Functionalized graphene oxide (GO) for the targeted intracellular delivery of hTERT siRNA was prepared by conjugating GO with polyethylene glycol (PEG) and folic acid, followed by the loading of siRNA with the aid of 1-pyrenemethylamine hydrochloride via p-p stacking. It was found that it could target the HeLa in vitro and the transfected hTERT siRNA could knockdown the protein expression level and mRNA level efficiently.

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In order to realize the hepatocyte-specific targeted delivery of anti-tumor drug and gene, lactosylated chitosan oligosaccharide (LCO) functionalized graphene oxides (GO-LCO) containing quaternary ammonium groups (GO-LCO+) were prepared. The formation and composition of GO-LCO+ were confirmed by FTIR, AFM, TGA and zeta-potential. The in vitro cells uptakes of this functionalized GO were investigated and the results showed that GO-LCO+ can deliver fluorescein FAM-labeled DNA sequence (FAM-DNA) into human hepatic carcinoma cells (QGY-7703) with higher efficiency than positively charged chitosan oligosaccharide (CO) functionalized graphene oxides (GO-CO+) without Lactose acid modification. The loading efficiency of doxorubicin chloride (Dox) on GO-LCO+ with 477 µg/mg was obtained at the initial Dox concentration of 0.45 mg/ml and release of Dox on GO-LCO+ showed strong pH dependence. The toxicity of GO-LCO+ before and after loading with Dox toward QGY-7703 cells was further investigated. Our results suggest the functionalized GO to be used as a nanocarrier for hepatocyte targeted co-delivery of anti-tumor drugs and genes with low cytotoxicity, promising for future applications in anticancer drug and gene combined therapy.