Well-defined amphiphilic poly(
ethylene glycol) and poly(dehydroabietic ethyl
methacrylate) block copolymers (PEG-b-PDAEMA) were prepared by atom transfer radical polymerization. The
methacrylate block contains a characteristic hydrophobic, biocompatible and economical dehydroabietic moiety. PEG-b-PDAEMA block copolymer micellar nanoparticles loaded with
piperlongumine (PLGM) were successfully prepared by a nanoprecipitation method. In vitro and in vivo behaviors of these nanoparticles were thoroughly examined by a set of characterization techniques. Confocal
laser scanning microscopy study revealed that these nanoparticles could be well taken up by
cancer cells. In vivo near-infrared fluorescence imaging showed that the PLGM-loaded nanoparticles effectively targeted the
tumor site by the enhanced permeability and retention (EPR) effect in H22
tumor-bearing mice. The in vivo antitumor examination found that PLGM-loaded nanoparticles exhibited superior efficacy in impeding the
tumor growth compared to the commercially available Taxol® and free PLGM formulation. The changes in
body weights and blood biochemical profiles were also compared to investigate the safety of PLGM and PEG-b-PDAEMA
nanoparticle drug delivery system.