姜黄素半乳糖化十六酰壳聚糖聚合物胶束的制备  

Preparation of curcumin-loaded galactosylated hexadecanoyl chitosan polymeric micelles

作　　者：姜羽凤[1] 王晓明[1] 胡巧红[1,2] 黎燕君[1] 

机构地区：[1]广东药学院药剂系,广东广州510006 [2]广东药学院临床药学系,广东广州510006

出　　处：《广东药学院学报》2012年第5期465-469,共5页Academic Journal of Guangdong College of Pharmacy

基　　金：广东省自然科学基金项目(8151022401000021);广东省科技计划项目(2009B030801346)

摘　　要：目的制备姜黄素半乳糖化棕榈酰壳聚糖聚合物胶束,并考察制备工艺对包封率和载药量的影响。方法以半乳糖化十六酰壳聚糖(GHC)为载体材料,采用乳化-溶剂挥发法制备姜黄素聚合物胶束;应用正交试验考察药物∶载体质量比、油相∶水相体积比、超声时间对载药聚合物胶束包封率和载药量的影响,以对制备工艺进行优化;以透射电镜(TEM)和动态光散射粒度分析仪(DLS)对聚合物胶束的形态、粒径和Zeta电位进行测定。结果药物∶载体质量比对胶束的包封率和载药量影响最大,其次为油相∶水相体积比和超声时间。最佳条件为药物∶载体质量比为1∶15,油相∶水相体积比为1∶7,超声时间为30min。制备的载药胶束的形状为球形,大小均匀,平均粒径为179.7 nm,Zeta电位约为76.46 mV,包封率为96.3%,载药量为9.1%。结论所采用的乳化-溶剂挥发法制备工艺适于制备姜黄素聚合物胶束。Objective To prepare curcumin-loaded galactosylated hexadecanoyl chitosan polymeric micelles,and observe the effect of preparation process on encapsulation efficiency and drug loading.Methods With galactosylated hexadecanoyl chitosan（GHC） as drug carrier,curcumin-loaded polymeric micelles were prepared by emulsifying-solvent evaporation technique.With encapsulation efficiency and drug loading as indexes,orthogonal design experiment was used to optimize drug ∶carrier ratio,oil ∶water phase volume ratio and ultrasonic time.The morphology of polymeric micelles was observed by transmission electron microscope（TEM）.The particle size and zeta potential were determined by dynamic light scattering particle size analyzer（DLS）.Results The optimal formulation and process were as follows： the ratio of drug to carrier material was 1∶15,the ratio of oil phase to water phase was 1∶7,and the ultrasound time was 30 minutes.The drug loading and encapsulation efficiency were 9.1% and 96.3%,respectively.The results showed that polymeric micelles were spherical and uniform.The average particle size and Zeta potential were 179.7 nm and 76.46 mV,respectively.Conclusion The emulsifying-solvent evaporation technique is suitable for preparing curcumin-loaded polymeric micelles.

关 键 词：半乳糖化十六酰壳聚糖 乳化-溶剂挥发法 姜黄素 聚合物胶束 

分 类 号：R283[医药卫生—中药学]