In vivo evaluation of acute intravenous toxicity of a [Ga-68]Ga-PSMA-11-microemulsion
Zeevaart, Jan Rijn
Kalombo, Lonji M.
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Microemulsions (MEs) are reported to improve the efficacy of a drug, minimise side effects and toxicity of the encapsulated compound. MEs are hypothesized to aid in making the encapsulated compound, which has been incorporated within the ME, safe in vivo due to reduced side effects and toxicity to the kidneys and other non-target organs. This study aimed to contribute to knowledge on the toxicity of the ME delivery system and ME containing [68Ga]Ga-PSMA-11 with specific reference to intravenous tail vein administration. ME and [68Ga]Ga-PSMA-11-ME were synthesized by homogenisation under high temperature and a dose of 150 μl per mouse was administered intravenously in 10 healthy male BALB/c mice. The mice were monitored and evaluated for 14 days for clinical signs, mortality, body weights, and gross necropsy findings. The mice were euthanized after the respective 14-day period followed by isolation of respective organs and blood samples. Blood test results included assessment of alanine transaminase, aspartate transaminase, total protein, urea, creatinine and serum lipid levels. There were no abnormal changes observed in the body weight, coat condition, respiration, mobility and behaviour of any of the mice during the study. The survival rate was 10/10 mice (100%) after 14 days. None of the treatment groups showed any treatment related toxicity to either ME or [68Ga]Ga-PSMA-11-ME. Blood testing showed that liver and kidney function was in the normal range in both mice groups. This treatment regimen of the administered ME and [68Ga]Ga-PSMA-11-ME concentration caused no acute toxicity to small rodents but further investigations are required in larger animal models to justify the safety of [68Ga]Ga-PSMA-11-ME injections into humans
- Faculty of Health Sciences