Table III.
Pharmacokinetic Parameter | Paclitaxel from Taxol® Control | Paclitaxel from PAX7′C6 in CrEL:EtOH | Paclitaxel from PAX7′C6 in PEG-b-PCL | PAX7′C6 from PAX7′C6 in CrEL:EtOH | PAX7′C6 from PAX7′C6 in PEG-b-PCL |
---|---|---|---|---|---|
AUCinf (μgh/ml) | 7.194 ± 1.495 | 1.519 ± 0.235a | 51.113 ± 1.362b,c | 16.247 ± 3.062 | 392.758 ± 31.501d |
Vdβ (L/kg) | 3.377 ± 0.687 | 13.125 ± 1.498a | 1.602 ± 0.504b,c | 4.678 ± 0.765 | 0.259 ± 0.030d |
CLrenal (L/h/kg) | 0.900 ± 0.203 | 0.635 ± 0.072 | 0.014 ± 0.002b,c | 0.004 ± 0.001 | 3.378 × 10−06 ± 4.291 × 10−07d |
CLhepatic (L/h/kg) | 0.655 ± 0.220 | 6.274 ± 1.094a | 0.182 ± 0.004b,c | 0.656 ± 0.121 | 0.026 ± 0.002d |
CLtot (L/h/kg) | 1.556 ± 0.400 | 6.909 ± 1.070a | 0.196 ± 0.005b,c | 0.661 ± 0.122 | 0.026 ± 0.002d |
Fe (%) | 58.913 ± 5.953 | 9.695 ± 1.805a | 6.959 ± 0.851b | 0.656 ± 0.081 | 0.014 ± 0.003d |
KE (h−1) | 0.453 ± 0.033 | 0.522 ± 0.022 | 0.145 ± 0.036b,c | 0.145 ± 0.027 | 0.101 ± 0.007 |
t1/2 (h) serum | 1.548 ± 0.122 | 1.333 ± 0.055 | 5.602 ± 1.656b,c | 5.131 ± 0.989 | 6.946 ± 0.479 |
t1/2 (h) urine | 10.932 ± 2.091 | 10.898 ± 1.526 | 15.827 ± 0.808b,c | 7.042 ± 0.290 | 17.102 ± 1.947d |
MRT (h) | 1.100 ± 0.214 | 1.912 ± 0.103a | 4.291 ± 0.767b,c | 7.635 ± 1.107 | 4.138 ± 0.380d |
Extraction ratio (ER) | 0.377 ± 0.126 | 3.606 ± 0.628a | 0.105 ± 0.002b,c | 0.377 ± 0.070 | 0.015 ± 0.001d |
Denotes statistical significant difference (P< 0.05) between paclitaxel after iv administration of control Taxol® (paclitaxel in Cremophor EL:Ethanol) and paclitaxel after iv administration of control PAX7′C6 in Cremophor EL:Ethanol.
Denotes statistical significant difference (P < 0.05) between paclitaxel after iv administration of control Taxol® (paclitaxel in Cremophor EL:Ethanol) and paclitaxel after iv administration of PAX7′C6 in PEG-b-PCL.
Denotes statistical significant difference (P < 0.05) between paclitaxel after iv administration of control PAX7′C6 in Cremophor EL:Ethanol and paclitaxel after iv administration of PAX7′C6 in PEG-b-PCL.
Denotes statistical significant difference (P < 0.05) between PAX7′C6 after iv administration of control PAX7′C6 in Cremophor EL:Ethanol and PAX7′C6 after iv administration of PAX7′C6 in PEG-b-PCL.