Druvasarika Barji, Suyash M. Patil, Nitesh K. Kunda
Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John’s University, Jamaica, NY 11439, USA
Summary
Pulmonary delivery of cancer therapeutics has a huge untapped potential for the treatment of lung cancer. Inhalable polymeric nanoparticles are an attractive strategy as they provide localized delivery of drug with minimal systemic adverse effects. In this study, Dacomitinib (DMB), a second-generation tyrosine kinase inhibitor (TKI) used in the treatment EGFR (epidermal growth factor receptor) mutant non-small cell lung cancer (NSCLC),was developed as an inhalable polymeric nanoparticle formulation. Dacomitinib has been successfully encapsulated into nanoparticles (NPs)s resulting in a size of 202 ± 32.5 nm with a PDI of 0.183 ± 0.061, and zetapotential of −19.39 ± 2.50 mV. The NPs exhibited an entrapment efficiency of 55.06 ± 6.3% and a drug loading of 27 ± 0.01%. With respect to in vitro drug release, the DMB-NPs showed sustained drug release with cumulative release of 39.2 ± 7.5% over 5 days. Moreover, DMB-NPs demonstrated efficient lung deposition with mass median aerodynamic diameter of 3.77 ± 0.17 μm and fine particle fraction of 80.86 ± 1.02%.
Key Message
This study reported the formulation development of polymeric dacomitinib nanoparticles for NSCLC treatment with optimum particle characteristics and excellent in vitro aerosol performance.