PURPOSE: To validate pig esophageal epithelium as a model for the permeability barrier of the buccal mucosa, the transport of fentanyl across the two tissues was compared in vivo. METHODS: The epithelia were separated by immersing the excised mucosae into an isotonic saline solution at 60--65 degrees C. Fentanyl was delivered as the citrate salt at a concentration of 1 or 2 mg/mL buffered at one of four pH values (between 6.0 and 7.4). RESULTS: Across both barriers, drug transport increased proportionally with concentration as expected. However, drug flux was not linearly related to the unionized fraction of the drug; indeed, fentanyl delivery was significant even when 98.5% of the drug was in the ionized form. CONCLUSIONS: Buccal and esophageal fluxes were very similar under all conditions suggesting that the esophageal epithelium is a representative tool for buccal transport studies in vitro.
PURPOSE: To validate pig esophageal epithelium as a model for the permeability barrier of the buccal mucosa, the transport of fentanyl across the two tissues was compared in vivo. METHODS: The epithelia were separated by immersing the excised mucosae into an isotonic saline solution at 60--65 degrees C. Fentanyl was delivered as the citrate salt at a concentration of 1 or 2 mg/mL buffered at one of four pH values (between 6.0 and 7.4). RESULTS: Across both barriers, drug transport increased proportionally with concentration as expected. However, drug flux was not linearly related to the unionized fraction of the drug; indeed, fentanyl delivery was significant even when 98.5% of the drug was in the ionized form. CONCLUSIONS: Buccal and esophageal fluxes were very similar under all conditions suggesting that the esophageal epithelium is a representative tool for buccal transport studies in vitro.
Authors: J B Streisand; J R Varvel; D R Stanski; L Le Maire; M A Ashburn; B I Hague; S D Tarver; T H Stanley Journal: Anesthesiology Date: 1991-08 Impact factor: 7.892
Authors: A J Hoogstraate; C Cullander; J F Nagelkerke; S Senel; J C Verhoef; H E Junginger; H E Boddé Journal: Pharm Res Date: 1994-01 Impact factor: 4.200
Authors: Verônica Santana de Freitas-Blanco; Michelle Franz-Montan; Francisco Carlos Groppo; João Ernesto de Carvalho; Glyn Mara Figueira; Luciano Serpe; Ilza Maria Oliveira Sousa; Viviane Aparecida Guilherme Damasio; Lais Thiemi Yamane; Eneida de Paula; Rodney Alexandre Ferreira Rodrigues Journal: PLoS One Date: 2016-09-14 Impact factor: 3.240