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- Title
Zr-Labeled Paramagnetic Octreotide-Liposomes for PET-MR Imaging of Cancer.
- Authors
Abou, Diane; Thorek, Daniel; Ramos, Nicholas; Pinkse, Martijn; Wolterbeek, Hubert; Carlin, Sean; Beattie, Bradley; Lewis, Jason
- Abstract
Purpose: Dual-modality PET/MR platforms add a new dimension to patient diagnosis with high resolution, functional, and anatomical imaging. The full potential of this emerging hybrid modality could be realized by using a corresponding dual-modality probe. Here, we report pegylated liposome (LP) formulations, housing a MR T contrast agent (Gd) and the positron-emitting Zr (half-life: 3.27 days), for simultaneous PET and MR tumor imaging capabilities. Methods: Zr oxophilicity was unexpectedly found advantageous for direct radiolabeling of preformed paramagnetic LPs. LPs were conjugated with octreotide to selectively target neuroendocrine tumors via human somatostatin receptor subtype 2 (SSTr2). Zr-Gd-LPs and octreotide-conjugated homolog were physically, chemically and biologically characterized. Results: Zr-LPs showed reasonable stability over serum proteins and chelator challenges for proof-of-concept in vitro and in vivo investigations. Nuclear and paramagnetic tracking quantified superior SSTr2-recognition of octreotide-LP compared to controls. Conclusions: This study demonstrated SSTr2-targeting specificity along with direct chelator-free Zr-labeling of LPs and dual PET/MR imaging properties.
- Subjects
PARAMAGNETIC materials; OCTREOTIDE acetate; LIPOSOMES; POSITRON emission tomography; MAGNETIC resonance imaging; CANCER diagnosis; ZIRCONIUM chelates
- Publication
Pharmaceutical Research, 2013, Vol 30, Issue 3, p878
- ISSN
0724-8741
- Publication type
Article
- DOI
10.1007/s11095-012-0929-8