Background Phytochemicals encompass a diverse array of bioactive substances originating from plants, exhibiting a broad spectrum of possible health-promoting effects. Nonetheless, the clinical uses of these compounds are restricted due to their limited solubility, stability, bioavailability, and target selectivity. Nanotechnology-based delivery methods present a viable approach to address these problems and enhance the properties and biological activity of phytochemicals. Nanoformulations have the potential to augment the solubility, bioavailability, and pharmacokinetics of phytochemicals by means of several methods. One potential approach to enhance the surface area and solubility of phytochemicals is by lowering their particle size. The process of adsorption of surfactants onto phytochemical particles can lead to the formation of micelles, which exhibit solubility in water. Nanoformulations have the potential to enhance the uptake of phytochemicals across many biological barriers, including the intestinal epithelium. Objective To study the potential of nanoformulation in enhancing the therapeutic action of phytochemicals Method Systemic review was performed while considering some aspects of PRISM guidelines. Result The nanoparticles have a great potential in delivering the phytochemicals and could of great help in the management of various diseases. Although, exhaustive research and clinical trials are yet demanded to provide the evidential proof for the same. Conclusion In conclusion, the utilisation of ligand-functionalized nanoparticles enables the precise targeting of phytochemicals to particular cells or tissues. The field of nanotechnology has significant promise in transforming the advancement and administration of phytochemicals for medicinal and preventative applications. The utilisation of nanotechnology holds promise in addressing the obstacles related to the physicochemical characteristics of phytochemicals, hence enabling the development of enhanced and precise delivery systems for these advantageous molecules.