This work develops a new multifunctional biocompatible anticancer nanoformulation to provide targeted image-guided cancer-selective therapeutics. It consists of three active covalently bound components: (1) biocompatible nitrogen-doped graphene quantum dots (GQDs) as a multifunctional delivery and imaging platform, (2) hyaluronic acid (HA) unit targeted to the CD44 receptors on a variety of cancer cells, and (3) oxidative stress-based cancer-selective ferrocene (Fc) therapeutic. The biocompatible GQD platform synthesized from glucosamine exhibits high-yield intrinsic fluorescence. It is utilized for tracking Fc-GQD-HA formulation in vitro indicating internalization enhancement in HeLa cells targeted by the HA over non-cancer HEK-293 cells not overexpressing CD44 receptor. Fc-GQD-HA, non-toxic at 1 mg/mL to HEK-293 cells, induces cytotoxic response in HeLa enhanced over time, while therapeutic ROS generation by Fc-GQD-HA is ~3 times greater than that of Fc alone. This outlines the targeted delivery, imaging, and cancer-specific treatment capabilities of the new Fc-GQD-HA formulation enabling desired cancer-focused nanotherapeutic approach.

这项工作开发了一种新的多功能生物相容性抗癌纳米制剂，以提供靶向图像引导的癌症选择性治疗。它由三个共价结合的活性成分组成：(1) 生物相容的氮掺杂石墨烯量子点 (GQD) 作为多功能传递和成像平台，(2) 靶向各种癌细胞上 CD44 受体的透明质酸 (HA) 单元和 (3) 基于氧化应激的癌症选择性二茂铁 (Fc) 治疗剂。由氨基葡萄糖合成的生物相容性 GQD 平台表现出高产的内在荧光。它用于在体外跟踪 Fc-GQD-HA 制剂，表明 HA 靶向的 HeLa 细胞相对于未过度表达 CD44 受体的非癌 HEK-293 细胞的内化增强。Fc-GQD-HA，1 时无毒 mg/mL 到 HEK-293 细胞，诱导 HeLa 中的细胞毒性反应随着时间的推移而增强，而 Fc-GQD-HA 产生的治疗性 ROS 比单独的 Fc 高约 3 倍。这概述了新的 Fc-GQD-HA 制剂的靶向递送、成像和癌症特异性治疗能力，从而实现了所需的以癌症为中心的纳米治疗方法。