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

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.

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.