ArticlePharmaceuticals (Basel, Switzerland)2024
Optimization and Appraisal of Nintedanib-Loaded Mixed Polymeric Micelles as a Potential Nanovector for Non-Invasive Pulmonary Fibrosis Mitigation.
Article in Pharmaceuticals (Basel, Switzerland), 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
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Who cites it
6 citing papers in PubMed.
- Unleashing innovative cross-organ fibrosis therapies by harnessing the omics revolution.JCI insight · 2026Review
- Improving the bioavailability of nintedanib by formulating inhalable ufasomes as a targeted therapy for non-small cell lung cancer.International journal of pharmaceutics: X · 2026Article
- β-Sitosterol-loaded leciplexes attenuate rheumatoid arthritis in rats by modulating JAK2/STAT3, NF-κB, and p38 MAPK signaling pathways.Naunyn-Schmiedeberg's archives of pharmacology · 2026Article
- Repurposing losartan potassium against rheumatoid arthritis via transdermally-delivered leciplexes: Accentuated efficacy through modulation of angiotensin II/AT1R/AT2R axis.International journal of pharmaceutics: X · 2025Article
- A Microemulsion for Oral Delivery of Nintedanib - QbD-Enabled Formulation Development, In-Vitro Characterization & In-Vivo Pharmacokinetic Assessment.The AAPS journal · 2025Article
- Hyaluronic acid-coated capecitabine nanostructures for CD44 receptor-mediated targeting in breast cancer therapy.RSC advances · 2025Article
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Authors and funding
5 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
BACKGROUND/
objectivesNintedanib (NTD), a triple tyrosine kinase receptor inhibitor, is the recommended first-line tackling option for idiopathic pulmonary fibrosis (IPF). Nevertheless, the adequacy of NTD is curtailed by issues associated with its low solubility, first-pass effect, poor bioavailability, and liver toxicity. The objective of our work was to develop a non-invasive intratracheal (i.t.) nanoparadigm based on NTD-loaded polymeric mixed micelles (NTD-PMMs) that can effectively treat IPF by sustaining the release of NTD, and snowballing its bioavailability, solubility, and efficacy.
methodsDesign-Expert
resultsThe formulation composition with 309.217 mg of Soluplus, 150 mg of Tween 80, and 40 mg of sodium deoxycholate was found to fulfill the requisites of an optimum NTD-PMMs formulation. The optimum NTD-PMMs formulation divulged 90.26% entrapment efficiency with a surface charge of -14.72 mV and a nanoscale diameter of 61.36 nm. Also, it substantially sustained the release of NTD by 66.84% after 24 h and manifested a pronounced stability. In vivo histopathology investigations verified the safety of NTD-PMMs delivered intratracheally. Moreover, pharmacokinetic analyses disclosed accentuated relative bioavailability of the optimized NTD-PMMs by 2.4- and 3.82-fold as compared with both the i.t. and oral crude NTD suspensions, respectively.
conclusionsOverall, the current results elicited the potential of PMMs to serve as a promising pulmonary nanovector for the targeted delivery of NTD.
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