PEGylated liposomes of dimethylcurcumin: preparation, in vitro antitumor effect and in vivo pharmacokinetics

Dimethylcurcumin (DMC) is a derivative of curcumin. Studies have shown that DMC can enhance the degradation of androgen receptors (AR), thereby inhibiting AR-related diseases. However, the extremely poor water solubility and fast metabolism in vivo of DMC greatly limit its clinical applications. In the present study, poly(ethylene glycol)-modified liposomes loaded with DMC (DMC@PEG-Liposomes) were prepared by an improved membrane hydration method. The prescription of the liposomes was optimized to obtain DMC@PEG-Liposomes with a particle size between 110 and 150 nm, moderate encapsulation efficiency and good freeze-drying stability. In vitro release studies showed that DMC@PEG-Liposomes displayed Fickian release at pH 7.4 and non-Fickian release at pH 5.0. Compared with free DMC, DMC@PEG-Liposomes were more toxic to 22Rv1 and HepG2 cells in vitro. DMC@PEG-Liposomes also exhibited enhanced AUC0-t as compared to free DMC in in vivo pharmacokinetic studies. These results suggest that DMC@PEG-Liposomes are a promising DMC formulation for anticancer DMC delivery.