Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Biomimetic Artificial Membrane Permeability Assay over Franz Cell Apparatus Using BCS Classified Drugs

Version 1 : Received: 8 September 2020 / Approved: 9 September 2020 / Online: 9 September 2020 (10:25:54 CEST)

A peer-reviewed article of this Preprint also exists.

de Souza Teixeira, L.; Vila Chagas, T.; Alonso, A.; Gonzalez-Alvarez, I.; Bermejo, M.; Polli, J.; Rezende, K.R. Biomimetic Artificial Membrane Permeability Assay over Franz Cell Apparatus Using BCS Model Drugs. Pharmaceutics 2020, 12, 988. de Souza Teixeira, L.; Vila Chagas, T.; Alonso, A.; Gonzalez-Alvarez, I.; Bermejo, M.; Polli, J.; Rezende, K.R. Biomimetic Artificial Membrane Permeability Assay over Franz Cell Apparatus Using BCS Model Drugs. Pharmaceutics 2020, 12, 988.

Journal reference: Pharmaceutics 2020, 12, 988
DOI: 10.3390/pharmaceutics12100988

Abstract

A major parameter controlling the extent and rate of oral drug absorption is permeability through the lipid bilayer of intestinal epithelial cells. Here, a biomimetic artificial membrane permeability assay (Franz-Bampa) was validated using Franz cells apparatus. Both high and low permeability drugs (metoprolol and mannitol, respectively) were used as external standards. Biomimetic properties of Franz-Bampa were also characterized by electron paramagnetic resonance spectroscopy (EPR). Moreover, the permeation profile for the 14 BCS class I-IV drugs cited in the FDA guidance (including other drugs as acyclovir, cimetidine, diclofenac, ibuprofen, piroxicam, and trimethoprim) were measured across Franz-Bampa. Apparent permeability (Papp) was compared to literature fraction dose absorbed in humans (Fa%). Papp in Caco-2 cells and Corti artificial membrane were likewise compared to Fa% to assess Franz-Bampa performance. Mannitol and metoprolol Papp values across Franz-Bampa were lower (3.20 x 10-7 and 1.61 x 10-5 cm/s, respectively) than those obtained across non-impregnated membrane (2.27 x 10-5 and 2.55 x 10-5 cm/s, respectively), confirming lipidic barrier resistivity. Performance of the Franz cell permeation apparatus using an artificial membrane showed similar log linear correlation (R2 = 0.664) with Fa%, as seen for Papp in Caco-2 cells (R2 = 0.805). Data support the validation of the Franz-Bampa method for use during drug discovery process.

Subject Areas

Franz-Bampa; BCS drugs; biomimetic membrane; Franz cell; passive drug transport

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