Cancer is among the leading causes of death worldwide, causing a significant rise in mortality and morbidity. In this regard, nanotechnology gained a plethora of attention from researchers, owing to its nano-size and larger surface area, leading to one of the most effective drug delivery systems for chemotherapeutic agents. Indeed, they enhance the bioavailability and targeting of antitumor drugs. The formulations developed utilizing nanotechnology have been used for a long to deliver anticancer drugs. Still, they greatly suffered from several restrictions to effectively deliver the incorporated drug at the specific site. Recently, an advanced technique of developing Surface Modified Nanocarriers (SMN) addressed the shortcomings of older nanotechnology-based formulations. Specifically, ligands or other conjugates attached to the nanocarriers for targeting site-specific tumor/s have been more successful in offering site-specific drug targeting and reducing cell toxicity coupled with prolonged and sustained drug delivery.<br>