N-三甲基壳聚糖包覆牛血清白蛋白脂质体的制备及质量影响因素研究

目的:制备N-三甲基壳聚糖(TMC)包覆的牛血清白蛋白(BSA)脂质体,并考察其质量影响因素。方法:采用逆相蒸发法制备BSA脂质体,壳聚糖与碘甲烷进行季胺化反应合成TMC,用于脂质体包衣,制备TMC包覆的BSA脂质体。采用高速离心考马斯亮蓝G-250法测定包封率,考察脂类大豆卵磷脂(PC):胆固醇(CH):磷脂酰丝氨酸(PS)组成比、TMC与脂相质量比、离子强度对脂质体包封率和粒径的影响。结果:所考察因素对粒径和包封率均有影响,以脂类组成PC:CH:PS(8:9:1)、TMC与脂相质量比0.25:1、离子强度小于20 mmol·L~(-1)为宜,所制脂质体包封率为(46.82±2.07)%。结论:TMC可包覆BSA制备脂质体,所得制剂粒径均匀,稳定性好。

Factors Influencing the Preparation and Quality of Bovine Serum Albumin Liposomes Coated with N- trimethyl Chitosan

OBJECTIVE： To prepare bovine serum albumin （BSA） liposomes coated with N- trimethyl chitosan（TMC） and study the factors influencing the quality of the preparation. METHODS： BSA liposomes were prepared by the method of reverse phase evaporation. TMC polymers for coating liposomes were synthesized by quaternary amination reaction between chitosan and methyl iodide. The TMC coated BSA liposomes were prepared. The entrapment efficiency of BSA liposomes was determined by high speed centrifugation - Coomassie brilliant blue G- 250 dye method. The effects of the composition ratio of soybean lecithin （PC） ： cholesterol （CH） ： phosphatidylserine （PS）, the mass ratio of TMC to total lipid and the ionic strength on particle size and entrapment efficiency were investigated. RESULTS： All the factors investigated had influences on particle size and entrapment efficiency. The optimal formulation was as follows： PC ： CH ： PS was 8 ： 9 ： 1, TMC to lipid phase ratio was 0.25 ： 1 and ionic strength was less than 20 mmol · L^-1. The entrapment efficiency prepared in the above conditions was （46.82 ± 2.07）%. CONCLUSION： The TMC- coated BSA tiposomes were obtained successfully and the preparation had uniform particle size and good stability.