This study aims to develop and evaluate the pimozide-loaded lipid nanoparticles (LNPs) designed for the targeted treatment of non-small cell lung cancer (NSCLC). Employing the microemulsion technique, three distinct types of LNPs were synthesized: solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC), and liquid lipid carriers (LLC). These formulations were optimized in order to transform them into fine powders through spray drying. An assessment of their encapsulation efficiency (EE%), particle size, moisture sorption, surface morphology, and anti-proliferative activity against A549 lung cancer cells were evaluated.