Oral cavity carcinoma (OCC) remains an ongoing public health problem. Emerging nanotechnology provides alternative treatment approaches. This review covers the up-to-date literature in the human OCC treatment field. We explored the growing body of evidence to reveal novel and highly promising diagnostic and therapeutic applications of nanotechnology in this field. Various types of nanoparticles have been tested for applications in OCC. Imaging modalities in addition to nanocarriers are discussed. The encouraging contribution of lymphotropic nanoparticles contrast in the diagnosis of metastatic cervical lymph nodes needs to be confirmed. The development of the sentinel lymph node procedure and photodynamic therapy may lead to breakthrough therapies in order improve clinical outcomes and quality of life. In this perspective, cancer nanotechnology has the potential to revolutionize the treatment of OCC patients.