posted on 2020-03-12, 17:40authored byAlessio Molinari, Giulia Iovenitti, Arianna Mancini, Giovanni Luca Gravina, Monia Chebbi, Maura Caruana, Giulia Vignaroli, Francesco Orofino, Enrico Rango, Adriano Angelucci, Elena Dreassi, Silvia Schenone, Maurizio Botta
Gold-nanoparticle
(AuNP)-conjugated drugs represent a promising
and innovative antitumor therapeutic approach. In our study, we describe
the design, the synthesis, the preparation, and the characterization
of AuNPs conjugated with the pyrazolo[3,4-d]pyrimidine
derivative SI306, a c-Src inhibitor. AuNPs–SI306 showed a good
loading efficacy (65%), optimal stability in polar media and in human
plasma, and a suitable morphological profile: a ζ-potential
of −43.9 mV, a nanoparticle diameter of 48.6 nm, and a 0.441
PDI value. The antitumoral activity of AuNPs–SI306 was evaluated in vitro in the glioblastoma model, by the low-density growth
assay, and also in combination with radiotherapy (RT). Results demonstrated
that AuNPs had a basal radiosensitization ability and that AuNPs–SI306,
when used in combination with RT, were more effective in inhibiting
tumor cell growth with respect to AuNPs and free SI306.