitz, Sanford D. von Recum, Horst A. Desai, Amar B. Pharmaceutics Article As the prevalence of age-related fibrotic diseases continues to increase, novel antifibrotic therapies are emerging to address clinical needs. However, many novel therapeutics for managing chronic fibrosis are small-molecule drugs that require frequent dosing to attain effective concentrations. Although bolus parenteral administrations have become standard clinical practice, an extended delivery platform would achieve steady-state concentrations over a longer time period with fewer administrations. This study lays the foundation for the development of a sustained release platform for the delivery of (+)SW033291, a potent, small-molecule inhibitor of the 15-hydroxyprostaglandin dehydrogenase (15-PGDH) enzyme, which has previously demonstrated efficacy in a murine model of pulmonary fibrosis. Herein, we leverage fine-tuned cyclodextrin microparticles—specifically, β-CD microparticles (β-CD MPs)—to extend the delivery of the 15-PGDH inhibitor, (+)SW033291, to over one week. MDPI 2021-12-30 /pmc/articles/PMC8779392/ /pubmed/35056981 http://dx.doi.org/10.3390/pharmaceutics14010085 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 Dogan, Alan B. Rohner, Nathan A. Smith, Julianne N. P. Kilgore, Jessica A. Williams, Noelle S. Markowitz, Sanford D. von Recum, Horst A. Desai, Amar B. Polymer Microparticles Prolong Delivery of the 15-PGDH Inhibitor SW033291 |
title | Polymer Microparticles Prolong Delivery of the 15-PGDH Inhibitor SW033291 |
title_full | Polymer Microparticles Prolong Delivery of the 15-PGDH Inhibitor SW033291 |
title_fullStr | Polymer Microparticles Prolong Delivery of the 15-PGDH Inhibitor SW033291 |
title_full_unstemmed | Polymer Microparticles Prolong Delivery of the 15-PGDH Inhibitor SW033291 |
title_short | Polymer Microparticles Prolong Delivery of the 15-PGDH Inhibitor SW033291 |
title_sort | polymer microparticles prolong delivery of the 15-pgdh inhibitor sw033291 |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8779392/ https://www.ncbi.nlm.nih.gov/pubmed/35056981 http://dx.doi.org/10.3390/pharmaceutics14010085 |
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