NIR excitation of upconversion nanohybrids containing a surface grafted Bodipy induces oxygen-mediated cancer cell death

We report the preparation of water-dispersible, ca. 30 nm-sized nanohybrids containing NaYF4:Er3+, Yb3+ up-conversion nanoparticles (UCNPs), capped with a polyethylene glycol (PEG) derivative and highly loaded with a singlet oxygen photosensitizer, specifically a diiodo-substituted Bodipy (IBDP). The photosensitizer, bearing a carboxylic group, was anchored to the UCNP surface and, at the same time, embedded in the PEG capping; the combined action of the UCNP surface and PEG facilitated the loading for an effective energy transfer and, additionally, avoided photosensitizer leaching from the nanohybrid (UCNP-IBDP@PEG). The effectiveness of the nanohybrids in generating singlet oxygen after near-infrared (NIR) excitation (975 nm) with a continuous wavelength (CW) laser was evidenced by using a probe molecule. In vitro assays demonstrated that the UCNP-IBDP@PEG nanohybrid was taken up by the SH-SY5Y human neuroblastoma-derived cells showing low cytotoxicity. Moreover, ca. 50% cancer cell death was observed after NIR irradiation (45 min, 239 mW).