Imaging Biotin Trafficking In Vivo with Positron Emission Tomography

[Image: see text] The water-soluble vitamin biotin is essential for cellular growth, development, and well-being, but its absorption, distribution, metabolism, and excretion are poorly understood. This paper describes the radiolabeling of biotin with the positron emission tomography (PET) radionuclide carbon-11 ([(11)C]biotin) to enable the quantitative study of biotin trafficking in vivo. We show that intravenously administered [(11)C]biotin is quickly distributed to the liver, kidneys, retina, heart, and brain in rodents—consistent with the known expression of the biotin transporter—and there is a surprising accumulation in the brown adipose tissue (BAT). Orally administered [(11)C]biotin was rapidly absorbed in the small intestine and swiftly distributed to the same organs. Preadministration of nonradioactive biotin inhibited organ uptake and increased excretion. [(11)C]Biotin PET imaging therefore provides a dynamic in vivo map of transporter-mediated biotin trafficking in healthy rodents. This technique will enable the exploration of biotin trafficking in humans and its use as a research tool for diagnostic imaging of obesity/diabetes, bacterial infection, and cancer.