Early diagnosis and treatment of cancer is rapidly advancing thanks to the development of nanotechnology. Here, upconversion nanoparticles (UCNPs) are particularly promising as they are finding a wide range of applications in drug delivery and tumor imaging. In this report, a novel UCNP-based transport system is proposed for the delivery of the hypericin (Hyp) photosensitizer into malignant tumors. Core-shell NaYF4:Yb3+,Er3+@NaYF4:Nd3+ UCNPs were prepared by thermal decomposition and coated with poly(N,N-dimethylacrylamide-co-2-aminoethyl acrylate)-alendronate [P(DMA-AEA)-Ale], which endowed them with colloidal and chemical stability; finally, Hyp was conjugated. Internalization of CS-UCNP@P(DMA-AEA)-Ale-Hyp nanoparticles by Jurkat cells was successfully validated by multimodal imaging using a microstructural chamber, upconversion luminescence, and Raman microspectroscopy. After irradiation at 590 nm, CS-UCNP@P(DMA-AEA)-Ale-Hyp nanoparticles provided a markedly more effective photodynamic effect than Hyp alone at identical Hyp concentrations due to apoptosis as confirmed by caspase-3 activation. MTT assays showed that Hyp-free nanoparticles were non-cytotoxic, whereas CS-UCNP@P(DMA-AEA)-Ale-Hyp particles significantly reduced cell viability after irradiation. Considering that Hyp release from the nanoparticles was higher in the acidic environment typical of tumors compared to physiological ones, UCNP@P(DMA-AEA)-Ale-Hyp particles are a suitable candidate for future in vivo applications.

Center for Interdisciplinary Biosciences Technology and Innovation Park P J Šafárik University in Košice Jesenná 5 041 54 Košice Slovakia

Department of Biophysics Institute of Physics Faculty of Science P J Šafárik University in Košice Jesenná 5 041 54 Košice Slovakia

Institute of Animal Biochemistry and Genetics Centre of Biosciences Slovak Academy of Sciences Dúbravská cesta 9 840 05 Bratislava Slovakia

Institute of Experimental Physics Slovak Academy of Sciences Department of Biophysics Watsonova 47 040 01 Košice Slovakia

Institute of Macromolecular Chemistry Czech Academy of Sciences Heyrovského nám 2 162 00 Prague Czech Republic

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