Pharmacokinetics of Geraniol and Its Metabolites in Mice After Oral Administration

Geraniol is an acyclic monoterpene alcohol that is extracted from the essential oils of aromatic plants. Geraniol has several biological activities such as anti‐cancer, anti‐inflammatory, antioxidant, and neuroprotective effects. However, the pharmacokinetics of geraniol and its metabolites after oral administration remain unknown in mice. To investigate the pharmacokinetics, the blood concentrations were measured in C57BL/6J mice by LC‐MS/MS after oral administration of geraniol at a dose of 200 mg/kg. The C max for blood levels of geraniol was only 0.05 ± 0.01 μg/mL at 1 h after administration. In contrast, geranic acid, one of the geraniol metabolites, rapidly reached a peak level that was markedly higher than that of geraniol. Furthermore, the glucuronide conjugate of geraniol was detected at a higher level than geraniol. These results indicate that geraniol is rapidly converted to geranic acid or glucuronide conjugate after oral administration. Moreover, geraniol was detected in the liver and the brain, whereas 8‐hydroxygeraniol was not detected in any tissues. In contrast, geranic acid was detected in several tissues in the order of kidney > liver = lung > brain. Therefore, the metabolites of geraniol are present in the blood and tissues of mice treated with geraniol, and various pharmacological effects of geraniol may be caused by its metabolites.