The therapeutic application of deoxypodophyllotoxin (DPT) is limited due to its poor
water solubility and stability. In the present study, the micelles assembled by the
amphiphilic block copolymers (mPEG-PDLLA) were constructed to improve the solubility
and safety of DPT for their in vitro and in vivo application. The central composite
design was utilized to develop the optimal formulation composed of 1221.41 mg mPEG-PDLLA,
the weight ratio of 1 : 4 (mPEG-PDLLA : DPT), 30 mL hydration volume and the hydration
temperature at 40 °C. The results showed that the micelles exhibited uniformly spherical
shape with the diameter of 20 nm. The drug-loading and entrapment efficiency of deoxypodophyllotoxin-polymeric
micelles (DPT-PM) were about (20 � 2.84)% and (98 � 0.79)%, respectively, indicating
that the mathematical models predicted well for the results. Compared to the free
DPT, the cytotoxicity showed that blank micelles possessed great safety for Hela cells.
In addition, the DPT loaded micelle formulation achieved stronger cytotoxicity at
the concentration of 1 × 10 −7 mol·L −1 , which showed significant difference from
free DPT ( P < 0.05). In conclusion, the micelles were highly promising nano-carriers
for the anti-tumor therapy with DPT.