Fabrication and characterization of dihydromyricetin encapsulated zein-caseinate nanoparticles and its bioavailability in rat.

Dihydromyricetin (DMY) encapsulated zein-caseinate nanoparticles (DZP) were fabricated by antisolvent method. The encapsulation and loading efficiency of DMY in DZP were 90.2% and 22.6% as determined by HPLC. DZP is spherical with particle size and ζ potential of 206.4 nm and -29.6 mV, respectively. Physicochemical characterization showed that DMY existed in amorphous form in DZP and its interaction with proteins was found. The fabrication of DZP significantly improved the stability of DMY. Besides, the diffusion rate of DMY in DZP was faster than its suspensions in both simulated gastric and intestinal fluid. The adhesion of DMY in mice gastrointestinal tract was also improved. Besides DMY itself, its methylated metabolites with further sulfation and glucuronide were identified in rat plasma by UPLC-QTOF-MS. UPLC-QqQ-MS/MS quantitative analysis showed that the oral bioavailability of DMY was 1.95 times enhanced. Besides, the concentration of DMY metabolites in plasma were all increased.