Cancer is the main cause of fatality all over the world with a considerable growth rate. Many biologically active nanoplatforms are exploited for tumor treatment. Of nanodevices, hyaluronic acid (HA)‐based systems have shown to be promising candidates for cancer therapy due to their high biocompatibility and cell internalization. Herein, surface functionalization of different nanoparticles (NPs), e.g., organic‐ and inorganic‐based NPs, is highlighted. Subsequently, HA‐based nanostructures and their applications in cancer therapy are presented.