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脂质体中共包封二乙基二硫代氨基甲酸钠(DETC)和锌酞菁(ZnPc)可提高光毒性活性,对抗(MDA-MB-231)人乳腺癌细胞。

Co-encapsulation of sodium diethyldithiocarbamate (DETC) and zinc phthalocyanine (ZnPc) in liposomes promotes increases phototoxic activity against (MDA-MB 231) human breast cancer cells.

机构信息

Department of Chemical Engineering and Food Engineering, Federal University of Santa Catarina, Brazil; Postgraduate Program in Health Science, University of the Extreme South Santa Catarina, Brazil.

Department of Chemical Engineering and Food Engineering, Federal University of Santa Catarina, Brazil.

出版信息

Colloids Surf B Biointerfaces. 2021 Jan;197:111434. doi: 10.1016/j.colsurfb.2020.111434. Epub 2020 Nov 4.

DOI:10.1016/j.colsurfb.2020.111434
PMID:33166932
Abstract

There has been considerable interest in the development of novel photosensitisers for photodynamic therapy (PDT). The use of liposomes as drug delivery systems containing simultaneously two or more drugs is an attractive idea to create a new platform for PDT application. Therefore, the aim of this study was to evaluate the synergistic effect of diethyldithiocarbamate (DETC) and zinc phthalocyanine (PDT) co-encapsulated in liposomes. The reverse-phase evaporation method resulted in the successful encapsulation of DETC and ZnPc in liposomes, with encapsulation efficiencies above 85 %, mean size of 308 nm, and zeta potential of - 36 mV. The co-encapsulation decreased the cytotoxic effects in mouse embryo fibroblast (NIH3T3) cells and inhibited damage to human erythrocytes compared to free DETC + ZnPc. In addition, both the free drugs and co-encapsulated ones promoted more pronounced phototoxic effects on human breast cancer cells (MDA-MB231) compared to treatment with ZnPc alone. This synergistic effect was determined by DETC-induced decreases in the antioxidant enzyme activity of superoxide dismutase (SOD) and glutathione (GSH).

摘要

人们对开发用于光动力疗法 (PDT) 的新型光敏剂产生了浓厚的兴趣。使用脂质体作为同时包含两种或更多种药物的药物递送系统是创建 PDT 应用新平台的一个有吸引力的想法。因此,本研究的目的是评估二乙基二硫代氨基甲酸盐 (DETC) 和锌酞菁 (PDT) 共同包封在脂质体中的协同作用。反相蒸发法成功地将 DETC 和 ZnPc 包封在脂质体中,包封效率超过 85%,平均粒径为 308nm,zeta 电位为-36mV。与游离的 DETC+ZnPc 相比,共包封降低了对小鼠胚胎成纤维细胞 (NIH3T3) 细胞的细胞毒性作用,并抑制了对人红细胞的损伤。此外,与单独使用 ZnPc 相比,游离药物和共包封药物都能更显著地对人乳腺癌细胞 (MDA-MB231) 产生光毒性作用。这种协同作用是由 DETC 诱导的超氧化物歧化酶 (SOD) 和谷胱甘肽 (GSH) 的抗氧化酶活性降低所决定的。

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