Ferulic acid (FA), a phenolic compound abundant in the cell walls of seeds, leaves, and roots of various fruits, vegetables, cereals, and grains, is renowned for its wide range of biological activities, including antioxidant, anti-inflammatory, antimicrobial, and anticancer properties. Despite its therapeutic potential, the clinical application of FA is hindered by challenges such as poor water solubility, limited bioavailability, rapid metabolism, and instability under physiological conditions. To address these issues, nanotechnology has emerged as a transformative approach, enhancing FA's pharmacokinetic profile. Various nanoparticle-based systems, including polymer-based and lipid-based nanoparticles, have been developed to encapsulate FA. These systems have demonstrated significant improvements in FA's solubility, stability, and bioavailability, with studies showing enhanced antioxidant activity and controlled release profiles. Further, the surface engineering of these nanoparticles provides targeted drug/phytochemical delivery potential. The targeted delivery of drugs/phytochemicals significantly enhances the therapeutic efficacy and minimizes systemic side effects. This review explores the therapeutic potential of FA, the limitations in its clinical application, and the advancements in nanoparticle-based delivery systems that are paving the way for its effective therapeutic use.