Chemotherapy for the treatment of nasopharyngeal carcinoma (NPC) is usually associated with many side effects; therefore, its treatment options have not yet been completely resolved. Improving distribution to the targeted tumor region and enhancing the cellular uptake of drugs can efficiently alleviate the above adverse medical effects. Near-infrared (NIR) laser light-mediated photothermal therapy (PTT) and photodynamic therapy (PDT) are promising strategies for cancer treatment. In the present study, we developed an efficient multifunctional nanocluster with enhanced targeting and aggregation efficiency for PTT and PDT that is composed of a biocompatible folic acid (FA), indocyanine green (ICG) and 2-cyanobenzothiazole (CBT)-functionalized peptide labeled with an aldehyde sodium alginate-modified magnetic iron oxide nanoparticle (ASA-MNP)-based nanocarrier. FA can bind to folate receptors on cancer cell membranes to enhance nanocluster uptake. CBT-modified peptide can react with glutathione (GSH), which is typically present at higher levels in cancer cells, to form intracellular aggregates and increase the local concentration of the nanodrug. In in vitro studies, these nanodrugs displayed the desired uptake capacity by NPC cells and the ability to suppress the growth of cancer cells under laser irradiation. Animal studies validated that these nanodrugs are safe and nontoxic, efficiently accumulate in NPC tumor sites following injection via the caudal vein, and shows superior inhibition of tumor growth in a tumor-bearing mouse model upon near-infrared laser irradiation. The results indicate the potential application of the multifunctional nanoparticles (NPs), which can be used as a new method for the treatment of folate receptor-positive NPC.

用于治疗鼻咽癌 (NPC) 的化疗通常会带来许多副作用；因此，其治疗方案尚未完全解决。改善靶向肿瘤区域的分布，增强细胞对药物的吸收，可以有效缓解上述不良医学效应。近红外 (NIR) 激光光介导的光热疗法 (PTT) 和光动力疗法 (PDT) 是有前景的癌症治疗策略。在本研究中，我们开发了一种高效的多功能纳米团簇，具有增强的 PTT 和 PDT 靶向和聚集效率，由生物相容性叶酸（FA）组成，吲哚菁绿 (ICG) 和 2-氰基苯并噻唑 (CBT) 功能化肽标记有醛藻酸钠修饰的磁性氧化铁纳米颗粒 (ASA-MNP) 基纳米载体。FA 可以与癌细胞膜上的叶酸受体结合以增强纳米团簇的吸收。CBT 修饰的肽可以与谷胱甘肽 (GSH) 反应，谷胱甘肽通常以较高水平存在于癌细胞中，形成细胞内聚集体并增加纳米药物的局部浓度。在体外研究表明，这些纳米药物显示出 NPC 细胞所需的吸收能力以及在激光照射下抑制癌细胞生长的能力。动物研究证实，这些纳米药物安全无毒，注射后可有效积聚在鼻咽癌肿瘤部位通过尾静脉，并在近红外激光照射下在荷瘤小鼠模型中显示出对肿瘤生长的卓越抑制。结果表明多功能纳米颗粒（NPs）具有潜在的应用价值，可作为治疗叶酸受体阳性鼻咽癌的新方法。