Nanotechnology and nanoscience have dominated the scientific world by providing highly functional and efficient materials to be used in every facet of day-to-day life. Such a class of functional nanomaterials is the Carbon-based nanomaterials (CBNs), which envelops the nano-dimensional materials comprised of carbon atoms possessing miraculous properties. The CBNs offer higher level performance in various biomedical applications including drug delivery, tissue engineering, wound healing, biosensing and bioimaging fields. The present chapter covers the potent application of CBNs for controlled local release of therapeutics along with its superiority over conventional drug delivery modes used for dental diseases. Various types of CBNs used for dental drug delivery are summarized and discussed in details to bring forward the vast efficacy of CBNs in dentistry, which still remains a grey area in nanoscience. The chapter includes five illustrative figures to offer better relevance with the text, for the convenience of the readers.