The targeting of pharmaceuticals is a rapidly evolving strategy to overcome the difficulties in therapeutic delivery, especially to the tumor site. Unlike traditional drug delivery systems, nanoparticles based compounds attain superior accretion in the tumor site by their active or passive mechanisms. Due to their exclusive properties like small size, large surface-to-volume ratio, tunable surface chemistry, and the ability to encapsulate various drugs, the nano-sized carriers provide longer circulation time; easy penetration into cellular membranes; efficient site-specific targeting. Recent advancements in polymeric- nanomedicines involve targeting of polymer-based nanoparticles (NPs), micelles, polyplexes, dendrimers, polymersomes, drug/protein conjugates and lipid hybrid systems to tumor pathological site. With different functional moieties, NPs improve the performance in terms of targetability, circulation longevity, enhanced intracellular penetration, stimuli-sensitivity, and carrier-mediated visualization. This review highlighted different preparative techniques and types of nanoparticles in the most recent developments in cancer treatment including promising opportunities in targeted; combination therapy; and other medical and biomedical applications. Various delivery strategies and future prospects of nanoparticles are also enlisted. Apart from that, the review discusses the potential advances and targeting of polymeric nanocarriers within the scope of cancer therapeutic system to emphasize it as an auxiliary tool to the customary drug delivery systems.