Sustained Release of Antifibrotic Nintedanib from Polymer Microparticles Reduces Dosing Frequency While Reducing Inflammation in Murine Idiopathic Pulmonary Fibrosis
Emmanuel Einyat Opolot, Filip Goshevski, Rahul Chaudhary, Jessica A. Kilgore, Noelle S. Williams, Horst A. von Recum, Amar B. Desai
TL;DR
This study explores a new drug delivery system that extends the release of Nintedanib, reducing dosing frequency and inflammation in a mouse model of lung disease.
Contribution
A sustained-release system using beta-cyclodextrin polymer microparticles for Nintedanib is proposed to improve treatment of idiopathic pulmonary fibrosis.
Findings
NTB-loaded microparticles showed sustained plasma concentrations for over 70 hours in mice.
NTB-loaded microparticles reduced pro-inflammatory markers in a bleomycin-induced IPF model.
NTB-loaded microparticles required fewer injections than the standard daily regimen.
Abstract
Idiopathic pulmonary fibrosis (IPF) is a life-threatening, progressive lung disease with limited therapeutic options, often resulting in poor patient outcomes. Current treatments, such as Nintedanib (NTB) and Pirfenidone (PFD), require frequent administration, leading to adverse effects and low patient adherence. The purpose of this study was to investigate a sustained-release drug delivery system utilizing microparticles (MPs) composed of insoluble beta-cyclodextrin (β-CD) polymers to enhance the bioavailability and extend the release of NTB and PFD. A multidisciplinary approach, including in silico modeling, in vitro assays, and in vivo studies, was employed to assess the efficacy of β-CD-polymer MPs as drug carriers. Molecular docking simulations and surface plasmon resonance studies demonstrated a stronger binding affinity of NTB to β-CD-polymer MPs compared to PFD, suggesting an…
Genes, proteins, chemicals, diseases, species, mutations and cell lines named across the full text — each resolved to its canonical identifier and authoritative record.
Click any figure to enlarge with its caption.
Figure 1
Figure 2
Figure 3
Figure 4
Figure 5
Figure 6
Figure 7
Figure 8
Figure 9Peer Reviews
No public reviews on file for this paper yet. If you reviewed it on a platform where reviews are public (OpenReview, ICLR, NeurIPS, ICML), you can paste yours below so the community can read it here.
Videos
No videos yet. Explain this paper in a talk, walkthrough, or lecture? Add one.
Taxonomy
TopicsInterstitial Lung Diseases and Idiopathic Pulmonary Fibrosis · Inhalation and Respiratory Drug Delivery · Pneumocystis jirovecii pneumonia detection and treatment