Table 4.
Pharmacokinetic parameters of IV and nose-to-brain administration.
| Pharmacokinetic Parameter | Formulation | ||
|---|---|---|---|
| MEL | MEL-HSA | MEL-HSA-Tween | |
| Administration | IV | IN | IN |
| Ke (min−1) | 0.00213 | 0.00272 | 0.00231 |
| t1/2 (h) | 6.8 ± 3.1 | 4.7 ± 1.5 | 5.5 ± 1.6 |
| AUC 0–t (μmol/mL·min) | 626,296 ± 89,313 | 912,131 ± 212,767 | 946,683 ± 145,358 |
| AUC 0–∞ (μmol/mL·min) | 24,279 ± 12,254 | 22,788 ± 6139 | 23,300 ± 2539 |
| Cl (μg/kg)/(μmol/mL)/min | 0.0033 ± 0.0016 | 0.0029 ± 0.0001 | 0.0026 ± 0.0002 |
| Mean residence time (h) | 10.5 ± 4.5 | 7.3 ± 2.1 | 8.0 ± 2.2 |
| Drug targeting efficiency (%) | 100 | 223 | 182 |
| Absolute bioavailability (plasma) (%) | 100 | 65.3 | 83.2 |
| Absolute bioavailability (brain) (%) | 100 | 93.9 | 96.0 |