Integrin-targeting with peptide-bioconjugated semiconductor-magnetic nanocrystalline heterostructures
nanocrystalline heterostructures, photoactive semiconductor, magnetic nanostructure, cyclic RGD peptide, αvβ3 integrin, active targeting
Binary asymmetric nanocrystals (BNCs), composed of a photoactive TiO2 nanorod joined with a superparamagnetic γ-Fe2O3 spherical domain, were embedded in polyethylene glycol modified phospholipid micelle and successfully bioconjugated to a suitably designed peptide containing an RGD motif. BNCs represent a relevant multifunctional nanomaterial, owing to the coexistence of two distinct domains in one particle, characterized by high photoactivity and magnetic properties, that is particularly suited for use as a phototherapy and hyperthermia agent as well as a magnetic probe in biological imaging. We selected the RGD motif in order to target integrin expressed on activated endothelial cells and several types of cancer cells. The prepared RGD-peptide/BNC conjugates, comprehensively monitored by using complementary optical and structural techniques, demonstrated a high stability and uniform dispersibility in biological media. The cytotoxicity of the RGD-peptide/BNC conjugates was studied in vitro. The cellular uptake of RGD-peptide conjugates in the cells, assessed by means of two distinct approaches, namely confocal microscopy analysis and emission spectroscopy determination in cell lysates, displayed selectivity of the RGD-peptide-BNC conjugate for the αvβ3 integrin. These RGD-peptide-BNC conjugates have a high potential for theranostic treatment of cancer.
Tsinghua University Press
Gianpiero Valente,Nicoletta Depalo,Ivan de Paola,Rosa Maria Iacobazzi,Nunzio Denora,Valentino Laquintana,Roberto Comparelli,Emiliano Altamura,Tiziana Latronico,Michele Altomare,Elisabetta Fanizza,Marinella Striccoli,Angela Agostiano,Michele Saviano,Annarita Del Gatto,Laura Zaccaro,Maria Lucia Curri, Integrin-targeting with peptide-bioconjugated semiconductor-magnetic nanocrystalline heterostructures. NanoRes.2016, 9(3): 644–662