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

Mater Sci Eng C Mater Biol Appl. 2019 May:98:153-160. doi: 10.1016/j.msec.2018.12.078. Epub 2018 Dec 26.

Abstract

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 nanoparticle 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 (~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.

Keywords: 8arm-PEG; Co-delivery; Combination therapy; Nanoparticles; Self-assemble.

MeSH terms

  • Diosgenin / chemistry*
  • Drug Carriers / chemistry*
  • Drug Delivery Systems
  • Nanoparticles / chemistry
  • Polyethylene Glycols / chemistry*
  • Prodrugs / chemistry
  • Water / chemistry

Substances

  • Drug Carriers
  • Prodrugs
  • Water
  • Polyethylene Glycols
  • Diosgenin