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Gold nanoparticles were obtained by reduction of a tetrachloroaurate aqueous solution in the presence of a RGD-(GC)₂ peptide as stabilizer. As comparison, the behavior of the (GC)₂ peptide has been studied. The (GC)₂ and RGD-(GC)₂ peptides were prepared ad hoc by Fmoc synthesis. The colloidal systems have been characterized by UV–visible, TGA, ATR-FTIR, mono and bidimensional NMR techniques, confocal and transmission (TEM) microscopy, ζ-potential, and light scattering measurements. The efficient cellular uptake of Au-RGD-(GC)₂ and Au-(GC)₂ stabilized gold nanoparticles into U87 cells (human glioblastoma cells) were investigated by confocal microscopy and compared with the behavior of (GC)₂ capped gold nanoparticles. A quantitative determination of the nanoparticles taken up has been carried out by measuring the pixel brightness of the images, a measure that highlighted the importance …