Preclinical Assessment Addressing Intravenous Administration of a [68Ga]Ga-PSMA-617 Microemulsion: Acute In Vivo Toxicity, Tolerability, PET Imaging, and Biodistribution

Vusani Mandiwana; Lonji Kalombo; Rose Hayeshi; Jan Rijn Zeevaart; Thomas Ebenhan

doi:10.3390/molecules26092650

Preclinical Assessment Addressing Intravenous Administration of a [⁶⁸Ga]Ga-PSMA-617 Microemulsion: Acute In Vivo Toxicity, Tolerability, PET Imaging, and Biodistribution

Molecules. 2021 Apr 30;26(9):2650. doi: 10.3390/molecules26092650.

Authors

Vusani Mandiwana^{1

2}, Lonji Kalombo¹, Rose Hayeshi², Jan Rijn Zeevaart^{2

3}, Thomas Ebenhan^{2

4

5}

Affiliations

¹ Centre for Nanostructures and Advanced Materials CeNAM, Chemical Cluster, Advanced Functional Materials, Council for Scientific and Industrial Research, Pretoria 0001, South Africa.
² Department of Science and Technology, Preclinical Drug Development Platform, North West University, Potchefstroom 2520, South Africa.
³ Radiochemistry, South African Nuclear Energy Corporation (Necsa), Pelindaba, Brits 0240, South Africa.
⁴ Department of Nuclear Medicine, University of Pretoria and Steve Biko Academic Hospital, Pretoria 0001, South Africa.
⁵ Preclinical Imaging Facility, NuMeRI, Pelindaba, Brits 0242, South Africa.

Abstract

It has been herein presented that a microemulsion, known to be an effective and safe drug delivery system following intravenous administration, can be loaded with traces of [⁶⁸Ga]Ga-PSMA-617 without losing its properties or causing toxicity. Following tolerated IV injections the capability of the microemulsion in altering [⁶⁸Ga]Ga-PSMA-617 distribution was presented at 120 min post injection based on its ex vivo biodistribution results.

Keywords: 68Ga; PSMA-617; [68Ga]Ga-PSMA-617-ME; biodistribution; in vivo; microPET/CT; microemulsion; prostate cancer; toxicity.

MeSH terms

Administration, Intravenous
Animals
Biomarkers
Chemical Phenomena
Dipeptides / administration & dosage
Dipeptides / adverse effects
Dipeptides / pharmacokinetics*
Edetic Acid / administration & dosage
Edetic Acid / adverse effects
Edetic Acid / analogs & derivatives*
Edetic Acid / pharmacokinetics
Emulsions* / chemistry
Gallium Isotopes
Gallium Radioisotopes
Heterocyclic Compounds, 1-Ring / administration & dosage
Heterocyclic Compounds, 1-Ring / adverse effects
Heterocyclic Compounds, 1-Ring / pharmacokinetics*
Male
Mice
Oligopeptides / administration & dosage
Oligopeptides / adverse effects
Oligopeptides / pharmacokinetics*
Positron Emission Tomography Computed Tomography
Positron-Emission Tomography / methods*
Prostate-Specific Antigen
Radiopharmaceuticals*
Tissue Distribution
Toxicity Tests, Acute
Zinc Isotopes

Substances

Biomarkers
Dipeptides
Emulsions
Gallium Isotopes
Gallium Radioisotopes
Heterocyclic Compounds, 1-Ring
Oligopeptides
PSMA-617
Radiopharmaceuticals
Zinc Isotopes
Zinc-68
gallium 68 PSMA-11
Edetic Acid
Prostate-Specific Antigen