Nutraceuticals are the bioactive chemical compounds, obtained from natural sources, having profound pharmacological activities. The well known phyto-ingredients with fantastic anticancer potential (e.g., curcumin, resveratrol, quercetin, genistein, and epigallocatechin gallate) have been encapsulated in biocompatible and biodegradable polymeric nanoparticles. Currently, anticancer nutraceuticals loaded in biodegradable polymeric nanoparticles demonstrate extraordinary results, revealing maximum solubility, absorption, bioavailability, and anticancer potential in comparison to nutraceuticals alone or in other drug delivery systems. Among these nutraceuticals, curcumin has been extensively studied and established as having optimal anticancer effects after integration in biocompatible and biodegradable polymeric nanoparticles.