Light-activated therapy (LAT) has attracted enormous attention over the past decades because light enables noninvasive activation or release of various therapeutic compounds, such as photosensitizers, chemotherapeutic drugs, proteins, and genes with high spatial and temporal resolution. However, most currently used photosensitive compounds in LAT are sensitive to ultraviolet (UV) or visible light which suffers from some limitations such as low tissue penetration and photodamage to living organisms. Upconversion nanoparticles (UCNPs) that can convert near-infrared (NIR) light to visible/UV light have been proven to be effective for LAT in vivo in recent years, owing to the high tissue penetration and minimal photocytotoxicity of NIR light. Furthermore, hydrophilic UCNPs with targeting moieties can transport hydrophobic drugs in biological media and achieve active targeting, thus enhancing the therapeutic efficacy. In this chapter, we review the recent advances in the field of UCNP-based LAT with focus on photodynamic therapy (PDT) and NIR light-triggered release and uncaging.Keywords Light-activated therapy Á Upconversion nanoparticles Á Near-infrared excitation Á Photodynamic therapy Á Photosensitizer Á Light-triggered drug release Á Uncaging
IntroductionThe past decades have seen considerable interest and progress in light-activated therapy (LAT), including photodynamic therapy (PDT), chemotherapy, gene therapy, and photothermal therapy (PTT) as light is noninvasive and controllable both spatially and temporally compared to other stimuli such as temperature, pH, ultrasound, and applied magnetic or electric fields [1,2]. Owing to these Zhenzhen Guo and Fan Zhang contributed together to this chapter.© Springer-Verlag Berlin Heidelberg 2015 F. Zhang, Photon Upconversion Nanomaterials, Nanostructure Science and Technology, DOI 10.1007/978-3-662-45597-5_9 285 advantages, this effective therapeutic approach is beneficial to control drug dosing in terms of quantity, location, and time, hence maximizing therapeutic effect while minimizing side effects [3]. However, the excitation of most commonly used photosensitizers for PDT and photoactive molecules for the release of chemotherapeutic drugs and genes relies on high-energy ultraviolet (UV) or visible light irradiation [4,5]. The tissue penetration depth of UV-visible light is shallow because of the scattering and absorption by tissue chromophores [6]. What is worse, the heterocyclic bases of DNA are major UV-absorbing chromophores in the skin. The absorption leads to damage of the DNA, which may result in the generation of tumors [7]. These limitations would greatly hamper their applications in vivo. Compared to UV and visible light, near-infrared (NIR) light has a larger penetration depth, lower levels of the auto-fluorescence , and photodamage effect [8] and is thus better suited for biomedical applications. Therefore, another component that is capable of converting NIR excitation into UV or visible emission should be introduced into current LAT systems in o...