Table 2.

Average PK parameter values (mean ± SD) following iv injection of 10 mg/kg of docetaxel in marketed diluted solution (Taxotere) or following oral administration in either aqueous diluted solution or combined with blank NCs embedded in microparticles at a dose of 250 mg/kg or docetaxel-loaded NCs embedded in microparticles (BI and BII), N = 4

Oral absorption study formulationCmax, ng/mLAUC, h ng/mLT1/2, hCL, L/h/kg
1. Docetaxel solution (i.v.)1,988.3 ± 307.95.4 ± 1.25.1 ± 0.7
2. Docetaxel solution (oral)19.5 ± 15.4109.5 ± 86.32.9 ± 2.276.5 ± 63.2
3. Docetaxel solution + blank microparticles (oral)132.5 ± 120.4232.8 ± 102.44.4 ± 1.937.1 ± 16.5
4. Docetaxel–PLGA4K double-coated NCs, BI (oral)2,299.6 ± 615.513,236.5 ± 1,702.60.7 ± 0.040.59 ± 0.23
5. Docetaxel–PLGA4K double-coated NCs, BII (oral)2,986.9 ± 1,859.417,280.3 ± 8,438.10.6 ± 0.020.67 ± 0.25

Cmax of 2 not significantly different from 3.

Cmax and CL of 4 and 5 significantly higher and smaller respectively than Cmax and CL of 2 and 3 (P < 0.001).

Cmax and CL of 4 not significantly different from 5.