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. 2021 Apr 30;26(9):2650.
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

Vusani Mandiwana  1   2 , Lonji Kalombo  1 , Rose Hayeshi  2 , Jan Rijn Zeevaart  2   3 , Thomas Ebenhan  2   4   5
Affiliations

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

Vusani Mandiwana et al. Molecules. .

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.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Representative maximum intensity projection microPET/CT images: Healthy BALB/c mice received a 0.1 mL intravenous injection of [68Ga]Ga-PSMA-617-ME via the lateral tail vein. PET/CT image acquisition data from (A) up to 40 min post injection was reconstructed and displayed and compared to (B) [68Ga]Ga-PSMA-617-ME PET/CT at 90–120 min. Recognized 68Ga-activity is visible in the myocardium (HE), both kidneys (KI), and the urinary bladder (UB).
Figure 2
Figure 2
SUV derived analysis of time-activity curves for heart, muscle, kidney, and bladder displayed up to 38 min after intravenous injection of [68Ga]Ga-PSMA-617 (black) and [68Ga]Ga-PSMA-617-ME (red). Results are expressed as mean (±standard error of mean (SEM); n = 4).
Figure 3
Figure 3
Ex vivo biodistribution (%ID/g) of [68Ga]Ga-PSMA-617 (black) and [68Ga]Ga-PSMA-617-ME (red) in blood and prefunded organs at 120 min after intravenous injections. Radioactive organ samples and radioactivity standards were measured using high-performance gamma counting. Results are expressed as mean (±SEM; n = 4). * P < 0.05; *** P < 0.001.
Figure 4
Figure 4
Organ and tissue biodistribution (%ID/g) of [68Ga]Ga-PSMA-617 (black) and [68Ga]Ga-PSMA-617-ME (red) 120 min after intravenous injection. Radioactive organ samples and radioactivity standards were measured using high-performance gamma counting. Results are expressed as mean (±SEM; n = 4). * P < 0.05.
Figure 5
Figure 5
Study design assessing acute in vivo toxicity and tolerability of intravenously administered 68Zn-PSMA-617 and in vivo imaging of [68Ga]Ga-PSMA-617-ME.
See this image and copyright information in PMC

References

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