Synthesis Of Phytosterol Dicarboxylates And Preparation Of Its Nanoliposome

Phytosterol is widely found in nuts, seeds and vegetable oils, is present in otherplant-based foods and fruits and vegetables, it has no toxic side effects on human body,and has a high physiological activity, its structural characteristics determine variousphysiological activity and extensive use. The researchers at home and abroad for themodification of phytosterol conducted in-depth research, created a variety of phytosterolderivatives through various methods.With phytosterol as reaction substrate, synthesized of the four phytosterolderivatives, its structure determined by FT-IR,1H NMR,13C NMR analysis means. Insynthesized of phytosterol adipic acid monoester as an example, through the singlefactor and orthogonal experiments, xylene as the reaction solvent and water carrier atthe same time, the molar ratio of adipic acid and phytosterol2:1, and the reaction timewas8h, the reaction temperature was140℃, the amount of catalyst was5%, the yieldcould reached96.05%.Synthesized of phytosterol monocarboxylates mixture, when the commencement ofagent for petroleum ether (60-90): ethyl acetate (v/v)=3:1, could realized phytosteroland phytosterol monocarboxylates of separation. Used silica gel columnchromatography for separation and purification of phytosterol monocarboxylates, whenpacked silica gel particle size was200~300mesh, packed height was65cm, silica gelcolumn separation weight of sample was1.500g, eluent petroleum ether (60-90): ethylacetate (v/v)=3:1, flow rate of1.4mL/min, the recovery rate of phytosterol succinatemonoester was95.4%, the recovery rate of phytosterol adipic acid monoester,phytosterol azelaic acid monoester and phytosterol sebacic acid monoester was96.2%,92.1%,90.6%respectively.Process for the preparation of phytosterol succinate monoester nanoliposomeswas studied, in phytosterol succinate monoester was120.0mg, tributyrin was20.0mg,Tween80was30.0mg, with10mL of anhydrous ethanol was melted, injected with asyringe into60mL pH uniform as6.8,0.01mol/L phosphate buffer solution, theaqueous phase temperature was50℃, using a rotary evaporator to remove residualethanol, and finally treated with an ultrasonic power was300W (1s on,1s off),ultrasonic time of60s, the prepared nanoliposome particle size of around100nm, Zetapotential in the vicinity of-40.0mV. Preparation of encapsulated drugs troxerutin nanoliposome, the influential factorsof the envelopment rate were investigated. When the weight of phytosterol succinatemonoester was120.0mg, tributyrin weight was20.0mg, pH6.8aqueous medium phase,the volume ratio of oil phase to aqueous phase was1:6, water bath temperature of50℃,the weight of troxerutin was7.0mg, the highest for the encapsulation of troxerutin ratewas65.4%.