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Encapsulation of therapeutic drugs inside nanoparticles has become the new norm in the field of drug delivery. Nanoparticles increase the therapeutic efficacy of the drugs by providing high loading efficiencies, shielding when in circulation, ability to target tumors, enhanced accumulations, and triggered release inside tumors. Polymeric nanoparticles have seen an unprecedented growth and usage in drug delivery and diagnostics in recent decades, and have emerged as extremely promising candidates for targeted delivery owing to their tunable properties, and the flexibility to design systems which respond to external stimuli such as pH, hyperthermia, redox, ultrasound, and magnetic field. This review summarizes recent exciting developments in the field of targeted polymeric nanoparticles for delivery of anti-cancer drugs, with a particular focus on functionalization with ligands, stimuli responsive and biodegradable systems. Further a critical overview of their design principles, drug release performance, and therapeutic advantages over conventional nanoparticles is discussed.