The evolution of polymer-based nanoparticle as a drug delivery carrier has greatly contributed to the development of advanced nano and micro-medicine in the past few decades. The polymer-based nanoparticles of biodegradable and biocompatible polymers such as poly (lactide-co-glycolide) and chitosan which have been approved by Food & Drug Administration and/or European Medicine Agency can particularly facilitate the maintaining of specific properties for a real transition from laboratory to the clinical oral and parental administration. This review presents an overview of the strategies of preparing polymeric nanoparticles and using them for targeting colorectal cancer. Theranostics and surface engineering aspects of nanoparticle design in colonic cancer delivery are also highlighted.