Pais-Silva Cleide, de Melo-Diogo Duarte, Correia Ilídio J
CICS-UBI - Centro de Investigação em Ciências da Saúde, Universidade da Beira Interior, Avenida Infante D. Henrique, 6200-506 Covilhã, Portugal.
CICS-UBI - Centro de Investigação em Ciências da Saúde, Universidade da Beira Interior, Avenida Infante D. Henrique, 6200-506 Covilhã, Portugal.
Eur J Pharm Biopharm. 2017 Apr;113:108-117. doi: 10.1016/j.ejpb.2017.01.002. Epub 2017 Jan 11.
IR780 iodide is a near-infrared (NIR) dye with a huge potential for cancer imaging and phototherapy. However, its biomedical application is strongly impaired by its lipophilic character. Herein, amphiphilic micelles based on d-α-tocopheryl polyethylene glycol succinate (TPGS) and d-α-tocopheryl succinate (TOS), two vitamin E derivatives with intrinsic anticancer activity, are explored to load IR780. IR780-loaded micelles with suitable sizes are obtained by using specific TPGS and TOS weight feed ratios during micelles formulation and these are able to encapsulate IR780 with high efficiency. In in vitro assays, the IR780-loaded micelles induce a cytotoxic effect in cancer cells upon exposure to NIR irradiation through the generation of reactive oxygen species (photodynamic therapy). This effective ablation of cancer cells is achieved using an ultra-low IR780 concentration. Moreover, IR780-loaded micelles also have the ability to act as photothermal and imaging agents, which widens their therapeutic and diagnostic potential. Overall, TPGS-TOS micelles are promising nanoplatforms for IR780-mediated cancer phototherapy and imaging.
IR780碘化物是一种近红外（NIR）染料，在癌症成像和光疗方面具有巨大潜力。然而，其亲脂性严重阻碍了它的生物医学应用。在此，基于d-α-生育酚聚乙二醇琥珀酸酯（TPGS）和d-α-生育酚琥珀酸酯（TOS）这两种具有内在抗癌活性的维生素E衍生物，探索了两亲性胶束用于负载IR780。在胶束制备过程中，通过使用特定的TPGS和TOS重量进料比，获得了具有合适尺寸的负载IR780的胶束，这些胶束能够高效包封IR780。在体外试验中，负载IR780的胶束在近红外照射下，通过产生活性氧（光动力疗法）对癌细胞产生细胞毒性作用。使用超低浓度的IR780就能实现对癌细胞的有效消融。此外，负载IR780的胶束还具有作为光热和成像剂的能力，这拓宽了它们的治疗和诊断潜力。总体而言，TPGS-TOS胶束是用于IR780介导的癌症光疗和成像的有前景的纳米平台。
