A novel vascular disrupting agents ( VDAs ) noncovalent polymeric nanomedicine: Significantly increased antitumor therapeutic efficiency

Comprehensive Summary Plinabulin, a potential vascular disrupting agent (VDA), has entered the phase III clinical trial. However, the antitumor efficacy of Plinabulin is only moderate, which is probably because of the short action time of acting on tubulin. To maintain a constant VDAs concentration around the tumor vascular endothelial cells, in this study, we developed a novel Plinabulin derivate named HBP and further prepared noncovalent HBP nanoparticles (HBP NPs). We examined and compared the antitumor efficiency of HBP and HBP NPs in 4T1 tumor-bearing mice. HBP NPs significantly increased therapeutic efficiency than HBP, even with a quarter dose. These findings exhibited in this paper further confirmed the opinion that VDAs nanomedicine could markedly enhance tumor therapeutic effect more than small molecular VDAs.