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.%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(PEC-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细胞摄取牢和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1h达到最高浓度,而且细胞抑制率明显增大,约为3的2倍.
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