The aim of this study was to develop and optimize moronic acid-loaded nanoparticles for potential use in cancer therapy. Moronic acid, a pentacyclic triterpenoid with promising anticancer properties, suffers from poor water solubility and low bioavailability, limiting its clinical applications. To overcome these challenges, moronic acid nanoparticles were synthesized using the solvent evaporation method, with polyvinyl alcohol (PVA) as a stabilizer. Key formulation variables, including moronic acid concentration, PVA concentration, and homogenization speed, were systematically optimized using response surface methodology (RSM) to achieve nanoparticles with optimal size, polydispersity index (PDI), encapsulation efficiency, and drug loading efficiency. The optimized formulation achieved a particle size of 120 nm, a PDI of 0.18, an encapsulation efficiency of 90%, and a drug loading efficiency of 45%, which are ideal for effective drug delivery. The nanoparticles demonstrated a uniform size distribution and stability, ensuring predictable drug release. MTT assay results showed dose dependent cytotoxicity of the nanoparticles against HeLa, MCF-7, and A549 cancer cell lines, with the highest sensitivity observed in A549 cells. These findings suggest that moronic acid nanoparticles are a promising drug delivery system for cancer therapy, enhancing solubility, bioavailability, and therapeutic efficacy. This study demonstrates the successful encapsulation of moronic acid into nanoparticles and highlights the importance of optimizing formulation parameters for achieving stable, effective nanoparticle-based drug delivery systems. Future work should focus on in vivo studies to evaluate the therapeutic potential and safety of these nanoparticles in cancer treatment.