NIR light-induced imaging-guided cancer therapy is an encouraging route in the cancer theranostic field. Herein, we describe a novel nanoscale proposal, which is established by covalently implanting core-shell structured upconversion nanoparticles (UCNPs) with nanographene oxide (NGO) by a process utilizing polyethylene glycol (PEG), and consequently loading Chlorin e6 (Ce6) onto the surface of NGO. The acquired NGO-UCNP-Ce6 (NUC) nanocomposites can not only be employed as upconversion luminescence (UCL) imaging probes of cells and whole-body animals with high contrast for diagnosis, but also can generate reactive oxygen species (ROS) under 808 nm light excitation for photodynamic therapy (PDT); over and above, they can swiftly and proficiently translate the 808 nm photon into thermal energy for photothermal therapy (PTT). An extraordinarily enhanced and synchronized therapeutic effect paralleled to the individual PTT or PDT is achieved, rendering extraordinary therapeutic effectiveness for cancer treatment. Consequently, profiting from this inimitable multifunctional nanohybrid, the NUCs synthesized here are encouraging as a cohesive theranostic probe for impending UCL imaging-guided combinatorial PDT/PTT.

Lanthanide-doped photon upconverting nanomaterials are evolving as a new class of imaging contrast agents, offering highly promising prospects in the area of biomedical applications. Owing to their ability to convert long-wavelength near-infrared excitation radiation into shorter-wavelength emissions, these nanomaterials are well suited to yield properties of low imaging background, large anti-Stokes shift, along with high optical penetration depth of NIR light for deep tissue optical imaging or light-activated drug release and therapy. Such materials have potential for significant advantages in analytical applications compared to molecular fluorophores and quantum dots. The use of IR radiation as an excitation source diminishes autofluorescence and scattering of excitation radiation, which leads to a reduction of background in optical experiments. The upconverting nanocrystals show exceptional photostability and are constituted of materials that are not significantly toxic to biological organisms. Excitation at long wavelengths also minimizes damage to biological materials. In this detailed review, various mechanisms operating for the upconversion process, and methods that are utilized to synthesize and decorate upconverting nanoparticles are investigated to elucidate by what means absorption and emission can be tuned. Up-to-date reports concerning cellular internalization, biodistribution, excretion, cytotoxicity and in vivo toxic effects of UCNPs are discussed. Specifically, studies which assessed the relationship between the chemical and physical properties of UCNPs and their biodistribution, excretion, and toxic effects are reviewed in detail. Finally, we also deliberate the challenges of guaranteeing the biosafety of UCNPs in vivo.

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