Oral cancer is the 11th most common cancer in the world with a high morbidity rate. Various conventional therapies have been used for the treatment of oral cancer such as surgery, radiotherapy, and chemotherapy used either alone or in combination but these have many limitations, making them unsuitable for treating oral cancer. Nanotechnology has been emerged out as an innovative tool in the field of oral cancer which has proved to provide effective results overcoming the limitations of conventional drug therapies. This system involves a nanoparticle drug delivery system based on a targeted therapy in which therapeutic drugs or agents act on the targeted cells without affecting normal healthy cells. Literature has shown that several nanoparticles, organic and inorganic nanoparticles, have been used as the drug delivery system in different types of oral cancers such as oral squamous cell carcinoma, cancer of the tongue, head, and neck cancers. Drugs like cisplatin, 5-fluorouracil, methotrexate, doxorubicin, etc., when coated with nano-polymers have shown better results compared with conventional drugs in oral cancer. Other nanoparticles such as liposomes, hydrogels, nanodiamonds, carbon rods, etc. have also been used with minimal side effects. This paper aims to review and discuss various nanotechnology systems in the field of oral cancer and to evaluate the efficacy of these systems in treating oral cancer compared with conventional drug delivery methods.