Table 1

In vitro release and in vivo PK parameters of DTXL-TNPs. Time to 50% in vitro release was determined on the basis of measurements performed in duplicate. PK parameters are average values.

Major componentssb-DTXLDTXL-TNP formulation
EtOH:polysorbate 80 (1:2)PLA 6.5/PLGA-PEG 28/5 (1:1)PLA 6.5/PLA-PEG 16/5 (1:1)PLA-PEG 16/5
In vitro at 37°C
  Time to 50% release (hours)61945
In vivo (n = 6)
  Cmax (ng/ml)59519,60254,76767,267
  AUC (hours × ng/ml)48922,75296,844327,680
  Volume of distribution (Vz) (ml/kg)70,417665187103
  Clearance (ml hour−1 kg−1)9,2892375111
  Terminal half-life (t1/2) (hours)5.21.92.66.6