负载锌酞菁的SDC/TPGS混合胶束的制备与表征  

Preparation and characterization of SDC/TPGS mixed micelles loaded with Zinc phthalocyanine

作　　者：卢小鸾 付阳洋 刘佳敏 喻昌木 杨敏[1] LU Xiaoluan;FU Yangyang;LIU Jiamin;YU Changmu;YANG Min(School of Pharmaceutical Sciences,Guizhou University,Guiyang,Guizhou,550025 P.R.China)

机构地区：[1]贵州大学药学院

出　　处：《华西药学杂志》2020年第1期1-6,共6页West China Journal of Pharmaceutical Sciences

基　　金：国家自然科学基金资助项目(批准号:21562014);贵州中烟科技项目(黔烟工技[2015]8号)

摘　　要：目的制备载锌酞菁(ZnPc)的混合胶束,并进行体外评价。方法以脱氧胆酸钠(SDC)和D-α生育酚聚乙二醇琥珀酸酯(TPGS)为载体材料,采用透析法制备载ZnPc的混合胶束。结果成功制得粒径约为90 nm的棒状ZnPc-SDC/TPGS混合胶束,Zeta电位为2.58±1.61 mV,包封率为91.07%±0.24%,载药量为14.38%±0.04%。混合胶束的形成或裂解控制了单线态氧(1O2)的产生,荧光的消失使更多的能量被转移到周围的氧气以产生更多1O2。体外释放动力学表明:ZnPc缓慢释放且无突释效应。结论SDC和TPGS可通过超分子自组装形成混合胶束,体外评价表明:SDC/TPGS混合胶束是ZnPc潜在的优良载体。OBJECTIVE To prepare zinc phthalocyanine loaded mixed micelles and evaluate them in vitro.METHODS Sodium deoxycholate(SDC)and D-alpha tocopherol polyethylene glycol succinate(TPGS)were used as carriers,and the mixed micelles loaded with zinc phthalocyanine were prepared by the dialysis method.Laser particle size analyzer and transmission electron microscopy were used to characterize the size distribution,Zeta potential and morphology of micelles,whose entrapment efficiency,drug loading and release kinetics in vitro were determined and the spectral properties and the formation of singlet oxygen(1O2)were investigated.RESULTS The rod-shaped ZnPc-SDC/TPGS mixed micelles with a particle size of about 90 nm were successfully prepared.The Zeta potential was 2.58±1.61 mV,the encapsulation efficiency was 91.07%±0.24%,and the drug loading was 14.38%±0.04%.The formation or cleavage of the mixed micelle controlled the production of active 1O2,and the disappearance of fluorescence caused more energy to be transferred to the surrounding oxygen to produce more1O2,with slow release of ZnPc and no burst effect.CONCLUSION SDC and TPGS can form mixed micelles by supramolecular self-assembly.In vitro evaluation indicates that SDC/TPGS mixed micelles are potential excellent carriers for ZnPc.

关 键 词：光动力学疗法 锌酞菁 脱氧胆酸钠 D-α生育酚聚乙二醇琥珀酸酯 超分子自组装 混合胶束 单线态氧 体外评价 

分 类 号：R94[医药卫生—药剂学]