Abstract:Objective: To investigate the general properties of the complexes of VEGF siRNA-loaded RGD-conjugated gold nanoparticles (GNPs) (GNPs-TyrRGD-VEGFsiRNA) and their impact on necrotic effect of radiofrequency ablation (RFA) in the liver. Methods: GNPs-TyrRGD-VEGFsiRNA complexes were synthetized by chemical and electrostatic adsorption methods and the discreteness of the complexes was examined by electron microscope. The stability of the VEGF siRNA in the complexes was tested by gel electrophoresis, the cytotoxicity of complexes to normal hepatic cells was determined by CCK-8 assay, the binding capacities of the complexes to normal hepatic cells and liver cancer cells after co-incubation were analyzed by using electron microscopy, and the impact of the complexes on the necrotic effect of RFA were observed in the in-vitro pig liver. Results: The complexes showed a higher discreteness than the naked GNPs and the content of VEGF siRNA in the complexes was approximately equal to the initially loaded content. Both the complexes and naked GNPs exhibited almost no cytotoxicity to the normal hepatic cells at a concentration below 30% and the binding ability of the complexes to the liver cancer cells was significantly greater than that to the normal hepatic cells (P<0.05), but the naked GNPs showed no difference between binding ability to the two types of cells (P>0.05). The lesion diameter induced by RFA with the complexes injected through radiofrequency needle was significantly larger than that in control group with saline injection [(2.19±0.24) cm vs. (1.71±0.14) cm, P<0.05]. Conclusion: GNPs-TryRGD-VEGFsiRNA complexes can integrate targeted concentration and targeted therapy as a whole, and may also be helpful for enhancing the efficacy of liver cancer RFA treatment.