The development of new photodynamic therapy (PDT) agents designed for bladder cancer (BC) treatments is of utmost importance to prevent its recurrence and progression towards more invasive forms. Here, three different porphyrinic photosensitizers (PS) (TMPyP, Zn-TMPyP, and P1-C₅) were non-covalently loaded onto graphene oxide (GO) or graphene quantum dots (GQDs) in a one-step process. The cytotoxic effects of the free PS and of the corresponding hybrids were compared upon blue (BL) and red-light (RL) exposure on T24 human BC cells. In addition, intracellular reactive oxygen species (ROS) and singlet oxygen generation were measured. TMPyP and Zn-TMPyP showed higher efficiency under BL (IC₅₀: 0.42 and 0.22 μm, respectively), while P1-C₅ was more active under RL (IC₅₀: 0.14 μm). In general, these PS could induce apoptotic cell death through lysosomes damage. The in vitro photosensitizing activity of the PS was not compromised after their immobilization onto graphene-based nanomaterials, with being the most promising hybrid system under RL (IC₅₀: 0.37 μg/mL). Overall, our data confirm that GO and GQDs may represent valid platforms for PS delivery, without altering their performance for PDT on BC cells. View Full-Text

中文翻译：

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氧化石墨烯和石墨烯量子点作为阳离子卟啉的传递系统：对 T24 人膀胱癌细胞的光抗增殖活性评估

开发用于膀胱癌 (BC) 治疗的新型光动力疗法 (PDT) 药剂对于防止其复发和向更具侵袭性的形式发展至关重要。在这里，三种不同的卟啉光敏剂 (PS)（TMPyP、Zn-TMPyP 和 P1-C ₅）通过一步过程非共价加载到氧化石墨烯（GO）或石墨烯量子点（GQD）上。在 T24 人 BC 细胞上的蓝光 (BL) 和红光 (RL) 暴露后，比较了游离 PS 和相应杂交体的细胞毒性作用。此外，还测量了细胞内活性氧 (ROS) 和单线态氧的产生。TMPyP 和 Zn-TMPyP 在 BL 下表现出更高的效率（IC ₅₀分别为 0.42 和 0.22 μm），而 P1-C ₅在 RL (IC ₅₀ : 0.14 μm)下更活跃。一般来说，这些 PS 可以通过溶酶体损伤诱导细胞凋亡。PS 固定在基于石墨烯的纳米材料上后，其体外光敏活性并未受到影响，是 RL 下最有前途的混合系统（IC ₅₀ : 0.37 μg/mL）。总体而言，我们的数据证实 GO 和 GQD 可能代表有效的 PS 传递平台，而不会改变它们在 BC 细胞上的 PDT 性能。查看全文