呋喃二烯脂质体的制备及理化性质考察  

Preparation and physicochemical property of furanodiene liposomes

作　　者：陈宁[1] 杨静 姜伟化[1] 孙林林[1] 王琳[1] 王东凯[1] 殷栋二 

机构地区：[1]沈阳药科大学,沈阳110016 [2]海南省药品审核认证管理中心,海口570216 [3]海南碧凯药业有限公司,海口570311

出　　处：《中国新药杂志》2015年第16期1883-1889,共7页Chinese Journal of New Drugs

摘　　要：目的:制备呋喃二烯脂质体,并考察其理化性质。方法:用乙醇注入法制备呋喃二烯脂质体,在单因素试验的基础上,以磷脂浓度、脂药比和磷脂/胆固醇的比例为自变量,以包封率、载药量、粒径为因变量,采用星点设计-效应面法优化处方,并预测较优处方且进行验证,按优化条件制备脂质体,考察其粒径、Zeta电位、体外释放等理化性质。结果:最佳制备条件:磷脂浓度为11.95 mg·m L-1,脂药比为9.77,磷脂/胆固醇为8.32,此条件下制备的脂质体包封率为81.35%,载药量为4.86%,粒径为114.5 nm。结论:乙醇注入法制备的脂质体粒度均匀、包封率高、稳定性好,并有一定的缓释作用。Objective： To optimize the preparation conditions of furanodiene liposomes and to evaluate the physieochemical property. Methods： Furanodiene liposomes were prepared by an ethanol injection method. Based on the single-factor experiments, central composite design-response surface methodology involved three independent variables, namely the concentration of phospholipid, ratio of phospholipid to drug （w/w） and ratio of phospholipid to cholesterol （w/w） , and entrapment efficiency, drug loading and diameter were used as dependent variables. The predicted optimal prescription was validated and physicochemical properties of furanodiene liposomes including the particle size, zeta-potential and the release characteristics in vitro were evaluated. Results： The optimal technology was that the concentration of phospholipid was 11.95 mg· mL^-1, weight ratio of phospholipid to drug was 9.77, and weight ratio of phospholipid to cholesterol was 8.32, respectively. The entrapment rate was 81.35% , drug loading was 4.86% , and particle size was 114.5 nm on the basis of the above optimal conditions. Conclusion ： Furanodiene liposomes prepared by ethanol injection method show a high level of drug encapsulation, uniform particle size distribution and good stability. Furanodiene liposomes have sustained-release effect in vitro.

关 键 词：呋喃二烯 脂质体 星点设计-效应面法 体外释放 

分 类 号：R943.41[医药卫生—药剂学]