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Use of an In Vitro Skin Parallel Artificial Membrane Assay (Skin-PAMPA) as a Screening Tool to Compare Transdermal Permeability of Model Compound 4-Phenylethyl-Resorcinol Dissolved in Different Solvents

Absorption through the skin of topically applied chemicals is relevant for both formulation development and safety assessment, especially in the early stages of development. However, the supply of human skin is limited, and the traditional in vitro methods are of low throughput. As an alternative, a...

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Autores principales: Sinkó, Bálint, Bárdos, Vivien, Vesztergombi, Dániel, Kádár, Szabina, Malcsiner, Petra, Moustie, Anne, Jouy, Chantal, Takács-Novák, Krisztina, Grégoire, Sebastien
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
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Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8625559/
https://www.ncbi.nlm.nih.gov/pubmed/34834173
http://dx.doi.org/10.3390/pharmaceutics13111758
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author Sinkó, Bálint
Bárdos, Vivien
Vesztergombi, Dániel
Kádár, Szabina
Malcsiner, Petra
Moustie, Anne
Jouy, Chantal
Takács-Novák, Krisztina
Grégoire, Sebastien
author_facet Sinkó, Bálint
Bárdos, Vivien
Vesztergombi, Dániel
Kádár, Szabina
Malcsiner, Petra
Moustie, Anne
Jouy, Chantal
Takács-Novák, Krisztina
Grégoire, Sebastien
author_sort Sinkó, Bálint
collection PubMed
description Absorption through the skin of topically applied chemicals is relevant for both formulation development and safety assessment, especially in the early stages of development. However, the supply of human skin is limited, and the traditional in vitro methods are of low throughput. As an alternative, an artificial membrane-based Skin Parallel Artificial Membrane Permeability Assay (Skin-PAMPA) has been developed to mimic the permeability through the stratum corneum. In this study, this assay was used to measure the permeability of a model compound, 4-phenylethyl-resorcinol (PER), dissolved in 13 different solvents that are commonly used in cosmetic formulation development. The study was performed at concentrations close to the saturated solution of PER in each solvent to investigate the maximum thermodynamic potential of the solvents. The permeability of PER in selected solvents was also measured on ex vivo pig skin for comparison. Pig ear skin is an accepted alternative model of human skin. The permeability coefficient, which is independent of the concentration of the applied solution, showed a good correlation (R(2) = 0.844) between the Skin-PAMPA and the pig skin permeation data. Our results support the use of the Skin-PAMPA to screen the suitability of different solvents for non-polar compounds at an early stage of formulation development.
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spelling pubmed-86255592021-11-27 Use of an In Vitro Skin Parallel Artificial Membrane Assay (Skin-PAMPA) as a Screening Tool to Compare Transdermal Permeability of Model Compound 4-Phenylethyl-Resorcinol Dissolved in Different Solvents Sinkó, Bálint Bárdos, Vivien Vesztergombi, Dániel Kádár, Szabina Malcsiner, Petra Moustie, Anne Jouy, Chantal Takács-Novák, Krisztina Grégoire, Sebastien Pharmaceutics Article Absorption through the skin of topically applied chemicals is relevant for both formulation development and safety assessment, especially in the early stages of development. However, the supply of human skin is limited, and the traditional in vitro methods are of low throughput. As an alternative, an artificial membrane-based Skin Parallel Artificial Membrane Permeability Assay (Skin-PAMPA) has been developed to mimic the permeability through the stratum corneum. In this study, this assay was used to measure the permeability of a model compound, 4-phenylethyl-resorcinol (PER), dissolved in 13 different solvents that are commonly used in cosmetic formulation development. The study was performed at concentrations close to the saturated solution of PER in each solvent to investigate the maximum thermodynamic potential of the solvents. The permeability of PER in selected solvents was also measured on ex vivo pig skin for comparison. Pig ear skin is an accepted alternative model of human skin. The permeability coefficient, which is independent of the concentration of the applied solution, showed a good correlation (R(2) = 0.844) between the Skin-PAMPA and the pig skin permeation data. Our results support the use of the Skin-PAMPA to screen the suitability of different solvents for non-polar compounds at an early stage of formulation development. MDPI 2021-10-21 /pmc/articles/PMC8625559/ /pubmed/34834173 http://dx.doi.org/10.3390/pharmaceutics13111758 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Sinkó, Bálint
Bárdos, Vivien
Vesztergombi, Dániel
Kádár, Szabina
Malcsiner, Petra
Moustie, Anne
Jouy, Chantal
Takács-Novák, Krisztina
Grégoire, Sebastien
Use of an In Vitro Skin Parallel Artificial Membrane Assay (Skin-PAMPA) as a Screening Tool to Compare Transdermal Permeability of Model Compound 4-Phenylethyl-Resorcinol Dissolved in Different Solvents
title Use of an In Vitro Skin Parallel Artificial Membrane Assay (Skin-PAMPA) as a Screening Tool to Compare Transdermal Permeability of Model Compound 4-Phenylethyl-Resorcinol Dissolved in Different Solvents
title_full Use of an In Vitro Skin Parallel Artificial Membrane Assay (Skin-PAMPA) as a Screening Tool to Compare Transdermal Permeability of Model Compound 4-Phenylethyl-Resorcinol Dissolved in Different Solvents
title_fullStr Use of an In Vitro Skin Parallel Artificial Membrane Assay (Skin-PAMPA) as a Screening Tool to Compare Transdermal Permeability of Model Compound 4-Phenylethyl-Resorcinol Dissolved in Different Solvents
title_full_unstemmed Use of an In Vitro Skin Parallel Artificial Membrane Assay (Skin-PAMPA) as a Screening Tool to Compare Transdermal Permeability of Model Compound 4-Phenylethyl-Resorcinol Dissolved in Different Solvents
title_short Use of an In Vitro Skin Parallel Artificial Membrane Assay (Skin-PAMPA) as a Screening Tool to Compare Transdermal Permeability of Model Compound 4-Phenylethyl-Resorcinol Dissolved in Different Solvents
title_sort use of an in vitro skin parallel artificial membrane assay (skin-pampa) as a screening tool to compare transdermal permeability of model compound 4-phenylethyl-resorcinol dissolved in different solvents
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8625559/
https://www.ncbi.nlm.nih.gov/pubmed/34834173
http://dx.doi.org/10.3390/pharmaceutics13111758
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