Figure 2. HPβCD enhances the bioavailability of naringenin.

(a) 11 mM naringenin, either alone or in a complex with 45 mM HPβCD, was added to the top apical chamber of a Caco-2 model of human intestinal transport. In the presence of HPβCD, the concentration of naringenin was increased in the bottom basal side from 40±20 nM to 510±70 nM, representing an 11-fold enhancement of transport across the Caco-2 monolayer. (b) Phase image of Caco-2 monolayer grown for 21 days on collagen-coated transwell membranes. Barrier resistance remained unchanged during the course of the experiment. (c) Male Sprague-Dawley rats were fed 20 mg/kg body weight naringenin either alone, or as a HPβCD-naringenin complex. Blood samples were collected sequentially and analyzed for naringenin content by LC-MS. HPβCD-naringenin complex had higher oral bioavailability compared to naringenin alone. AUC_0-10 of the HPβCD-naringenin complex increased by 7.4-fold (p = 0.005), and maximal concentration, C_max increased by 14.6-fold (p = 0.002).