Table 5.
Pharmacokinetic Parameters of Docetaxel (DTX) Following IV Administrations of Different Formulations at a Dose of 5 mg/kg Body Weight in Rats (n = 3)
| Parameter | Free DTX | Free DTX/PIC | DTX_NCs | D/P_NCs | Tra-D/P_NCs | Per-D/P_NCs | Dual-D/P_NCs |
|---|---|---|---|---|---|---|---|
| C0 (μg/mL) | 0.123±0.04 | 0.436±0.227 | 0.399±0.130 | 0.450±0.245 | 0.414±0.100 | 0.572±0.373 | 0.518±0.140 |
| t1/2 (h) | 5.32±0.24 | 6.11±2.36 | 7.65±1.54 | 7.88±1.41 | 5.85±1.20 | 6.41±0.77 | 7.52±1.19 |
| AUC0-last (h×μg/mL) | 0.487±0.037 | 0.659±0.050 | 0.986±0.177 | 0.897±0.215 | 0.928±0.145 | 0.849±0.031 | 0.826±0.087 |
| AUC0-inf (h×μg/mL) |
0.524±0.037 | 0.713±0.071 | 1.064±0.219 | 0.941±0.243 | 0.954±0.144 | 0.883±0.042 | 0.859±0.100 |
| CL (L/h/kg) | 9.58±0.70 | 7.06±0.66 | 4.82±0.89 | 5.59±1.61 | 5.33±0.87 | 5.67±0.27 | 5.88±0.72 |
| Vd (L/kg) | 73.43±5.22 | 60.77±17.43 | 52.09±6.54 | 61.62±7.78 | 44.40±7.13 | 52.67±8.62 | 63.13±6.46 |
| Relative bioavailability (%) | 100 | 136 | 203 | 180 | 182 | 169 | 164 |
Note: Values are the mean±standard deviation.
Abbreviations: C0, initial plasma concentration; Cmax, highest observed plasma concentration; t1/2, elimination half-life; AUC0-last, area under the plasma concentration–time curve from 0 h to the last sampling time point; AUC0-inf, area under plasma concentration–time curve extrapolated to infinity; CL, plasma clearance; Vd, apparent volume of distribution; PIC, pictilisib; NCs nanocarriers; D, DTX; P, PIC; Tra, trastuzumab; Per, pertuzumab.