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Current progress in nanomedicine has exploited the possibility of designing tumor-targeted nanocarriers being able to deliver radionuclide payloads in a site or molecular selective manner to improve the efficacy and safety of cancer imaging and therapy. Radionuclides of auger electron-, α-, β-, and γ-radiation emitters have been surface-bioconjugated or after-loaded in nanoparticles to improve the efficacy and reduce the toxicity of cancer imaging and therapy in preclinical and clinical studies. This article provides a brief overview of current status of applications, advantages, problems, up-to-date research and development, and future prospects of nanotargeted radionuclides in cancer nuclear imaging and radiotherapy. Passive and active nanotargeting delivery of radionuclides with illustrating examples for tumor imaging and therapy are reviewed and summarized. Research on combing different modes of selective delivery of radionuclides through nanocarriers targeted delivery for tumor imaging and therapy offers the new possibility of large increases in cancer diagnostic efficacy and therapeutic index. However, further efforts and challenges in preclinical and clinical efficacy and toxicity studies are required to translate those advanced technologies to the clinical applications for cancer patients.

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Nanotechnology holds signifi cant promise for improving the development of new and paradigm shift tools for the targeted personalized diagnostics and therapeutics of cancer and other diseases. Current progress in nanotechnology has exploited the possibility of designing tumor-targeted nanocarriers that can deliver radionuclide payloads in a site or molecular selective manner to improve the effi cacy and safety of nuclear imaging and radiotherapy. Radionuclides of auger electron-, α-, β-, γ-and positronemitters have been after-loaded, inserted and surface bioconjugated in nanoparticles (NPs) to improve the effi cacy and to reduce the toxicity in preclinical studies. In addition, the combining of disease-specifi c multifunctional, multimodality and multivalent delivery of nanocarriers will hopefully achieve earlier disease detection and better treatment.The aim of this chapter is to provide an overview of nanotargeted radionuclides, up-to-date research and development, current status of applications, advantages, problems and future prospects and challenges. Two major strategies of passively and actively nanotargeted radiopharmaceuticals with illustrating examples are briefl y reviewed and summarized. Current advances in research of passive targeting co-delivery of radionuclides and chemotherapeutics, and advantages of nanocarriers in multifunctional and multimodality application for nuclear imaging and radiotherapy are discussed. Finally, radiotoxicology/nanotoxicology, clinical research and regulatory issues are also briefl y explored. Research on the combining different modes of selective delivery of radionuclides with targeted nanocarriers offers the new possibility Handbook of Nanobiomedical Research Downloaded from www.worldscientific.com by UNIVERSITY OF TOKYO on 06/05/15. For personal use only. 78 G. Ting et al. of increasing personalized diagnostic effi cacy and radiotherapeutic index. However, further efforts and challenges in preclinical and clinical effi cacy and toxicity studies are required to translate those advanced new technologies to the clinical applications for the healthcare benefi t of the patients.

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