氧化甾醇-磷脂脂质囊泡的制备及特性研究  

Preparation and Characteristics of Oxysterol-Phospholipid Vesicles

作　　者：汤文星[1] 郑思嘉[1] 王荣昌[1] 游秀华[1] 冷田东[2] 胡海燕[1] 颜光美[2] 

机构地区：[1]中山大学药学院,广东广州510006 [2]中山大学中山医学院,广东广州510080

出　　处：《中山大学学报（自然科学版）》2009年第4期73-77,共5页Acta Scientiarum Naturalium Universitatis Sunyatseni

基　　金：国家"863"计划资助项目(2006AA090502);广东省医学科学基金资助项目(B2007032)

摘　　要：氧化甾醇3,19?二羟基-胆甾烷-24-酮(DHCO)和3,β5,α6β-胆甾烷三醇(Triol)替代胆甾醇与大豆磷脂形成脂质囊泡的性质研究。采用乙醇注入法制备脂质囊泡,通过测定脂溶性及水溶性荧光探针在脂质囊泡中的荧光强度变化,考察囊泡膜流动性及通透性;通过测定脂质囊泡中游离DHCO及结合DHCO的浓度考察DHCO与磷脂的结合率;考察DHCO/磷脂比例、超声条件对脂质囊泡粒径大小和分布的影响。结果表明,DHCO、Triol与磷脂形成的脂质囊泡与胆甾烷(CHOL)-磷脂脂质囊泡的膜流动性无明显差异,但膜通透性稍有增大。DHCO与磷脂的结合率为82.58%。DHCO、Triol与大豆磷脂经简单工艺即可形成脂质囊泡。可通过调节DHCO/磷脂比例、超声条件获得具理想粒径和外观的脂质囊泡。氧化甾醇数量庞大,其作为脂质囊泡的新型"流动性缓冲剂"有巨大的发展潜力。To study characteristics of oxysterol-phospholipid vesicles using 3, 19-hydroxyl-cholestane -24 - one （DHCO） and 313, 5or, 613-cholestane-triol （Triol） as oxysterols, respectively. Oxysterolphospholipid vesicles were prepared by the ethanol-inpouring method. To measure fluidity and permeability of vesicles membrane, fluorescent intensities of lipophilic and hydrophilic fluorescence probes in the vesicles were determined. The inding percentage of DHCO and phospholipid to form vesicles was obtained by determining free and combined DHCO in DHCO-phospholipid vesicles solution. The effect of the ratio of DHCO to phospholipids and ultrasonic condition on the vesicle particle sizes and polydispersion index （PDI） was also investigated. DHCO-versicles and Triol-vesicles had no significant difference in membrane fluidity from cholesterol （CHOL） -vesicles, but resulted in larger permeability than CHOL-vesicles. The binding percentage of DHCO and phosoholioid was 82. 58%. The DHCO-vesivesicles can be easily prepared by simple preparing process. DHCO-versicles with desired sizes and PDI could be obtained by optimizing the ratio of DHCO to phospholipid and the ultrasound condition. Depending on a huge database of numerous steroids, oxysterols could be Viewed as potential ＂ flowability buffers＂ in the development of vesicles.

关 键 词：氧化甾醇 大豆磷脂 脂质囊泡 特性研究 

分 类 号：R944.9[医药卫生—药剂学]