Abstract
Nanomedicine has become an emerging field in imaging and therapy of malignancies. Nanodimensional drug delivery systems have already been used in the clinic, as carriers for sensitive chemotherapeutics or highly toxic substances. In addition, those nanodimensional structures are further able to carry and deliver radionuclides. In the development process, non-invasive imaging by means of positron emission tomography (PET) represents an ideal tool for investigations of pharmacological profiles and to find the optimal nanodimensional architecture of the aimed-at drug delivery system. Furthermore, in a personalized therapy approach, molecular imaging modalities are essential for patient screening/selection and monitoring. Hence, labeling methods for potential drug delivery systems are an indispensable need to provide the radiolabeled analog. In this review, we describe and discuss various approaches and methods for the labeling of potential drug delivery systems using positron emitters.
Highlights
The field of nanomedicine has attracted more and more interest over the last decades, as nanoparticles (NPs) and polymeric structures have been related to biological and pathophysiological questions
Non-invasive molecular imaging techniques are excellent tools to investigate pharmacological profiles and to identify the optimal nanodimensional architecture of the aimed-at drug delivery system. Multimodal hybrid technologies such as positron emission tomography (PET)/computed tomography (CT) or PET/magnetic resonance imaging (MRI) were developed giving the chance to examine the pharmacological profiles of NPs or polymers [3]
Since this review focuses on radiolabeling strategies for polymers and NPs for PET imaging, the radionuclides discussed are positron emitters
Summary
The field of nanomedicine has attracted more and more interest over the last decades, as nanoparticles (NPs) and polymeric structures have been related to biological and pathophysiological questions. Since this review focuses on radiolabeling strategies for polymers and NPs for PET imaging, the radionuclides discussed are positron emitters. It is possible to couple, e.g., NPs, which are MR-active to a chelating system enabling in vivo tracking by multimodal imaging techniques (e.g., PET/MRI). In vitro cell experiments demonstrated low cytotoxicity, in vivo studies showed a high uptake almost exclusively in the liver (80.9% ID/g) and spleen (36.6% ID/g) already after 10 min showing a decrease in the liver (53.5% ID/g) and further increase in the spleen (89.9% ID/g) 2 h p.i. The rapid accumulation in spleen and liver was confirmed by MRI and optical imaging studies, MRI studies showed a significant contrast enhancement due to the presence of the NPs. Considering the simple labeling method by just mixing [18F]fluoride with metallic (rare earth) NPs, the in vivo-stability is remarkable. The radiolabeling for NPs and polymers and their preliminary preclinical evaluation using the metallic PET nuclides 68Ga and 64Cu is summarized and discussed
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