Nanoemulsion Improves Oral Bioavailability and Transdermal Absorption Efficiency of Oxyresveratrol
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Abstract:
In this study, a nanoemulsion was prepared to improve the solubility of oxyresveratrol (OXY) in aqueous solutions. The effect of nanoemulsion on the bioavailability of OXY was evaluated through in vitro dissolution test, lipolysis test transmembrane transport test in Caco-2 monolayer model, and transdermal absorption test. The results showed that the bioavailability of OXY-loaded nanoemulsion and OXY itself was61.22% and 23.47%, respectively, in the fed state, and 56.12% and 22.45%, respectively, during the fasting state. The nanoemulsion increased the diffusion rate of OXY in the epithelial cells of the small intestine from medium to rapid, and the diffusion type was passive diffusion with an apparent permeability coefficient Papp (AP-BL) as 1.69×10-5 cm/sec, Papp (BL-AP) value as 8.94×10-6 cm/sec, and ER=Rpapp(AP-BL)/(BL-AP) as 1.89. The transdermal absorption of OXY-loaded nanoemulsion and OXY at the 6 h was 51.76 and 5.73 g/cm2 skin, respectively. Conclusions: The bioavailability of the OXY-loaded nanoemulsion was 3 times higher than that of the compound itself. Nanoemulsion significantly improved the absorption (by 2~4 times) and transmembrane transport efficiency of OXY (p<0.05) in the small intestinal epithelia cells. This study laid a research foundation for the application of OXY and provided a theoretical basis for enabling its efficacy.
