Table 5.
Effect of rapamycin concentration on permeation parameters from formulations F3 and F5.
| Rapamycin Concentration | Formulation | 0.05% | 0.1% | 0.2% | 0.5% | 1% | 2% |
|---|---|---|---|---|---|---|---|
| Thermodynamic activity (αv) | F3 | 0.05 | 0.1 | 0.2 | 0.5 | 1 | 1 |
| F5 | 0.5 | 1 | 1 | 1 | NT | NT | |
| Jss (µg cm−2 h−1) 1 | F3 | NT | 0.7 ± 0.05 † | 1.1 ± 0.07 † | 2.4 ± 0.1 † | NS | |
| 3.0 ± 0.2 | 3.1 ± 0.2 | ||||||
| F5 | 0.4 ± 0.05 | NS | NT | NT | |||
| 0.8 ± 0.08 | 0.8 ± 0.1 | 0.8 ± 0.09 | |||||
| Kp × 10−4 (cm h−1) 1 | F3 | NT | 6.8 ± 0.5 † | 5.4 ± 0.3 † | 3.9 ± 0.1 † | 2.9 ± 0.4 | 1.6 ± 0.07 |
| F5 | 8.7 ± 0.9 | 7.9 ± 0.8 | 4.4 ± 0.7 | 1.7 ± 0.2 | NT | NT | |
| Tlag (h) 1 | F3 | NT | NS | ||||
| 5.1 ± 0.5 | 4.8 ± 0.4 † | 4.7 ± 0.3 † | 4.7 ± 0.4 | 4.7 ± 0.3 | |||
| F5 | NS | NT | NT | ||||
| 5.3 ± 0.5 | 4.8 ± 0.6 | 5.4 ± 0.5 | 5.4 ± 0.5 | ||||
| D × 10−5 (cm2 h−1) 1 | F3 | NT | NS | ||||
| 3.0 ± 0.3 | 3.2 ± 0.2 † | 3.2 ± 0.2 † | 3.2 ± 0.3 | 3.2 ± 0.2 | |||
| F5 | NS | NT | NT | ||||
| 2.9 ± 0.3 | 3.2 ± 0.4 | 2.8 ± 0.3 | 2.8 ± 0.3 | ||||
| P skin/vehicle 1 | F3 | NT | 0.7 ± 0.05 † | 0.5 ± 0.05 | 0.4 ± 0.02 † | 0.3 ± 0.04 | 0.1 ± 0.01 |
| F5 | 1.0 ± 0.09 | 0.8 ± 0.06 | 0.4 ± 0.02 | 0.2 ± 0.02 | NT | NT | |
| Cumulative amount diffused (µg cm−2) at 24 h 1 | F3 | NT | 12.8 ± 1.2 † | 20.6 ± 1.1 † | 48.0 ± 2.9 † | NS | |
| 59.4 ± 4.9 | 61.2 ± 4.5 | ||||||
| F5 | 8.1 ± 1.0 | NS | NT | NT | |||
| 15.3 ± 1.5 | 16.8 ± 1.8 | 16.8 ± 1.5 | |||||
1 Data are represented as mean ± standard deviation of 6 assays (n = 6). † F3 versus F5 (for the same concentration): p < 0.05; NS: non-significant (for the same formulation); NT: not tested. Jss: steady-state flux; Kp: permeability coefficient; Tlag: lag time; D: diffusion coefficient (thickness set at 300 µm); Pskin/vehicle: partition coefficient between skin and vehicle.