Permeability of the Perindopril Arginine under In Vitro Conditions across Caco-2 Monolayer and Biomimetic Phospholipid Membrane
Abstract
:1. Introduction
2. Results
2.1. Effect of PA on Caco-2 Cells’ Viablility
2.2. Permeability Studies across the Caco-2 Monolayer
2.3. Permeability Studies across PermeaPad Membrane
3. Discussion
4. Materials and Methods
4.1. Permeability Studies Employing PermeaPad Membrane
4.1.1. Chemical Reagents and References
4.1.2. In Vitro Analysis
4.1.3. Compounds
4.2. Caco-2 Cell Culture
4.3. Cytotoxicity Analysis
4.4. Permeability Testing across Caco-2 Monolayer
4.5. Permeability Studying across PermeaPad 96-Well Plate
4.6. Quantification by HPLC
5. Conclusions
Author Contributions
Funding
Institutional Review Board Statement
Informed Consent Statement
Data Availability Statement
Conflicts of Interest
Sample Availability
References
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Substance | Concentration (mg/mL) | Papp × 10−6 (cm/s) | Compound Permeability |
---|---|---|---|
PA | 2.0 | 1.94 ± 0.96 | low |
PA | 1.0 | 0.72 ± 0.04 | low |
CAF | 0.5 | 126.5 ± 2.4 | high |
Substance | Chemical Formula | Molecular Weight (MW) | pKa | logP | Reference |
---|---|---|---|---|---|
PA | C25H46N6O7 | 542.7 | 3.17 (strongest acid) 5.67 (strongest base) | 0.65 0.56 | internal data |
CAF | C8H46N6O7 | 194.2 | 14 | 0.07 | PubChem [32] |
NF | C26H35NO7 | 473.6 | 4.1 | 1.98 4.85 | internal data |
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Kus, M.; Gorniak, K.; Czaklosz, P.; Olejnik, A.; Skupin-Mrugalska, P.; Ibragimow, I.; Piotrowska-Kempisty, H. Permeability of the Perindopril Arginine under In Vitro Conditions across Caco-2 Monolayer and Biomimetic Phospholipid Membrane. Molecules 2022, 27, 2232. https://doi.org/10.3390/molecules27072232
Kus M, Gorniak K, Czaklosz P, Olejnik A, Skupin-Mrugalska P, Ibragimow I, Piotrowska-Kempisty H. Permeability of the Perindopril Arginine under In Vitro Conditions across Caco-2 Monolayer and Biomimetic Phospholipid Membrane. Molecules. 2022; 27(7):2232. https://doi.org/10.3390/molecules27072232
Chicago/Turabian StyleKus, Marta, Klaudia Gorniak, Piotr Czaklosz, Anna Olejnik, Paulina Skupin-Mrugalska, Izabela Ibragimow, and Hanna Piotrowska-Kempisty. 2022. "Permeability of the Perindopril Arginine under In Vitro Conditions across Caco-2 Monolayer and Biomimetic Phospholipid Membrane" Molecules 27, no. 7: 2232. https://doi.org/10.3390/molecules27072232