▎ 摘 要
While small interfering RNA (siRNA) technology has becomea powerfultool that can enable cancer-specific gene therapy, its translationto the clinic is still hampered by the inability of the genes aloneto cell transfection, poor siRNA stability in blood, and the lackof delivery tracking capabilities. Recently, graphene quantum dots(GQDs) have emerged as a novel platform allowing targeted drug deliveryand fluorescence image tracking in visible and near-infrared regions.These capabilities can aid in overcoming primary obstacles to siRNAtherapeutics. Here, for the first time, we utilize biocompatible nitrogen-and neodymium-doped graphene quantum dots (NGQDs and Nd-NGQDs, respectively)for the delivery of Kirsten rat sarcoma virus (KRAS) and epidermalgrowth factor receptor (EGFR) siRNA effective against a variety ofcancer types. GQDs loaded with siRNA noncovalently facilitate successfulsiRNA transfection into HeLa cells, confirmed by confocal fluorescencemicroscopy at biocompatible GQD concentrations of 375 mu g/mL.While the GQD platform provides visible fluorescence tracking, Nddoping enables deeper-tissue near-infrared fluorescence imaging suitablefor both in vitro and in vivo applications.The therapeutic efficacy of the GQD/siRNA complex is verified by successfulprotein knockdown in HeLa cells at nanomolar siEGFR and siKRAS concentrations.A range of GQD/siRNA loading ratios and payloads are tested to ultimatelyprovide substantial inhibition of protein expression down to 31-45%,comparable with conventional Lipofectamine-mediated delivery. Thisdemonstrates the promising potential of GQDs for the nontoxic deliveryof siRNA and genes in general, complemented by multiwavelength imagetracking.