肝靶向牛血清白蛋白脂质体的制备及理化性质研究

Studies on preparation of hepatic-targeted bovine serum albumin liposome and its physicochemical properties

目的:研制肝靶向牛血清白蛋白(bovine serum albumin,BSA)脂质体,并研究其理化性质,为蛋白质药物的肝靶向给药提供一种新模型。方法:首先采用逆相蒸发法制备BSA负电荷脂质体,再用O-羧甲基-N-乳糖酰化壳聚糖(O-carboxymethyl N-galactosylated chitosan,Gal-CMCS)修饰,制备肝靶向BSA脂质体,并考察脂质体的形态、粒径、Zeta电位、包封率及稳定性等理化性质。结果:制得的肝靶向BSA脂质体在电镜下呈类圆形,粒径分布均匀,平均粒径为(284.1±5.41)nm,BSA包封率为(34.21±1.73)%,Zeta电位为(+27.1±1.17)mV,4℃下放置3个月粒径和包封率无明显变化。结论:成功制备了肝靶向BSA脂质体,其具有良好的稳定性和较高的药物包封率,可作为蛋白质药物肝靶向给药的一种新模型。

Objective：To prepare the hepatic-targeted Bovine serum albumin（BSA）liposome and study its physicochemical properties, to providing a new hepatic-targeted drug delivery system for protein-drug, nethods：Liposome was prepared by reverse phase evaporation method,and then the liposome was coated with O-carboxymethyl N-galactosylated chitosan （Gal-CMCS）. The shape,particle size,Zeta potential,entrapment efficiency and stability were investigated. Results：Hepatic-targeted BSA liposome was round and uniform;its mean particle size was（284.1 ±5.41 ）nm;the entrapment efficiency was（34.21±1.73）%; Zeta potential was（＋27.1 ±1.17） mV; and there was no obvious change in entrapment efficiency and particle size at 4℃ within 3 months. Conelusion：The hepatic-targeted BSA liposome was successfully prepared,with good stability and high entrapment effieieney,thus providing a new hepatic-targeted drug delivery system for protein-drug.