Purpose <p>Non-small cell lung cancer (NSCLC) is the most prevalent type of lung cancer and has poor survival rates despite decades of therapeutic advances. Small-molecule tyrosine kinase inhibitors, such as erlotinib (ERL), are widely used for the treatment of primary lung tumors. However, oral administration, the predominant route, often results in suboptimal drug concentrations at the tumor site and dose-limiting systemic toxicities. The objective of this study was to improve the pharmaceutical properties of ERL by developing an inhalable polymeric micellar formulation for targeted pulmonary delivery.</p> Methods <p>A co-solvent evaporation method was employed to develop a micellar formulation of ERL composed of TPGS-<i>b</i>-PCL copolymers. The optimal formulation was characterized by high-performance liquid chromatography, dynamic light scattering, and transmission electron microscopy. The in vitro drug release and aerosol performance, through NGI, were evaluated. In vitro cytotoxicity using MTT and apoptosis assays was performed to assess the anticancer efficacy against A549 cells.</p> Results <p>The optimal ERL-loaded micelles (TPGS-<i>b</i>-PCL) exhibited a spherical shape with a mean diameter of ~ 44&#xa0;nm, high encapsulation efficiency (~ 90%), and a slightly positively charged zeta potential. ERL was released relatively slowly from the copolymers, and aerosol performance testing demonstrated favorable aerosol properties, with a mass median aerodynamic diameter &lt; 3&#xa0;μm and a fine particle fraction (FPF_&lt; 5) &gt; 80%. The feasibility study using cytotoxicity assays showed that ERL-loaded micelles achieved potent antitumor activity.</p> Conclusion <p>These findings highlight the potential of ERL-loaded TPGS-<i>b</i>-PCL for local treatment of NSCLC. Further investigation is necessary to assess the tolerability and efficacy of the inhalable ERL micellar therapy in vivo using appropriate preclinical NSCLC models.</p>