Functionalization of 68Ga-Radiolabeled Nanodiamonds with Octreotide Does Not Improve Tumor-Targeting Capabilities

Thomas Wanek; Marco Raabe; Md Noor A Alam; Thomas Filip; Johann Stanek; Mathilde Loebsch; Christian Laube; Severin Mairinger; Tanja Weil; Claudia Kuntner

doi:10.3390/ph17040514

Functionalization of ⁶⁸Ga-Radiolabeled Nanodiamonds with Octreotide Does Not Improve Tumor-Targeting Capabilities

Pharmaceuticals (Basel). 2024 Apr 17;17(4):514. doi: 10.3390/ph17040514.

Authors

Thomas Wanek^{1

2}, Marco Raabe^{3

4

5}, Md Noor A Alam^{3

4}, Thomas Filip^{2

6}, Johann Stanek^{1

2}, Mathilde Loebsch^{2

7}, Christian Laube⁸, Severin Mairinger^{2

9}, Tanja Weil^{3

4}, Claudia Kuntner^{1

2

10}

Affiliations

¹ Department of Biomedical Imaging and Image-Guided Therapy, Medical University of Vienna, 1090 Vienna, Austria.
² Preclinical Molecular Imaging, AIT Austrian Institute of Technology GmbH, 2444 Seibersdorf, Austria.
³ Synthesis of Macromolecules, Max Planck Institute for Polymer Research, 55128 Mainz, Germany.
⁴ Institute of Inorganic Chemistry I, Ulm University, 89081 Ulm, Germany.
⁵ Institute of Atomic and Molecular Sciences, Academia Sinica, Taipei 115201, Taiwan.
⁶ Institute of Animal Breeding and Genetics, University of Veterinary Medicine, 1210 Vienna, Austria.
⁷ Core Facility Laboratory Animal Breeding and Husbandry (CFL), Medical University of Vienna, 1090 Vienna, Austria.
⁸ Leibniz-Institute of Surface Engineering (IOM), 04318 Leipzig, Germany.
⁹ Department of Clinical Pharmacology, Medical University of Vienna, 1090 Vienna, Austria.
¹⁰ Medical Imaging Cluster (MIC), Medical University of Vienna, 1090 Vienna, Austria.

Abstract

Nanodiamonds (NDs) are emerging as a novel nanoparticle class with growing interest in medical applications. The surface coating of NDs can be modified by attaching binding ligands or imaging probes, turning them into multi-modal targeting agents. In this investigation, we assessed the targeting efficacy of octreotide-functionalized ⁶⁸Ga-radiolabelled NDs for cancer imaging and compared it with the tumor uptake using [⁶⁸Ga]Ga-DOTA-TOC. In vivo studies in mice bearing AR42J tumors demonstrated the highest accumulation of the radiolabeled functionalized NDs in the liver and spleen, with relatively low tumor uptake compared to [⁶⁸Ga]Ga-DOTA-TOC. Our findings suggest that, within the scope of this study, functionalization did not enhance the tumor-targeting capabilities of NDs.

Keywords: AR42J tumor-bearing mice; nanodiamonds; preclinical imaging; small animal PET.

Grants and funding

667192/European Union