主动载药法制备盐酸小檗碱脂质体

 目的　采用主动载药法制备盐酸小檗碱脂质体,并考察其包封率的影响因素。方法　以阳离子交换树脂法分离脂质体,于347nm处测定吸光度,计算包封率;考察加药顺序、孵化时间、孵化温度、外水相pH值及粒径对包封率的影响。 结果　被动载药法得到的包封率仅有13.3%,主动载药法的包封率最高可达84.6%。主动载药法中,加药顺序不同,得到的包封率亦有不同;包封率随着孵化温度的升高和孵化时间的增加有提高的趋势;外水相最佳pH值为6.8;粒径小,包封率高。 结论　主动载药法适于制备盐酸小檗碱脂质体。

Preparation of berberine hydrochloride liposomes by active loading method

OBJECTIVE To prepare berberine hydrochloride liposomes by active loading method,and study the influence of different factors on the entrapment efficiency.METHODS Cation exchange resin was used to separate the free berberine hydrochloride (Ber) from the liposomes.UV spectrophotometry at 347nm was used to determine the entrapment efficiency of Ber liposomes,which diminished the interference of phosphatidyl choline on Ber.The influences of various factors,including adding sequence,incubation time,incubation temperature,pH value of external water phase and the particle size of the lipsome,on the entrapment efficiency were investigated.RESULTS The entrapment efficiency with passive loading was only 13.3%;while up to 84.6% with active loading method.Different entrapment efficiencies were obtained with different adding sequence.Entrapment efficiency was enhanced by increasing incubation time and temperature,and decreasing particle size.The optimal pH value of external water phase was 6.8.CONCLUSION Active loading is suitable for preparing berberine hydrochloride liposome.