Oral squamous cell carcinoma (OSCC) is the most common malignant tumor that occurs in the oral mucosa. Pathological biopsy is still the current gold standard for OSCC diagnosis; however, some drawbacks need to be overcome. Therefore, it is urgently needed to find a non-invasive targeted technology for OSCC early diagnosis. Fluorescent optical imaging using near infrared (NIR) dyes tagged to tumor specific target will benefit such developments. Gastrin releasing peptide receptor (GRPR) is an attractive target for OSCC imaging and therapy. In this study, we synthesized nano-graphene oxide (NGO) nanoparticles with GRPR-specific peptides AF750-6Ahx-Sta-BBN via hydrogen bond and π–π bonds (NGO-BBN-AF750), and investigated their receptor binding, cell uptake and internalization in HSC-3 cells. NGO-BBN-AF750 and AF750-6Ahx-Sta-BBN showed a similar binding affinity to GRPR on HSC-3 cells. In contrast to AF750-6Ahx-Sta-BBN antagonist peptide, NGO-BBN-AF750 showed cellular internalization property. Overall, this study proposes a NGO nanoclusters-based nanoprobe for GRPR targeted near-infrared fluorescence imaging for OSCC. Nanoparticle-based delivery systems have shown highly significant potential in the delivery of a wide range of therapeutic agents.

口腔鳞状细胞癌（OSCC）是口腔黏膜中最常见的恶性肿瘤。病理活检仍是目前OSCC诊断的金标准。但是，需要克服一些缺点。因此，迫切需要找到一种用于OSCC早期诊断的非侵入性靶向技术。使用标记到肿瘤特异性靶标的近红外（NIR）染料进行的荧光光学成像将有利于这种发展。胃泌素释放肽受体（GRPR）是OSCC成像和治疗的诱人靶标。在这项研究中，我们通过氢键和π–π键（NGO-BBN-AF750）合成了具有GRPR特异性肽AF750-6Ahx-Sta-BBN的纳米氧化石墨烯（NGO）纳米颗粒，并研究了它们的受体结合，细胞摄取HSC-3细胞的内在化和内在化。NGO-BBN-AF750和AF750-6Ahx-Sta-BBN对HSC-3细胞显示出与GRPR相似的结合亲和力。与AF750-6Ahx-Sta-BBN拮抗剂肽相反，NGO-BBN-AF750显示出细胞内在化特性。总的来说，这项研究提出了一种基于NGO纳米团簇的纳米探针，用于GRPR靶向OSCC的近红外荧光成像。基于纳米颗粒的递送系统在广泛治疗剂的递送中显示出高度显着的潜力。