In the recent decades, polymers are widely used as biomaterials due to their favourable properties such as good biocompatibility, easy design and preparation, structural varieties and interesting bio-mimetic character. The use of biodegradable polymeric nanoparticles (NPs) for controlled drug delivery has shown significant therapeutic potential. Concurrently, targeted delivery technologies are becoming increasingly important as a scientific area of investigation. The current review entails an in-depth discussion of biodegradable polymeric nanoparticles with respect to types, formulation aspects as well as site-specific drug targeting using various ligands modifying the surface of polymeric nanoparticles with special insights to the field of oncology. Ultimately the goal of polymeric nanoparticle drug delivery is the emergence of a nano-fabricated therapeutic drug release device with the capacity to enough hold and release of various active agents on demand.