Abstract

Abstract Luteolin (LUT, 3′,4′,5,7-tetrahydroxyflavon) is a low water-soluble flavonoid with multiple biogicially activities. In this study, high water-soluble LUT nanoparticle was prepared by liquid anti-solvent precipitation and vacuum freeze-dry technology to enhance bioavailability and inhibit liver microsomal peroxidation in rats. When the concentration of LUT in the nanoparticles was 10.7 ± 0.3% (w/w), the size of LUT nanoparticles in water was successfully decreased to 127.5 ± 23.1 nm, and the amorphous state was reached. Meanwhile, the saturated solubility of LUT nanoparticles in deionized water (149.69 ± 12.6 µg) increased by 132.74 times. On the basis of the abovementioned results, LUT nanoparticles achieved excellent results in dissolution rates, lipid oxidation in vitro and bioavailability. Finally, results showed that the small particle size and amorphous state of LUT nanoparticles considerably improved their solubility in the solution medium, thereby enhancing their antioxidant ability and bioavailability.

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