乳腺癌（BC）是全球女性最常见的恶性肿瘤，其高转移率是仅次于肺癌的第二大死亡原因。目前，他莫昔芬 (TAM) 是一种疏水性抗癌剂和选择性雌激素调节剂 (SERM)，已获得 FDA 批准，显示出针对 BC 的潜在抗癌活性，但非靶向给药具有严重的副作用，限制了其普遍应用。因此，将抗癌药物精确释放到肿瘤部位，可以提高疗效并减少对身体的副作用。纳米技术已成为解决过量 TAM 毒性问题的最重要策略之一，因为纳米制剂能够在较长时间内向癌细胞提供所需量的 TAM。鉴于此，在靶向药物递送中使用荧光碳纳米颗粒为提高 TAM 治疗的功效、安全性和特异性带来了新的希望。在这里，我们使用壳聚糖分子合成了生物相容性碳纳米颗粒（CNP），不含任何有毒表面钝化剂。合成的 CNP 具有良好的水分散性，并在激发时发出强烈的蓝色荧光（360 nm 光源）。 CNP 的表面已通过点击化学用叶酸功能化，以提高恶性细胞对靶向药物的吸收。成功利用癌细胞和正常细胞之间的 pH 差异来触发目标部位的 TAM 释放。孵育 6 小时后，CNP 在酸性 pH 条件下释放了约 74% 的 TAM 药物。体外研究还表明，用合成的 CNP 治疗后，可以显着抑制肿瘤生长。版权所有 © 2024 Elsevier B.V. 保留所有权利。

Breast cancer (BC) is the most common malignancy among females worldwide, and its high metastasis rates are the leading cause of death just after lung cancer. Currently, tamoxifen (TAM) is a hydrophobic anticancer agent and a selective estrogen modulator (SERM), approved by the FDA that has shown potential anticancer activity against BC, but the non-targeted delivery has serious side effects that limit its ubiquitous utility. Therefore, releasing anti-cancer drugs precisely to the tumor site can improve efficacy and reduce the side effects on the body. Nanotechnology has emerged as one of the most important strategies to solve the issue of overdose TAM toxicity, owing to the ability of nano-enabled formulations to deliver desirable quantity of TAM to cancer cells over a longer period of time. In view of this, use of fluorescent carbon nanoparticles in targeted drug delivery holds novel promise for improving the efficacy, safety, and specificity of TAM therapy. Here, we synthesized biocompatible carbon nanoparticles (CNPs) using chitosan molecules without any toxic surface passivating agent. Synthesized CNPs exhibit good water dispersibility and emit intense blue fluorescence upon excitation (360 nm source). The surface of the CNPs has been functionalized with folate using click chemistry to improve the targeted drug uptake by the malignant cell. The pH difference between cancer and normal cells was successfully exploited to trigger TAM release at the target site. After six hours of incubation, CNPs released ∼ 74 % of the TAM drug in acidic pH. In vitro, studies have also demonstrated that after treatment with the synthesized CNPs, significant inhibition of the tumor growth could be achieved.Copyright © 2024 Elsevier B.V. All rights reserved.