There are many types of diseases associated with the oral cavity. As an adjunct to professional oral dental care, various drug delivery systems have been developed to improve the treatment or prevention of these diseases. In this manuscript, the current status of drug delivery strategies for these common orofacial diseases is reviewed. Biomineral-binding drug delivery and on-demand drug release are suggested to be considered in the future design of drug delivery systems for orofacial diseases. Apparently, this research field deserves much more attention from both pharmaceutical scientists and dental health professionals.