Oral cancer is a common malignant life-threatening tumor. Despite some advances in traditional therapy, mortality and mobidity rates are high due to delayed diagnosis and ineffective treatment. Additionally, some patients inevitably suffer from various fatal adverse effects during the course of therapy. Therefore, it is imperative to develop novel methods to eradicate oral cancer cells with minimal adverse effects on normal cells. Nanotechnology is a promising and novel vehicle for the diagnosis and treatment of oral cancer with encouraging recent achievements. In this review, we present state-of-the-art nanotechnology-based drug delivery systems employed in the domain of oral cancer, especially for its enhanced diagnosis and therapy. We describe in detail the types of nanotechnology used in the management of oral cancer and summarize administration routes of nanodrugs. Finally, the potential and prospects of nanotechnology-based drug delivery systems as promising modalities of diagnosis and therapy of oral cancer are highlighted.