Transcellular transport of C-K across monolayers of Caco-2, MDCKII, and MDR1-MDCKII cells in the absence or presence of P-gp inhibitors
Data are presented as mean ± S.D. (n = 3). Pa-b refers to the permeability from the apical to basolateral side, and Pb-a refers to the permeability from the basolateral to apical side. The values of permeability were compared between different directions, and intracellular amounts were compared to the control group. Data are the means ± S.D. of three independent experiments.
| Cell Model | Inhibitor | Inhibitor Concentration | Pa-b | Pb-a | Efflux Ratio (Pb-a/Pa-b) | Intracellular Amounts |
|---|---|---|---|---|---|---|
| μM | ×10−6 cm/s | ×10−6 cm/s | nmol/mg | |||
| Caco-2 | – | – | 1.16 ± 0.33 | 30.96 ± 4.31** | 26.6 | 0.01 ± 0 |
| Verapamil | 50 | 3.39 ± 0.41 | 9.89 ± 0.11* | 2.9 | 0.50 ± 0.01*** | |
| Cyclosporine A | 20 | 3.30 ± 0.67 | 3.62 ± 0.22 | 1.1 | 0.15 ± 0.01*** | |
| MDCKII | – | – | 0.58 ± 0.12 | 1.13 ± 0.11* | 1.8 | 0.27 ± 0.03 |
| MDR1-MDCKII | – | – | 1.84 ± 0.70 | 33.64 ± 8.08** | 18.2 | 0.08 ± 0.01** |