Abstract
The sublingual and buccal routes of administration have significant advantages for both local and systemic drug delivery. They have shown to be an effective alternative to the traditional oral route, especially when fast onset of action is required. Drugs can be rapidly and directly absorbed into the systemic circulation via venous drainage to the superior vena cava. Therefore, they are useful for drugs that undergo high hepatic clearance or degradation in the gastrointestinal tract, and for patients that have swallowing difficulties. Drugs administered via the sublingual and buccal routes are traditionally formulated as solid dosage forms (e.g., tablets, wafers, films, and patches), liquid dosage forms (e.g., sprays and drops), and semi-solid dosage forms (e.g., gels). Conventional dosage forms are commonly affected by physiological factors, which can reduce the contact of the formulation with the mucosa and lead to unpredictable drug absorption. There have been a number of advances in formulation development to improve the retention and absorption of drugs in the buccal and sublingual regions. This review will focus on the physiological aspects that influence buccal and sublingual drug delivery and the advances in nanoparticulate drug delivery approaches for sublingual and buccal administration. The clinical development pipeline with formulations approved and in clinical trials will also be addressed.
Highlights
Drugs are generally administered in the oral cavity to either treat local conditions or for the systemic absorption of drugs
For effective drug delivery via the sublingual or buccal route of administration, several physiological factors should be considered in drug formulation design and development
Conventional dosage forms are commonly affected by physiological factors, which can reduce the contact of the formulation with the mucosa and lead to unpredictable drug absorption
Summary
Drugs are generally administered in the oral cavity to either treat local conditions (e.g., infections and ulcers) or for the systemic absorption of drugs. The surface area of the oral mucosa is relatively small (100–200 cm2), with the sublingual and buccal regions having an estimated surface area of 26.5 ± 4.2 cm and 50.2 ± 2.9 cm, respectively (Czerkinsky and Holmgren, 2012; Kraan et al, 2014). These regions in the oral cavity are lined by non-keratinized, stratified squamous epithelium that is 100–200 μm and 8–12 cells thick in the sublingual region, and 500–800 μm and 40–50 cells thick in the buccal region (Czerkinsky and Holmgren, 2012; Kraan et al, 2014). Components from the saliva binds to the surface of the buccal and sublingual epithelium
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