Yuan Donglan, Lu Zhiqiang, Xu Xindan, Liu Wei
Nuclear Medicine Department, the First Affiliated Hospital of Nanjing Medical University, Nanjing, 210029, China.
Department of Radiotherapy, School of Medicine, Zhongda Hospital, Southeast University, Nanjing, 210009, China.
Discov Oncol. 2024 Dec 18;15(1):794. doi: 10.1007/s12672-024-01682-x.
To construct polydopamine (PDA)-based nanoparticles (NPs) for combined chemotherapy (CT) and photothermal therapy (PTT) of thyroid tumors by conjugating doxorubicin (DOX) via Schiff base reaction and decorating with RGD peptide.
PDA NPs were synthesized using dopamine hydrochloride (DA) as the raw material and reacted with DOX-PEG-NH to obtain PDA-DOX NPs. Subsequently, RGD peptide was coupled with PDA-DOX NPs for modification. Their size, charge, and shape were characterized using DLS and SEM. The assembly of DOX was verified by ultraviolet-visible spectroscopy (UV-Vis), and the release efficiency of DOX under different pH conditions was calculated. The antitumor effect of RGD@PDA-DOX was validated in KTC-1 cells and tumor-bearing nude mice.
The prepared RGD@PDA-DOX exhibited excellent dispersion, stability, and biocompatibility. PDA-DOX possessed superior photothermal conversion efficiency, capable of rapidly elevating the solution temperature within 5 min. In vitro studies revealed that the inhibitory rate of RGD@PDA-DOX combined with 808 nm laser on KTC-1 cells reached 92% (p < 0.05). In vivo experiments demonstrated that RGD@PDA-DOX exhibits no cytotoxicity. The modification with RGD peptides enables RGD@PDA-DOX to target tumor regions and accumulate over an extended period. Additionally, RGD@PDA-DOX, when combined with an 808 nm laser, significantly inhibits tumor growth.
RGD@PDA-DOX can effectively accumulate in tumor regions and demonstrates excellent anti-tumor efficacy. It may serve as a feasible approach for the effective treatment of thyroid tumors, providing further evidence and data for clinical translation.
通过席夫碱反应共轭阿霉素（DOX）并用RGD肽修饰，构建用于甲状腺肿瘤联合化疗（CT）和光热治疗（PTT）的聚多巴胺（PDA）基纳米颗粒（NPs）。
以盐酸多巴胺（DA）为原料合成PDA NPs，并与DOX-PEG-NH反应得到PDA-DOX NPs。随后，将RGD肽与PDA-DOX NPs偶联进行修饰。使用动态光散射（DLS）和扫描电子显微镜（SEM）对其尺寸、电荷和形状进行表征。通过紫外可见光谱（UV-Vis）验证DOX的组装情况，并计算不同pH条件下DOX的释放效率。在KTC-1细胞和荷瘤裸鼠中验证RGD@PDA-DOX的抗肿瘤效果。
制备的RGD@PDA-DOX表现出优异的分散性、稳定性和生物相容性。PDA-DOX具有优异的光热转换效率，能够在5分钟内迅速提高溶液温度。体外研究表明，RGD@PDA-DOX联合808 nm激光对KTC-1细胞的抑制率达到92%（p < 0.05）。体内实验表明，RGD@PDA-DOX无细胞毒性。用RGD肽修饰使RGD@PDA-DOX能够靶向肿瘤区域并长时间积累。此外，RGD@PDA-DOX与808 nm激光联合使用时，能显著抑制肿瘤生长。
RGD@PDA-DOX能有效在肿瘤区域积累，并表现出优异的抗肿瘤疗效。它可能是有效治疗甲状腺肿瘤的一种可行方法，为临床转化提供了进一步的证据和数据。
