Nanotargeted Radiopharmaceuticals for Nuclear Imaging and Radiotherapy

Abstract

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.

Radiotherapy of the Excretable Radioactive Gold Nanocomposite with Intratumoral Injection

“…Since the nanotechnology was studied for decades, the nanomaterials have been designed to target a tumor by the unique physical-chemical properties [4]. By combination of nanotechnology and radiotherapy, various radioisotopes, Manuscript In and 166 Ho, can be fabricated to form nanoparticles or incorporated with nanoparticles as nanocomposites for radiotherapy [5], [6].…”

Future Perspectives of Radionanomedicine Using the Novel Micelle-Encapsulation Method for Surface Modification

“…Such multifunctional radionanomedicines can deliver multiple cancertargeting ligands (for improvement of target specificity), therapeutic radionuclides or therapeutic drugs (for therapy) and diagnostic radionuclides (for diagnosis) simultaneously. Indeed, the development of multifunctional radionanomedicine has become a possible state-of-the-art in nanomedicine research [5,6]. We will focus on the recent achievements of multifunctional radionanomedicine and its future perspectives.…”

Complexos derivados do fragmento <i>fac</i>-[M(CO)₃L] (M = Re e Tc) com ligantes multidentados como novos agentes para radioterapia e radiodiagnóstico

“…Quando o objetivo é a terapia, o efeito da radiação é utilizado para destruir células tumorais [24,25]. A radionuclideoterapia envolve o uso de um radiofármaco que seletivamente se acumula no tecido canceroso, destruindo-o através da emissão de uma partícula α, β ou um elétron Auger [24].…”

“…A radionuclideoterapia envolve o uso de um radiofármaco que seletivamente se acumula no tecido canceroso, destruindo-o através da emissão de uma partícula α, β ou um elétron Auger [24]. Essas partículas possuem um pequeno poder de penetração, mas apresentam uma alta energia [24].…”

“…Dentre os radionuclídeos destinados à terapia, a maioria dos atualmente utilizados no tratamento do câncer são os radioisótopos emissores de radiação α e β, sendo os emissores β os mais utilizados [24,26]. Os nuclídeos emissores de radiação β possuem baixos valores de energia de transferência linear (LET) e uma faixa de penetração no tecido que vai de 1 a 10 mm, podendo assim serem aplicados no tratamento de pequenos até mesmo grandes aglomerados de células tumorais [24].…”