Colloidal gold nanoparticles are targeting probes to improve varlitinib delivery into cancer cells. The nanoconjugates were designed by the bioconjugation of pegylated gold nanoparticles with varlitinib via carbodiimide-mediated cross-linking and characterized by infrared and X-ray photoelectron spectroscopy. The drug release response shows an initial delay and a complete drug release after 72 h is detected. In vitro experiments with MIA PaCa-2 cells corroborate that PEGAuNPsVarl conjugates increase the varlitinib toxic effect at very low concentrations (IC50 = 80 nM) if compared with varlitinib alone (IC50 = 259 nM). Our results acknowledge a decrease of drug side effects in normal cells and an enhancement of drug efficacy against to the pancreatic cancer cells reported.