Table 1. Single transport studies of NSAIDs across PBMEC/C1-2 and ECV304.
substance | PSblank | PSall | PScell | PEall | PEcell | Ratio to Diazepam* | |
[µL/min] | [µL/min] | [µL/min] | [µm/min] | [µm/min] | |||
PBMEC/C1-2 | |||||||
Piroxicam study | Piroxicam | 8.69±0.72 | 4.63±0.36 | 9.91±1.60 | 11.02±0.87 | 23.82±3.81 | 0.55±0.05 |
Diazepam | 8.94±0.72 | 5.99±0.35 | 18.15±3.21 | 14.27±0.84 | 43.82±7.64 | ||
CF | 9.42±0.94 | 4.01±0.09 | 7.00±0.28 | 9.56±0.22 | 16.67±0.67 | ||
Ibuprofen study | Ibuprofen | 6.72±0.12 | 3.45±0.15 | 7.10±0.65 | 8.22 ±0.36 | 16.95±1.54 | 0.46±0.01 |
Diazepam | 9.25±0.49 | 5.76±0.18 | 15.27±1.27 | 13.71±0.43 | 36.47±3.03 | ||
CF | 11.69±0.30 | 4.47±0.08 | 7.24±0.21 | 10.65±0.19 | 17.25±0.49 | ||
Meloxicam study | Meloxicam | 8.03±1.21 | 3.15±0.10 | 5.18±0.28 | 7.50±0.25 | 12.34±0.68 | 0.41±0.13 |
Diazepam | 7.28±0.77 | 4.66±0.56 | 12.96±4.28 | 11.10±1.33 | 32.29±10.20 | ||
CF | 10.09±1.18 | 4.17±0.07 | 7.12±0.19 | 9.94±0.16 | 16.95±0.46 | ||
Tenoxicam study | Tenoxicam | 7.47± 0.31 | 4.13±0.07 | 9.25±0.33 | 9.84±0.16 | 22.04±0.78 | 0.49±0.01 |
Diazepam | 9.17±0.47 | 6.17±0.10 | 18.86±0.94 | 14.69±0.24 | 44.95±2.24 | ||
CF | 10.16±0.47 | 4.33±0.18 | 7.54±0.54 | 10.31±0.42 | 17.99±1.28 | ||
Diclofenac study | Diclofenac | 5.83±0.26 | 2.52±0.16 | 4.44±0.48 | 6.00±0.38 | 10.60±1.15 | 0.18±0.02 |
Diazepam | 8.00±0.12 | 6.04±0.10 | 24.69±1.74 | 14.39±0.25 | 58.93±4.14 | ||
CF | 10.07±0.41 | 4.39±0.08 | 7.79±0.24 | 10.46±0.18 | 18.56±0.58 | ||
Celecoxib study | Celecoxib | 6.07±0.45 | 2.92±0.19 | 5.62±0.71 | 6.95±0.45 | 13.44±1.69 | 0.32±0.03 |
Diazepam | 8.64±0.44 | 5.79±0.36 | 17.50±3.20 | 13.78±0.86 | 42.30±7.61 | ||
CF | 12.09±0.36 | 4.91±0.12 | 8.25±0.35 | 11.68±0.30 | 19.66±0.83 | ||
ECV304 | |||||||
Piroxicam study | Piroxicam | 8.53±0.36 | 3.21±0.07 | 5.15±0.19 | 7.65±0.18 | 12.27±0.46 | 0.42±0.01 |
Diazepam | 10.13±0.43 | 5.57±0.02 | 12.39±0.11 | 13.26±0.05 | 29.49±0.27 | ||
CF | 10.24±0.30 | 1.60±0.06 | 1.90±0.09 | 3.81±0.15 | 4.52±0.20 | ||
Ibuprofen study | Ibuprofen | 5.54±0.71 | 2.02±0.02 | 3.19±0.05 | 4.82±0.05 | 7.60±0.13 | 0.31±0.02 |
Diazepam | 8.21±0.29 | 4.60±0.13 | 11.43±0.68 | 10.94±0.32 | 24.86±1.63 | ||
CF | 10.30±1.45 | 1.54±0.11 | 1.81±0.15 | 3.67±0.26 | 4.32±0.36 | ||
Meloxicam study | Meloxicam | 5.80±0.26 | 1.77±0.13 | 2.56±0.27 | 4.23±0.32 | 6.10±0.65 | 0.19±0.02 |
Diazepam | 7.49±0.45 | 4.81±0.14 | 13.40±1.14 | 11.44±0.34 | 32.00±2.71 | ||
CF | 9.70±0.66 | 1.61±0.004 | 1.92±0.01 | 3.82±0.01 | 4.58±0.01 | ||
Tenoxicam study | Tenoxicam | 7.12±0.50 | 2.16±0.02 | 3.11±0.04 | 5.15±0.05 | 7.40±0.10 | 0.28±0.01 |
Diazepam | 8.92±0.72 | 4.97±0.08 | 11.21±0.41 | 11.83±0.19 | 26.71±0.98 | ||
CF | 11.58±0.67 | 1.58±0.08 | 1.83±0.11 | 3.77±0.19 | 4.36±0.26 | ||
Diclofenac study | Diclofenac | 4.08±0.41 | 1.50±0.08 | 2.38±0.19 | 3.58±0.18 | 5.67±0.46 | 0.14±0.03 |
Diazepam | 6.46±1.01 | 4.66±0.15 | 16.67±1.88 | 11.09±0.36 | 39.95±4.48 | ||
CF | 8.14±0.30 | 1.36±0.19 | 1.63±0.28 | 3.23±0.46 | 3.89±0.67 | ||
Celecoxib study | Celecoxib | 5.10±0.06 | 1.39±0.17 | 1.91±0.32 | 3.31±0.41 | 4.57±0.76 | 0.23±0.02 |
Diazepam | 10.20±1.48 | 4.58±0.34 | 8.32±1.12 | 10.91±0.80 | 19.93±2.67 | ||
CF | 11.45±0.89 | 1.88±0.08 | 2.25±0.11 | 4.47±0.18 | 5.35±0.26 |
Ratio to Diazepam is calculated by average PEcell data of the investigated NSAID and the corresponding diazepam value, CF = carboxyfluorescein.
Summary of permeability data of single transport studies with NSAIDs piroxicam, ibuprofen, meloxicam, tenoxicam, diclofenac and celecoxib across PBMEC/C1-2 as well as ECV304 cell layers. In each transport study one NSAID was applied together with the two permeability markers diazepam and carboxyfluorescein at the same time (n = 3, data are presented as means ± SD).