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...

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Published in:Pharmaceutics 2021-12, Vol.14 (1), p.85
Main Authors: 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
Format: Article
Language:eng
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Summary: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.
ISSN:1999-4923
1999-4923