ABSTRACT
INTRODUCTION: There have been several advances in the delivery of drugs through the buccal mucosa over the last 5 years, which have resulted in a number of new buccal delivery products appearing on the market. AREAS COVERED: This review discusses the most recent developments in the area of buccal and sublingual drug delivery, with a focus on marketed drugs. Likely future directions are also considered and reported. EXPERT OPINION: The future potential of buccal and sublingual delivery systems looks favorable. It is envisaged that in the future, buccal and sublingual delivery technologies will provide a platform for the successful delivery of vaccines and antigens. It is also foreseen that physical means of enhancing drug uptake (e.g., sonophoresis, iontophoresis and electroporation) will be commercialized for buccal delivery, thereby expanding the current drug candidate list for this area. The formulation of delivery systems for photosensitizers in photodynamic therapy is a potential emerging area, while buccal and sublingual delivery, in general, is attractive for the development of intellectual property.
Subject(s)
Drug Delivery Systems , Mouth Mucosa/metabolism , Administration, Buccal , Administration, Sublingual , Animals , Cheek , Chemistry, Pharmaceutical , Drug Delivery Systems/trends , Electroporation , Humans , Iontophoresis , VaccinesABSTRACT
The influence of experimental temperature on the permeability of model diffusants across porcine buccal mucosa was investigated in vitro. The permeability increased significantly as the experimental temperature was increased in increments of approximately 7°C. It was observed that the apparent permeability and temperature were related by an exponential relationship that conformed to the Arrhenius equation. Diffusants with higher lipophilicities--buspirone and bupivacaine--had lower activation energies for diffusion when compared to hydrophilic diffusants--antipyrine and caffeine. The activation energy for diffusion of the model diffusants decreased linearly with increasing distribution coefficients across porcine buccal mucosa. The results suggested that the buccal mucosa acts as a stronger barrier to the diffusion of hydrophilic diffusants than the lipophilic ones. The log-linear relationship between permeability and temperature indicates that temperature should be carefully controlled in diffusion experiments. These results also point to the possibility of developing heat-generating buccal delivery devices, especially for hydrophobic diffusants.
Subject(s)
Mouth Mucosa/metabolism , Pharmaceutical Preparations/administration & dosage , Pharmaceutical Preparations/metabolism , Temperature , Administration, Buccal , Animals , Diffusion , Mouth Mucosa/drug effects , Organ Culture Techniques/standards , Permeability , Pharmaceutical Preparations/standards , SwineABSTRACT
Porcine buccal mucosa has been used as an in vitro model to assess the potential of delivering a molecule via the transbuccal route. However, permeation studies across porcine buccal mucosa show high variability due to various experimental and biological factors. The variability associated with the use of different mucosal regions, tissue storage conditions and tissue processing methods on drug permeation was investigated in this study. The permeability of model diffusants was significantly higher in the region behind the lip when compared to the cheek region because the latter has a thicker epithelium. Porcine buccal mucosa retained its integrity in Kreb's bicarbonate ringer solution at 4 degrees C for 24 h while many other storage conditions resulted in loss of epithelial integrity. Separation of the epithelium from underlying connective tissue either surgically or by heat treatment resulted in an epithelial thickness of approximately 150 microm. Separation of epithelium from the underlying connective tissue by heat treatment did not adversely affect its permeability and integrity characteristics. Investigation of these important biological and experimental variables provides guidance for conducting in vitro transbuccal permeation studies.
