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Article

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

1
Institute of Pharmaceutical Sciences, Goiânia, Goiás 74175-100, Brazil
2
Laboratory of Biopharmacy and Pharmacokinetics (BioPK), Faculty of Pharmacy, Federal University of Goiás, Goiânia, Goiás 74175-100, Brazil
3
Institute of Physics, Federal University of Goiás, Goiânia, Goiás 74175-100, Brazil
4
Department of Engineering, Pharmacy Section, Miguel Hernandez University, 03550 Alicante, Spain
5
Faculty of Pharmacy, University of Maryland, Baltimore, MD 21021, USA
*
Author to whom correspondence should be addressed.
These authors contribute equally to this paper.
Pharmaceutics 2020, 12(10), 988; https://doi.org/10.3390/pharmaceutics12100988
Received: 8 September 2020 / Revised: 9 October 2020 / Accepted: 10 October 2020 / Published: 19 October 2020
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–PAMPA Pampa) was validated using a Franz cells apparatus. Both high and low permeability drugs (metoprolol and mannitol, respectively) were used as external standards. Biomimetic properties of Franz–PAMPA were also characterized by electron paramagnetic resonance spectroscopy (EPR). Moreover, the permeation profile for eight Biopharmaceutic Classification System (BCS) model drugs cited in the FDA guidance and another six drugs (acyclovir, cimetidine, diclofenac, ibuprofen, piroxicam, and trimethoprim) were measured across Franz–PAMPA. Apparent permeability (Papp) Franz–PAMPA values were correlated with fraction of dose absorbed in humans (Fa%) from the literature. Papp in Caco-2 cells and Corti artificial membrane were likewise compared to Fa% to assess Franz–PAMPA performance. Mannitol and metoprolol Papp values across Franz–PAMPA were lower (3.20 × 10−7 and 1.61 × 10−5 cm/s, respectively) than those obtained across non-impregnated membrane (2.27 × 10−5 and 2.55 × 10−5 cm/s, respectively), confirming lipidic barrier resistivity. Performance of the Franz cell permeation apparatus using an artificial membrane showed acceptable 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–PAMPA method for use during the drug discovery process. View Full-Text
Keywords: Franz–PAMPA; BCS drugs; biomimetic membrane; Franz cell; passive drug transport Franz–PAMPA; BCS drugs; biomimetic membrane; Franz cell; passive drug transport
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MDPI and ACS Style

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. https://doi.org/10.3390/pharmaceutics12100988

AMA Style

de Souza Teixeira L, Vila Chagas T, Alonso A, Gonzalez-Alvarez I, Bermejo M, Polli J, Rezende KR. Biomimetic Artificial Membrane Permeability Assay over Franz Cell Apparatus Using BCS Model Drugs. Pharmaceutics. 2020; 12(10):988. https://doi.org/10.3390/pharmaceutics12100988

Chicago/Turabian Style

de Souza Teixeira, Leonardo, Tatiana Vila Chagas, Antonio Alonso, Isabel Gonzalez-Alvarez, Marival Bermejo, James Polli, and Kênnia R. Rezende 2020. "Biomimetic Artificial Membrane Permeability Assay over Franz Cell Apparatus Using BCS Model Drugs" Pharmaceutics 12, no. 10: 988. https://doi.org/10.3390/pharmaceutics12100988

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