The purpose of this research was to prepare silibininloaded nano sized liposomes to improve their aqueous solubility and to optimize the preparation method. For the preparation, specific amount of cholesterol was dissolved into ethanol. After that, phosphatidylcholine from egg yolk (~60%) was dissolved into mixture about 20, 40, and 60 mg/mL, and subsequently, silibin in was dissolved into organic phase at approximate 250, 500, and 1000 μg/mL, respectively. The organic phase was regularly injected at 0.9 mL/min into phosphate buffered saline (PBS) using peristaltic pump under stirring. Liposomes were formed spontaneously as soon as lipid phase was in contact with the aqueous phase. Then, the liposome suspension was kept under stirring for 15 min. Thereafter, ethanol was removed by rotary evaporation under reduced pressure. As the result, silibin in loaded liposomes were circular shape which had lipid bilayer at edge of the liposome droplets and were multilamellarvesicles. In addition, average size of silibinin loaded liposome droplets were 148.27, 144.52, and 173.46 nm at 250, 500, and 1000 μg/mL silibinin concentrations, respectively. Zeta potentials of liposome particles were showed about -9.64, -12.03, and -12.79 mV. As concentration of phosphatidylcholine in ethanol increased, droplet size and zeta potential of the liposome increased. The average encapsulation efficiency of obtained liposome suspensions was 57.6%. In conclusion, the liposome preparation method established can be used to encapsulate various hydrophobic bioactives for food application such as beverage.
Silibinin, the major active constituent of silymarin, was known as having hepatoprotective effects against oxidative stress of the liver. However, it has poor oral bioavailability. Therefore, the purpose of this research was to prepare silibinin loaded nano sized liposomes to improve their bioavailability and to optimize the preparation method. Liposomes were prepared by ethanol injection method. An aqueous phase was prepared by adding tween 80 into phosphate buffer saline. Subsequently, a lipid phase was composed of phosphatidylcholine, cholesterol, and silibinin and they were mixed in a mass ratio of 8:1.2:1, respectively, at 60℃ and dissolved in absolute ethanol. After all compounds in the lipid phase was dissolved fully, the lipid phase was injected into an aqueous phase and was stirred at 500rpm, 60℃ for 30 min. Thereafter, ethanol in the mixture was removed by rotary evaporator and subsequently high pressure homogenizer was applied to the mixture at 120 Mpa to obtain nano size liposomes. As a result, silibinin loaded liposomes were obtained and they were circular shape which had lipid bilayer at edge of the liposome droplets and were multilamellar vesicles. Average size of the silibinin loaded liposomes were about 70-110 nm. As the faster injecting speed applied, the smaller particles size showed. In conclusion, the liposome preparation method can be used to encapsulate various functional bioactives for food application such as beverage.