β-桉油醇脂质体的超临界CO_2沉析法制备与理化性质测定  

Preparation of Liposome of Beta-Eudesmol by Supercritical Carbon Dioxide Precipitation and Measurement of its Physicochemical Properties

作　　者：文震[1] 刘波[1] 郑宗坤[1] 游新奎[1] 蒲一涛[1] 李琼[2] 

机构地区：[1]深圳大学化学与化工学院,广东深圳518060 [2]华南理工大学化学与化工学院,广东广州510640

出　　处：《高校化学工程学报》2010年第1期122-126,共5页Journal of Chemical Engineering of Chinese Universities

基　　金：国家自然科学基金项目(20606013);深圳大学科研启动基金(200816);广东省绿色化学产品技术重点实验室开放基金(GC200701)

摘　　要：为提高β-桉油醇的生物利用度与肝靶向性,将其包封为脂质体。利用超临界CO2沉析技术,将脂质体膜材与β-桉油醇制成脂质体混悬液,再经真空干燥,制备了冻干β-桉油醇脂质体,并对脂质体形态、粒径、包封率、载药量、稳定性等各项理化参数进行测定与表征。考察了超临界CO2压力、温度、共溶剂乙醇在CO2中摩尔分数[x(CH3CH2OH)]等因素对脂质体制备的影响,在压力为30MPa,温度为338K、x(CH3CH2OH)=15%条件下,脂质体包封率为87.2%,载药量为5.9%,平均粒径为448.5nm。所制备的冻干β-桉油醇脂质体具有良好的复水性能,包封率、溶出度、稳定性等理化性质均符合中国药典的规定,为β-桉油醇的肝靶向药物开发提供了固体制剂中间体。β-eudesmol was incorporated into liposome in order to improve its bioavailability and target delivery to hepatic cells. The liposome suspension of β-eudesmol was formed by supercritical carbon dioxide （SC-CO2） precipitation technology and was dried by vacuum freezing. The physicochemical properties of the freeze-dried liposome of β-eudesmol, such as the structure, size, entrapment efficiency and drug loading content, were measured. The effects of pressure, temperature of SC-CO2 and mole fraction of cosolvent ethanol in SC-CO2 （x（CH3CH2OH）） on liposome formation process were discussed. Under the found optimum operation conditions of 30 MPa, 338 K and x（CH3CH2OH）=15%, the entrapment efficiency, loading content and average size of the prepared liposome are 87.2%, 5.9% and 448.5 nm, respectively. The freeze-dried liposome of β-eudesmol has the good performance of redispersion in buffer solution. The physicochemical properties of the prepared liposome of β-eudesmol, such as entrapment efficiency, dissolution rate and stability, accord with the provisions of Chinese pharmacopoeia. The results show that the prepared liposome of β-eudesmol can be used as a solid immediate for the drug of liver cancer.

关 键 词：脂质体 β-桉油醇 超临界 沉析 

分 类 号：TQ460.62[化学工程—制药化工] R944.9[医药卫生—药剂学]