Journal
AAPS PHARMSCITECH
Volume 12, Issue 2, Pages 579-586Publisher
SPRINGER
DOI: 10.1208/s12249-011-9624-z
Keywords
activation energy; permeability enhancement; porcine buccal mucosa; temperature
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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 7A degrees 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.
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