负载空间链四(6-氨基己酸磺酰基)铝氯酞菁聚合物纳米粒子的合成及其离体光动力活性  

Synthesis of Polyion Micelle Incorporating Tetra-(6-carboxylic aminohexanoicsulfonyl) Phthalocyanine Aluminum(Ⅲ) and Its in vitro Photodynamic Therapy Efficacy

作　　者：陈莉莉[1] 彭亦如[1] 林萍萍[1] 阙寿林[1] 黄丽珊[1] 陈奎治[1] 徐国兴[2] 

机构地区：[1]福建师范大学化学与材料学院,福州350007 [2]福建医科大学附属第一医院．福州350005

出　　处：《无机化学学报》2011年第2期327-332,共6页Chinese Journal of Inorganic Chemistry

基　　金：国家自然科学基金(No.20604007);福建省自然科学基金(No.2008J0078);卫生部科学研究基金(No.WKJ2008-2-61);福建省科技厅重点项目(2007I0013)资助项目

摘　　要：以四磺酸铝氯酞菁1为原料,采用氨基转化法,经磺酰氯化和Hinsberg磺酰胺化反应合成四磺酰铝氯酞菁2和四(6-氨基己酸磺酰基)铝氯酞菁3,产物结构经元素分析,IR,1HNMR和MS-ESI表征。3在磷酸盐缓冲溶液中与两亲嵌段共聚物聚乙二醇-聚-L-赖氨酸(PEG-b-PLL)通过静电自组装,形成负载3的聚合物纳米粒子3/m。原子力显微镜(AFM)和透射电子显微镜(TEM)表明3/m具有球形核壳结构,直径约为10～20 nm。紫外-可见吸收光谱和荧光光谱法研究了3/m的光物理性质。通过对不同孵育时间的人脐带血内皮细胞(HUVEC)摄取药代动力学测定3/m细胞摄取率和MTT法评价3/m的离体光动力活性,相对自由酞菁3,3/m的细胞摄取率大大提高,且提前1 h达到最高浓度,而且细胞抑制率明显增大,约为3的2倍。Tetrachlorosulfonyl phthalocyanine aluminium（2） and tetra（6-carboxyl-aminohexanoicsulfonyl） phthalocyanine aluminium（3） were synthesized from（1） via sulfonylic chlorization and amidation reaction.The structures of above compounds were characterized by 1H NMR,IR,MS and elemental analysis.The polymeric micelle（3/m） was formed via an electrostatic interaction of anionic phthalocyanine aluminum and poly（ethylene glycol）-poly（L-lysine） block copolymers（PEG-b-PLL） in PBS buffer solution.AFM and TEM showed that 3/m formed spherical nanoparticles with a diameter of 10～20 nm.The photophysical properties of 3/m were changed compared to that of compound 3.The time-dependent uptake amount of 3/m in HUVEC cell showed that the uptake amount of 3/m was significantly increased and reached peak value by ahead of an hour compared with that of 3.The in vitro photodynamic therapy efficacy of 3 and 3/m were evaluated by MTT methods.The results indicated that the in vitro photodynamic therapy efficacy of 3/m was ca.2 fold compared to that of free phthalocyanine 3.

关 键 词：酞菁铝 空间链 聚合物纳米粒子 聚乙二醇单甲醚-聚-L-赖氨酸 合成 光动力活性 

分 类 号：O611.4[理学—无机化学] R979.1[理学—化学]