The buccal route offers an alternative for drug administration due to its advantages, including the avoidance of the gastrointestinal tract, the hepatic first-pass, enzymatic degradation and chemical instability of certain molecules that would pose a challenge to formulate orally. Moreover, the oral cavity has a lower enzyme content than the rest of the gastrointestinal tract, predictable transit times, easy administration, and provides the opportunity to readily halt drug administration. Additionally, the oral cavity is an organized system with stratified epithelium that allows manufacturing of pharmaceutical forms for drug delivery.

Due to the possibilities offered by this route, recent research efforts have been conducted towards the use of nanotechnology to enable buccal drug delivery. In this chapter, we discuss the anatomy of the oral cavity, relevant characteristics of the epithelium to drug delivery and delivery system permeation, types of nanocarriers that have been reported to-date and toxicity studies addressing nanotechnology.