Nanoparticles with multifunctionality are being designed and formulated to overcome various limitations of drugs as well as conventional drug delivery systems. Engineered nanoparticles to specifically target cancer cells have the ability to reduce collateral damage on normal tissue due to pan-toxic effects of drugs. Pragmatic approaches are in consideration to make advancement in cancer therapy as the new developed methods exhibited an improved targeted anticancer therapeutic delivery with better treatment outcomes. An effective cancer therapy requires both the passive and active targeting, along with a consistent knowledge of various physiologic barriers to successfully achieve targeted delivery. The nanoparticles can be linked with tumor targeting moieties like specific ligands, monoclonal antibodies, and carbohydrates for active targeting of cancer cells with great affinity and precision. This review presents some recent research on targeted delivery for cancer therapy and also discusses examples of types of engineered nanoparticles exploited for active cancer targeting.