Cancer is an epidemic and undoubtedly one of the leading causes of death in the present day. There are quite a few conventional treatments methods- chemotherapy, radiotherapy and surgical removal which have proven to be effective considering the results. However, the side effects of such treatments are profound and chances of reoccurrence are always on the cards. Thus, there comes the need for alternative methods of cancer treatment. Medicinal herbs utilized in the form of phytochemicals may offer the answer to this loophole as they are known to possess minimal side effects with good anticancer activity. Several phytochemicals have been studied and found to exhibit anticancer activity; however, their efficiency has been limited due to poor bioavailability. Polymeric nanoparticles (PNPs) may offer resort to this limitation, providing protection against harsh physiological conditions and enhancing efficiency of phytochemicals by sustained release property. A number of biocompatible and biodegradable polymers have been employed as nanocarriers for drug delivery. In this article, we have discussed different phytochemicals, their anticancer activity and molecular targets in certain cancer cells. In addition, the various types of polymers and methods used in the fabrication of phytochemical-loaded PNPs (PL-PNPs) have been discussed. The physicochemical properties of these nanoparticles such as polydispersity index, size, zeta potential, and release profile in different pH have been highlighted. Moreover, the anticancer activities of the PL-PNPs have been compared with that of pristine phytochemicals. Although there are a number of known anticancer phytochemicals, a vast multitude of natural products remain unexplored which can be harnessed in the future.