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Dual-ligand-modified cantharidin nanoparticles for the treatment of hepatocellular carcinoma via the inhibition of Ephb4 - PubMed

3 hours ago
  • #Cancer Therapy
  • #Drug Delivery
  • #Nanotechnology
  • Dual-ligand-modified cantharidin nanoparticles (GA-FA-CSLNs) were developed to enhance targeted treatment of hepatocellular carcinoma (HCC).
  • The nanoparticles use glycyrrhetinic acid (GA) for liver targeting and folate-PEG3500-DSPE (FA) for prolonged circulation to improve specificity and reduce toxicity.
  • In vitro studies demonstrated increased cellular uptake, lower IC50, and induced apoptosis (43.2%) in Huh-7 liver cancer cells.
  • Mechanistically, GA-FA-CSLNs inhibit the EphB4 pathway, downregulating EphB4 and Bcl-2 while upregulating caspase-3 and Bax.
  • In vivo results showed a 58.67% tumor inhibition rate, outperforming free cantharidin and sorafenib, with high survival and minimal toxicity.
  • Pharmacokinetic analysis revealed extended elimination half-life (2.54 hours) and a 3.2-fold increase in area under the curve compared to unmodified nanoparticles.