The present chapter focuses on the anticancer activity of nanocarriers at the level of the oral cavity. Oral cancers represent a subtype of head and neck cancers diagnosed in specific screenings. It specifically affects the buccal lining and adjacent structures of the oropharynx, determining a high risk of mortality as cancer spreads in the body through metastasis. Oral cancer becomes a critical health problem when the diagnosis is imposed at a later stage at which only time and the onset of appropriate interventions are decisive for the prognosis. In the new era of nanoscale drug delivery systems, oral cancer therapy aims to provide targeted effects of the active ingredients by assuming improved solubility, increased bioavailability, and reduced side effects. The recent findings of the past 10 years plead for achieving localized effects and disease regression by appealing to a plethora of new nanomaterials and hybrid structures using colloid science. Microemulsions and nanoemulsions, along with metallic, magnetic, and polymeric nanoparticles are just a couple of important platforms for drug delivery, designed to entrap both natural and synthetic drugs with promising anticancer activity in such emergent oral disease.