Table 3.
PK of PLP after administration in its liposomal encapsulated or free form in rabbits | ||||
---|---|---|---|---|
PLP | Single dose LN-PLP (mg/kg) | Single dose free PLP (mg/kg) | ||
1 | 10 | 1 | 10 | |
Clearance (mL hour-1 kg-1) | 1.35 | 0.53 | * | 5494 |
Terminal half –life (T½) (hours) | 19.4 | 39.9 | * | 0.06 |
Cmax (μg/mL) | 29.9 | 342.0 | 1.69 | 20.3 |
| ||||
PK of the active metabolite PL after administration of PLP in liposomal encapsulated or its free form in rabbits | ||||
PL | Single dose LN-PLP (mg/kg) | Single dose free PLP (mg/kg) | ||
1 | 10 | 1 | 10 | |
| ||||
Clearance (mL hour-1 kg-1) | nc* | nc* | 3831 | 2808 |
Terminal half –life (T½) (hours) | nc* | nc* | 0.29 | 0.25 |
Cmax (μg/mL) | 1.84 | 12.1 | 0.54 | 9.56 |
Half-life and clearance rate for 1mg/kg free PLP could not be determined due to undetectable PLP plasma levels after the first time point (t=0.08 hours).
Cmax, maximal concentration; LN, liposomal nanoparticle; PL, prednisolone (active metabolite); PLP, prednisolone phosphate (prodrug); T½; terminal half-live.
nc, not calculated because plasma concentrations result of indirect release;