An efficient prodrug-based nanoscale delivery platform constructed by water soluble eight-arm-polyethylene glycol-diosgenin conjugate

Drug resistance in tumors is one of the reasons result in the low anticancer efficiency of numerous drugs. Combination therapy has been proven to be a valid way against drug-resistant cancers. However, simply mix the drugs will not only cause many side efforts but also decrease anticancer effect. Herein, a self-assembled nano particle platform based on eight-arm-polyethylene glycol-diosgenin (8armPEG-DGN) conjugate was produced for encapsulating another hydrophobic anticancer drug. The 8armPEG-DGN/HCPT NPs were prepared through a simple nanoprecipitation method. The 8armPEG-DGN/HCPT NPs possess suitable size (similar to 107 nm) and high binary drug loading capacity (15.67 wt% of DGN and 14.72 wt% of HCPT). Laser confocal scanning microscopy revealed that 8armPEG-DGN/HCPT NPs significantly increased intracellular uptake toward B16 cells compared with free drugs. Cytotoxicity assay showed the IC50 of 8armPEG-DGN/HCPT NPs were lower than simply mixing DGN and HCPT. In vivo tumor transplantation assay indicated that 8armPEG-DGN/HCPT NPs exhibited superior tumor grown inhibition compared with free drugs and HCPT/DGN Mix. These studies showed that the prepared 8armPEG-DGN/HCPT NPs drug delivery system could serve as a promising candidate for cancer therapy.