The delivery of therapeutic agents to, or via, the oral cavity is limited by the efficient removal mechanisms that exist in this area. Lectins are proteins or glycoproteins that bind to specific sugar residues, and can, therefore, interact with the glycoconjugates present on cell surfaces or salivary mucins. Endogenous lectins could also be used as points of attachment for carbohydrate-containing delivery systems. This review considers the possibility of using lectins as targeting agents within the oral cavity and reports on some of the limited number of studies completed to date. As lectins are multifunctional molecules, the possibility of using them as both targeting and therapeutic agents is considered. Lectin-containing delivery systems are a potential innovation for targeted and prolonged therapy within the oral cavity, but considerations such as toxicity and cost will need to be addressed before their routine use becomes a reality.