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Eur J Nucl Med Mol Imaging (2016) 43:938940 DOI 10.1007/s00259-015-3299-8
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Cancer theranostics with 64Cu/177Lu-loaded liposomes
Emily B. Ehlerding1 & Shreya Goel2 & Weibo Cai1,2,3,4
Received: 19 December 2015 /Accepted: 22 December 2015 /Published online: 8 January 2016 # Springer-Verlag Berlin Heidelberg 2016
Personalized medicine has come to the forefront of cancer research and patient management in recent years. Among the many advances, nanomaterials stand to make significant impact in both the preclinical and clinical settings. Tumor-specific nanoconstructs should ideally allow for rapid concentration of imaging and/or therapeutic agents at the target site, and clear from the body within a reasonable period, thereby minimizing normal tissue toxicities. This idealized scenario is not yet a reality. Many nanoparticles can provide fantastic imaging and therapeutic capabilities in preclinical models, but their clinical applications to date have been limited by suboptimal pharmacokinetic and excretion profiles, systemic accumulation, and potential long-term toxicity [1, 2].
Among the myriad of nanocarriers proposed, liposomes are perhaps the most extensively investigated and have found many uses in the clinic [3]. Liposomes, which are closed bi-layer phospholipid systems, have long been recognized as efficient drug delivery vehicles [4], with the first liposomal constructs being described in the 1960s [5, 6]. Applications in metabolic disorders, diabetes, fungal infections, immuno-
logical diseases, cancer, etc. have been explored for liposomal drug delivery. Many liposomal drug systems have garnered regulatory approval in various countries, with a large number of others currently in various stages of clinical trials [7]. The use of liposomes as imaging agents has subsequently gained momentum as the drug delivery applications have expanded. Their uses for ultrasonic [8], fluorescence [9], magnetic resonance [10], and PET/SPECT imaging [11] have provided invaluable insights into the pharmacokinetics of these systems.
In this issue of the European Journal of Nuclear Medicine and Molecular Imaging, Petersen et al. evaluated the in vivo pharmacokinetics and dosimetry of PEGylated (i.e. polyethylene glycol-coated) liposomes for diagnostic (64Cu-liposomes) and radiotherapeutic (177Lu-liposomes) applications in neuroendocrine H727 tumor xenografts [12]. PEGylation of liposomes can be a double-edged sword, whereby too little PEG leads to suboptimal in vivo stability and too much...