Effect of Experimental Temperature on the Permeation of Model Diffusants Across Porcine Buccal Mucosa

• Published in: AAPS PharmSciTech 2011-06, Vol.12 (2), p.579-586
• Main Authors: Kulkarni, Upendra Dilip, Mahalingam, Ravichandran, Li, Xiaoling, Pather, Indiran, Jasti, Bhaskara
• Format: Article
• Language: English
• Subjects: Administration, Buccal; Animals; Biochemistry; Biomedical and Life Sciences; Biomedicine; Biotechnology; Diffusion; Indexing in process; Mouth Mucosa - drug effects; Mouth Mucosa - metabolism; Organ Culture Techniques - standards; Permeability; Pharmaceutical Preparations - administration & dosage; Pharmaceutical Preparations - metabolism; Pharmaceutical Preparations - standards; Pharmacology/Toxicology; Pharmacy; Research Paper; Swine; Temperature
• ISSN: 1530-9932; 1530-9932
• DOI: 10.1208/s12249-011-9624-z

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.