Table 2.
Papp (cm/s) and efflux ratio calculated for the Caco-2 cell studied at different concentrations of REG in the presence or absence of verapamil or valspodar (mean ± SD, n = 3)
| Compound |
P
app
× 10
-5
(cm/s)
|
ER |
|---|---|---|
| A→B B →A | ||
| REG (20 µM ) | 1.67 ± 0.04 1.07 ± 0.02 | 0.64 ± 0.02 |
| REG (40 µM ) | 1.84 ± 0.12 1.19 ± 0.16 | 0.65 ± 0.05 |
| REG (60 µM ) | 1.83 ± 0.04 1.46 ± 0.11 | 0.80 ± 0.07 |
| REG (40 µM ) + Verapamil (100 µM) | 1.96 ± 0.27 1.18 ± 0.2 | 0.61 ± 0.09 |
| REG (40 µM ) + Valspodar (5 µM) | 1.64 ± 0.05 1.12 ± 0.1 | 0.68 ± 0.07 |
The influence of concentration on the transport of REG across the Caco-2 cell monolayers is demonstrated at three concentrations (20, 40 and 60 µM) (Figure 2, a and b). No saturation was observed for the transport of REG in both directions (apical to basolateral and basolateral to apical) at the concentrations studied.