posted on 2021-08-06, 16:35authored byYingchao Li, Ran Zhang, Qi Zhang, Meiling Luo, Farong Lu, Zhonggui He, Qikun Jiang, Tianhong Zhang
Resveratrol (RES) suffers from poor
water solubility and extensive
metabolism, which lead to low bioavailability. A phospholipid complex
(PC) containing RES and a UDP-glucuronosyltransferase (UGT) inhibitor
was prepared to address these two limiting factors, thereby improving
RES bioavailability. First, 11 natural active ingredients metabolized
by similar enzyme subtypes to RES were screened in a glucuronidation
assay in liver microsomes. Then, glycyrrhetinic acid (GA), the strongest
inhibitor, was prepared with RES in a PC. RES-PC was prepared as a
control. As expected, the water solubility and the cumulative dissolution
of RES were significantly enhanced by RES-PC and RES/GA-PC. Compared
with the RES group, the AUC0–10 of RES and resveratrol-3-glucuronide
(R-3-G) in the RES/GA-PC group showed increases of 2.49- and 1.70-fold,
respectively, with the proportion of RES absorption to total absorption
increasing 1.45 times. These results demonstrated that RES/GA-PC could
improve the bioavailability of RES by increasing its water solubility
and inhibiting its glucuronidation.