Subtilisin FS33 RGDS-载酶纳米脂质体的制备与效果评价  

Preparation and Evaluation of RGDS-lipid Nanoparticles of Subtilisin FS33

作　　者：王成涛[1,2] 籍保平[2] 孙宝国[1] 曹雁平[1] 陈龙飞[2] 

机构地区：[1]北京工商大学化学与环境工程学院,北京100037 [2]中国农业大学食品科学与营养工程学院,北京100083

出　　处：《食品与发酵工业》2008年第11期1-5,共5页Food and Fermentation Industries

基　　金：国家973重点基础研究发展计划项目(2007CB707802)

摘　　要：研究评价了Subtilisin FS33 RGDS-载酶纳米脂质体的制备及其效果。按照正交设计试验确定硫酸铵梯度法制备载酶脂质体的工艺条件为:胆脂比1∶2,硫酸铵浓度为0.15 mol/L,孵化温度为45℃,酶脂比1∶1。制得的载酶脂质体粒径在50～150 nm左右,属于纳米级单室脂质体。在制备RGDS-载酶脂质体的工艺过程中,制备开始时就加入氨基酰化修饰的RGDS衍生物,其成品脂质体中RGDS含量可达到93μg/mL,并有利于分布于脂质体表面。RGDS-纳米脂质体中酶对于高温、极端pH、模拟胃肠道环境等条件的稳定性都有明显提高;酯酶存在时,脂质体中FS33释放速度明显加快,并可使血凝块完全溶解,表现出较好的溶栓效果。In order to increase bio-utilization and potential targeting of liposomes, we constructed subtilisin FS33 nano-liposome capsulation system with a synthetic peptide Arg-Gly-Asp-Ser （RGDS）, which is a specific antagonist of fibrinogen receptor on platelet membrane. In optimal condition, the nano-liposome has a diameter of 50--150 nm and therefore belongs to nano-single-room-liposome capsulation. Encapsulated FS33 in the liposome showed more tolerance to high temperature, extreme pHs, freezing and simulated intestinal juice than those untreated ones （P〈0.01）. When modified RGDS was applied at initial stages of liposome preparation, its RGDS was 93 μg/mL and was distributed in the surface of liposome. Existing esterase in pH7. 0 PBS buffer of nano-liposome capsulation system, FS33 release was remarkably quickened from nano-liposome and the blood clots gradually dissolved within 12 h （37 ℃）. This indicates that subtilisin FS33, unencapsulated and encapsulated, is capable of degrading blood clots.

关 键 词：SUBTILISIN FS33 硫酸铵梯度法 RGDS 脂质体 制备 稳定性 溶栓 

分 类 号：R94[医药卫生—药剂学]