Table II.
Bi-directional transport of [3H]-Etoposide, [3H]-Topotecan and [3H]-Vinblastine alone and in presence of moxifloxacin (500 µM), GF120198 (2 µM) and MK571 (50 µM) across MDCK-MDR and MDCK-MRP2. Values are expressed as mean ± SD (n=3).
| Cell line | Drug | Permeability (×10−6) cm/s | Efflux Ratio |
|
|---|---|---|---|---|
| AP-BL | BL-AP | |||
| MDCK-MDR1 | Etoposide | 3.57 ± 0.65 | 11.60 ± 1.78 | 3.25 |
| Etoposide + Moxifloxacin | 7.92 ± 1.78 | 12.84 ± 2.08 | 1.62 | |
| Etoposide + GF120918 | 10.71 ± 0.52 | 11.02 ± 1.45 | 1.03 | |
| Vinblastine | 1.55 ± 0.03 | 10.22 ± 0.47 | 6.59 | |
| Vinblastine + Moxifloxacin | 3.95 ± 0.46 | 8.92 ± 1.91 | 2.26 | |
| Vinblastine + GF120918 | 5.35 ± 0.40 | 7.14 ± 1.47 | 1.33 | |
| Topotecan | 0.75 ± 0.03 | 3.50 ± 0.28 | 4.63 | |
| Topotecan + Moxifloxacin | 1.56 ± 0.03 | 3.38 ± 0.16 | 2.16 | |
| Topotecan + GF120918 | 2.27 ± 0.18 | 3.14 ± 0.20 | 1.38 | |
| MDCK-MRP2 | Etoposide | 37.82 ± 2.70 | 206.76 ± 17.45 | 5.46 |
| Etoposide + Moxifloxacin | 89.34 ± 1.75 | 194.29 ± 12.58 | 2.17 | |
| Etoposide + MK571 | 175.62 ± 7.47 | 189.47 ± 20.42 | 1.08 | |
| Vinblastine | 13.50 ± 3.24 | 73.75 ± 8.16 | 5.46 | |
| Vinblastine + Moxifloxacin | 19.72 ±2.56 | 48.90 ± 6.70 | 2.48 | |
| Vinblastine + MK571 | 25.60 ± 4.42 | 35.58± 9.72 | 1.39 | |
| Topotecan | 8.06 ± 0.66 | 24.78 ± 2.44 | 3.07 | |
| Topotecan + Moxifloxacin | 12.67 ± 2.67 | 22.89 ± 3.54 | 1.80 | |
| Topotecan + MK571 | 19.51 ± 1.31 | 22.08 ± 2.79 | 1.13 | |