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新型聚乙二醇-聚L-赖氨酸负载四(对磺酸基偶氮苯基-4-氨基磺酰基)铝(Ⅲ)氯酞菁的纳米光敏剂的合成及离体光动力活性
Synthesis of Poly(ethylene glycol)-poly(L-lysine) Diblock Copolymer Incorporating Tetra-(p-sulfoazophenyl-4-aminosulfonyl)phthalocyanine Chloride Aluminum(Ⅲ) Polyion Nanoparticles and Its in vitro Photodynamic Therapy Efficacy
【摘要】 合成了一种新型四(对磺酸基偶氮苯基-4-氨基磺酰基)铝(Ⅲ)氯酞菁(S-AlPc),采用元素分析、IR、1H NMR和ESI-MS对配合物的结构进行了表征.S-AlPc中带负电荷的磺酸基与两亲嵌段共聚物聚乙二醇-聚L-赖氨酸(PEG-b-PLL)带正电荷的PLL嵌段通过静电作用自组装合成负载四(对磺酸基偶氮苯基-4-氨基磺酰基)铝(Ⅲ)氯酞菁聚合物纳米粒子(S-AlPc/PbP),直径约为10~20 nm.采用UV-Vis和稳态及瞬态荧光光谱法比较了S-AlPc和S-AlPc/PbP的光物理性质,并研究了它们对人脐静脉内皮细胞(HUVEC)的摄取量.与S-AlPc相比,包裹S-AlPc的聚合物纳米粒子S-AlPc/PbP的HUVEC摄取量有所提高,且提前1 h达到最大浓度.采用MTT法评价了S-AlPc和S-AlPc/PbP对HUVEC的光动力活性,S-AlPc/PbP的细胞抑制率大于S-AlPc.因此,S-AlPc/PbP是一类很有前景的第三代治疗脉络膜新生血管的光敏剂.
【Abstract】 A novel tetra-(p-sulfoazophenyl-4-aminosulfonyl)phthalocyanine aluminum(Ⅲ) chloride(S-AlPc) was synthesized and characterized by elemental analysis,IR,1H NMR and ESI-MS.Polyion nanoparticles(S-AlPc/PbP) loaded with S-AlPc were formed through electrostatic self-assemble by negatively charged sulfonate groups with positively charged PLL of the poly(ethylene glycol)-poly(L-lysine) amphiphilic diblock copolymer(PEG-b-PLL).The diameter of S-AlPc/PbP was about 10—20 nm.The photophysical properties of S-AlPc/PbP and S-AlPc were compared by UV-Vis,steady-state and time-resolved fluorescence spectroscopy.The time-depended uptake amounts of S-AlPc and S-AlPc/PbP in the human umbilical cord blood endothelial cells(HUVEC) were studied.The uptake amounts of S-AlPc/PbP by HUVEC reached maximum about one hour earlier than that of the S-AlPc.The phototoxicity of S-AlPc and S-AlPc/PbP was evaluated by MTT method.The inhibition rate of S-AlPc/PbP was also significantly increased.These results obviously indicated that S-AlPc/PbP is a potential 3rd generation photosensitizer for photodynamic therapy.
【Key words】 Phthalocyanine aluminium; Polyion nanoparticles; Photodynamic therapy efficacy; Poly(ethylene glycol)-poly(L-lysine) diblock copolymer; Photosensitizer;
- 【文献出处】 高等学校化学学报 ,Chemical Journal of Chinese Universities , 编辑部邮箱 ,2012年07期
- 【分类号】TQ460.7
- 【被引频次】3
- 【下载频次】192