Liu Lanxia, Ma Guilei, Zhang Chao, Wang Hai, Sun Hongfan, Wang Chun, Song Cunxian, Kong Deling
J Biomed Nanotechnol. 2016 Jun;12(6):1223-33. doi: 10.1166/jbn.2016.2243.
Self-quenchable indocyanine green (ICG)-encapsulated micelles with folic acid (FA)-targeting specificity (FA-ICG-micelles) were developed for biologically activatable photodynamic theranostics. FA-ICG-micelles were successfully prepared using the thin-film hydration method, which allows ICG to be encapsulated with a high drug loading that induces an efficient ICG-based quenched state. FA-ICG-micelles are initially in the "OFF" state with no fluorescence signal or phototoxicity, but they become highly fluorescent and phototoxic in cellular degradative environments. Importantly, via folate receptor-mediated endocytosis, the FA targeting of FA-ICG-micelles enhanced intracellular uptake and photodynamic therapy (PDT) efficacy. Systematic administration of FA-ICG-micelles to folate receptor-positive tumor-bearing mice elicited prolonged blood circulation, enhanced tumor accumulation and improved therapeutic efficiency compared to free ICG. Therefore, based on the FA-targeted specificity and switchable photoactivity, FA-ICG-micelles have potential for photodynamic theranostics in cancer.
为实现生物可激活的光动力诊疗，研发了具有叶酸（FA）靶向特异性的自猝灭吲哚菁绿（ICG）包裹的胶束（FA-ICG-胶束）。采用薄膜水化法成功制备了FA-ICG-胶束，该方法可使ICG以高载药量包裹，从而诱导高效的基于ICG的猝灭状态。FA-ICG-胶束最初处于“关闭”状态，无荧光信号或光毒性，但在细胞降解环境中会变得具有高荧光性和光毒性。重要的是，通过叶酸受体介导的内吞作用，FA-ICG-胶束的FA靶向作用增强了细胞内摄取和光动力疗法（PDT）的疗效。与游离ICG相比，向叶酸受体阳性荷瘤小鼠全身给药FA-ICG-胶束可延长血液循环时间，增强肿瘤蓄积并提高治疗效率。因此，基于FA靶向特异性和可切换的光活性，FA-ICG-胶束在癌症光动力诊疗方面具有潜力。
