Preparation And Evaluation Of Dihydromyricetin Loaded Micro/Nano Carriers

Dihydromyricetin(DMY),a natural flavonoid component from herbal medicines such as Hovenia and Ampelopsis grossedentata,has shown many curative effects such as anti-oxidant,anti-inflammatory,anti-tumor,and especially has a great therapeutic potential in hepatic-protective activity.However,the application in functional food of DMY is limited by its poor stability,solubility and bioavailability.Therefore,the objectives of this investigation were to design the DMY loaded micro/nano carriers with more functional lipids and emulsifiers to overcome the limitions existed in application and provide a new strategy for the application of DMY in functional foods.Firstly,the DMY loaded nano-emulsion(DMY-NE)was prepared containing 0.97 ± 0.06% of DMY and the entrapment efficiency was 73.36 ± 1.59%.The mean droplet size and PdI were 86.63 ± 0.41 nm and 0.090 ± 0.013,respectively.The stability results indicated that DMY-NE was stable during 4 weeks investigation and could be more suitable for storage in room or lower temperature.Besides,the antioxidant activity of DMY was not affected by incorporated in the nano-emulsion.Furthermore,in vitro release of DMY exhibited sustained-release properties and the stability of DMY could be enhanced by nano-emulsion system.After in vitro digestion,the bioaccessibility of DMY was found to increase dramatically by incorporated in nano-emulsion(91.92 ± 2.05%),which means DMY-NE could effectively promote the absorption and utilization of DMY and become one of the promising strategies for the application of DMY in functional food industry.Secondly,the DMY loaded liquid or solid self-emulsifying delivery system(DMY-L-SEDS or DMY-S-SEDS)were fabricated containing 5.01% and 3.07% of DMY,respectively.And the droplet sizes of the reconstituted emulsions from DMY-L-SEDS and DMY-S-SEDS were 67.82 ± 0.20 nm and 241.00 ± 4.80 nm,respectively.Besides,the DMY-L-SEDS was stable under 4 times of heating-cooling cycles and the DMY-S-SEDS showed good resistance against various storage conditions investigated for 10 weeks.Moreover,a better antioxidant activity of DMY-S-SEDS was observed when compared with DMY which may be attributed to the addition of linseed oil in formulation.After in vitro digestion,the bioaccessibility of DMY from DMY-L-SEDS and DMY-S-SEDS were nearly 2.4 and 1.9-fold higher than that of DMY powder.Then DMY-S-SEDS was added to the gastro-floating tablet formulation to simulate the in vitro dissolution process of DMY in application.The results showed that the application of DMY-S-SEDS was feasible,and a significant improvement in cumulative dissolution of DMY could be observed.Hence,the S-SEDS could be a promising strategy for the application of DMY in functional food industry.Thirdly,the dihydromyricetin-phospholipid phytosome(DMY-PC75)was prepared with 1:2(molar ratio)as reaction ratio of DMY to phospholipid and the recombination rate was 91.26 ± 2.17%.The antioxidant activity of DMY was enhanced by phospholipid in DMY-PC75.Furthermore,the release of DMY from DMY-PC75 suggested a prolonged release profile and the bioaccessibility of DMY was also improved about 2-fold.Hence,DMY-PC75 could be a promising strategy to overcome the poor solubility and low bioavailibility of DMY for further application in functional food industry.Finally,the in vivo safety and efficacy assessment of DMY and DMY loaded micro/nano carriers were evaluated.The results revealed that DMY was relatively safe for oral administration and the micro/nano carriers could enhance the absorption of DMY without causing intestinal mucosa damage.In addition,all kinds of the micro/nano carriers prepared could improve the efficacy in anti-drunkenness of DMY significantly and the liquid micro/nano carriers could show a better effect in improving the absorption and utilization of active ingredients compared with the solid micro/nano carriers.