Extraction And Purification Of β-arbutin From Pear Leaves And Study On The Characteristics Of Phospholipid Complex

Arbutin(4-hydroxyphenyl-β-D-glucopyranoside)is widely found in natural plants such as pears,blueberries,bearberries,and bilberries.The main drug functions of arbutin are: whitening,antibacterial,antitussive,antiasthmatic and so on.In this paper,pear leaves,a waste of agriculture and forestry,were used as raw materials to extract and separate arbutin,and the process conditions were optimized.The treatment effect of strong hydrophilic arbutin during skin administration was not good.Phospholipid compound technology using phospholipids as raw materials could effectively improve drug solubility and biomembrane permeability,and increase the body’s absorption of drugs.Arbutin phospholipid complex was prepared in this paper,and evaluated the structure formation,in vitro release,transdermal penetration,tyrosinase inhibitory effect and antioxidant activity.The main conclusions of the study were as follows:1.In the single factor experiments,the maximum arbutin extraction amounts of subcritical water extraction and organic solvent extraction were 14.3 mg/g and 12.3 mg/g,respectively,and the subcritical water extraction showed higher antioxidant activity.Therefore,the subcritical water extraction process was further optimized by response surface technology,under the conditions of time,temperature and material-to-liquid ratio of 52.23 min,201.18 ℃,and 1:42.8 respectively,and the predicted extraction amount of arbutin was 15.69 mg/g.The response surface prediction conditions were used for extraction,and 15.12 mg/g was the actual extraction amount of arbutin.2.The performance of various resin purification extracts was compared.The adsorption rate of XDA-1 was 94.2% and the desorption rate was 75.7%,which had good adsorption and desorption performance.Therefore,the XDA-1 resin was selected for the next study.The influencing factors of XDA-1 resin were investigated,and it was found that when the sample flow rate of the extract was 1 BV/h and the elution flow rate of 40% ethanol solution was 1.5 BV/h,the content of arbutin in the product obtained could reach67.2%.3.Four types of lipid carriers: ethosomes,W/O/W emulsion,nano-structured lipid carrier and phospholipid complex were prepared to improve the lipid solubility and bioavailability of arbutin.Among them,the phospholipid complex drug loading was 23%,much higher than the other three lipid carriers,so the phospholipid complex was used for further research.The characterization results of the phospholipid complex showed that the weak interaction between phospholipid and arbutin molecules formed complex.The in vitro release rate of arbutin in the phospholipid complex was slowed by 38.8%after 2 h,which increased the sustained release time of arbutin,and the cumulative amount of phospholipid complex penetration and skin deposition rate were increased to 23.5 and 1.75 times of arbutin respectively.At a concentration of 0.1 mg/m L,the inhibitory capacity of tyrosinase was 1.47 times that of arbutin,and phospholipid complex also showed higher in vitro antioxidant activity than arbutin.