IR780-loaded TPGS-TOS micelles for breast cancer photodynamic therapy

• Published in: European journal of pharmaceutics and biopharmaceutics Vol. 113; pp. 108 - 117
• Main Authors: Pais-Silva, Cleide, de Melo-Diogo, Duarte, Correia, Ilídio J.
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 01-04-2017
• Subjects: Biocompatible Materials; Breast cancer; Breast Neoplasms - drug therapy; Female; Humans; Indoles - administration & dosage; Indoles - therapeutic use; IR780 iodide; MCF-7 Cells; Micelles; Microscopy, Electron, Transmission; Photochemotherapy; Photodynamic therapy; Photothermal therapy; TPGS-TOS micelles; TPGS-TOS micelles; FDA; IR780-TTM; NP; RT; IR780 iodide; EPR; MCF-7; DLS; TPGS; Photothermal therapy; PTT; PDI; ANOVA; FBS; IC50; EMA; CLSM; EE; PBS; PDT; Photodynamic therapy; Breast cancer; DMEM-F12; H2DCF-DA; Dox; PEG; NIR; LC; ROS; MetOH; TOS; TEM
• ISSN: 0939-6411; 1873-3441
• DOI: 10.1016/j.ejpb.2017.01.002

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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.