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Pulmonary Delivery of Inhalable Sustained Release Nanocomposites Microparticles Encapsulating Osimertinib for
Iman M Alfagih1, Alanood Almurshedi1, Basmah Aldosari1
1Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
Pharmaceutics
|January 28, 2026
Summary
A novel dry powder inhalable formulation of Osimertinib (OSI) was developed for non-small cell lung cancer (NSCLC). This targeted delivery method enhances efficacy and reduces systemic toxicity compared to oral administration.
Area of Science:
- Pharmaceutical Technology
- Nanotechnology
- Oncology
Background:
- Osimertinib (OSI) is a key treatment for non-small cell lung cancer (NSCLC).
- Oral OSI administration has limitations including poor tumor targeting and significant systemic toxicity.
- Developing inhaled formulations offers a promising alternative for improved lung cancer therapy.
Purpose of the Study:
- To create and assess a novel dry powder inhalable formulation of Osimertinib (OSI).
- The formulation aims to achieve targeted delivery to lung tumors and minimize systemic side effects.
- This represents the first study on an inhaled dry powder formulation of OSI.
Main Methods:
- Chitosan-coated PLGA nanoparticles (PLGA-C NPs) encapsulating OSI were fabricated using emulsion-solvent evaporation.
- Respirable nanocomposite microparticles (NCMPs) were formed by spray-drying PLGA-C NPs with L-leucine.
- Characterization included particle size, zeta potential, encapsulation efficiency, in vitro cell studies, aerosolization, stability, and drug release.
Main Results:
- PLGA-C NPs showed optimal size (145.18 ± 3.0 nm), high encapsulation efficiency, and positive zeta potential.
- In vitro studies revealed a 3.6-fold lower IC50 for OSI-loaded NPs, with enhanced anti-migratory effects and cell cycle arrest.
- NCMPs demonstrated excellent aerosolization properties (MMAD 1.09 ± 0.23 μm, FPF 73.48 ± 8.6%) and sustained release (61.76 ± 3.9% at 24h).
Conclusions:
- The developed dry powder inhalable OSI formulation shows potential for improved therapeutic outcomes in NSCLC.
- This targeted delivery approach may significantly reduce systemic toxicity associated with oral OSI.
- This novel formulation offers a promising advancement in lung cancer treatment delivery.
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