Oral squamous cell carcinoma (OSCC) is a group of highly malignant tumors that may arise from the surface epithelium or minor salivary glands. Approximately 85% to 95% of all oral cancer is squamous cell carcinoma (OSCC) which is a very aggressive cancer, representing one of the most common malignancies worldwide. Oral potentially malignant disorders (OPMDs) regroup a variegate set of different histological lesions, characterized by the potential capacity to transform in OSCC. The conventional treatment modalities of oral cancer include surgical excision, radiation therapy, chemotherapy, or a combination of these approaches. These traditional methods may not use effectively due to their poor bioavailability. Hence, reformulation of drugs or improved drug delivery may enhance bioavailability. Targeted therapy is a novel approach to deliver drugs to specific cells, organs, cell organelles to improve the collection of the delivered active components in the desired site of action and decrease the side effects and systematic toxicity that accompanied conventional therapy. Nanodentistry uses nanotechnological approaches with a particle size of 10-9 meters including nondiagnostic, nanoparticles, and nanodrugs for diagnosing, treatment, and prevention of oral and dental diseases to improve dental health. This review describes different nanoparticles accompanied by therapeutic agents for effective and useful diagnosis and treatment of oral cancer.