3 years ago

Absorption and Distribution of Lupeol in CD‐1 Mice evaluated by UPLC‐APCI+‐MS/MS

M.H. Cháirez-Ramírez, J.A. Gallegos-Infante, M.R. Moreno-Jiménez, R.F. González-Laredo, N.E. Rocha-Guzmán

Abstract

Lupeol is a dietary triterpene that shows limited water solubility, which affects its bioavailability. It is well known that poor oral bioavailability is one of the major causes of therapeutic variability. Lupeol has been reported with multiple biological activities; however, there are no reports about its bioavailability. Therefore, the objective of this research was to evaluate the systemic bioavailability of lupeol. An experimental strategy with three groups of female CD‐1 strain mice was proposed (control, olive oil and lupeol in olive oil), at six experimental times (0.5, 2, 4, 8, 12 and 24 h) and four animals per experimental point. Mice were sacrificed for organs, urine, feces and blood collection. Lupeol was extracted from samples and analyzed by UPLC‐APCI+‐MS/MS, obtaining its pharmacokinetics parameters Tmax (6.444±0.851 h) and Cmax (8.071±2.930 μg/mL). It was possible to observe that direct digestion and absorption related to organs have shown an important concentration of lupeol at earlier administration times (stomach, 137.25±19.94 ng/mg and small intestine, 99.00±12.99 ng/mg). The main excretion route was fecal, with a peak at 12 h post‐administration (163.28±9.83 μg/mg). Absorption of lupeol by animals was better than expected despite its non‐polar nature (extent of absorption F=0.645±0.0581).

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