Wang Ying, Wang Yujie, Yang Yao, Leng Ling
Stem Cell and Regenerative Medicine Lab, Institute of Clinical Medicine, State Key Laboratory for Complex, Severe, and Rare Diseases, Peking Union Medical College Hospital, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100730, China.
Institute of Pharmaceutics, School of Pharmaceutical Sciences (Shenzhen), Sun Yat-sen University, Shenzhen, 518107, China.
Mater Today Bio. 2025 Aug 30;34:102262. doi: 10.1016/j.mtbio.2025.102262. eCollection 2025 Oct.
Melanoma is a severe eruptive disease caused by melanocyte lesions and characterized by aggressive tumors, which has become one of the fastest evolving cancers worldwide, and its incidence and mortality rates have shown larger increases than other types of cancers. Finding effective medicines has become an important topic in collaborative research. Many compounds have been removed from clinical application because of poor physicochemical properties, especially low solubility, a high clearance rate and toxic side effects. In this study, a reactive oxygen species (ROS)-responsive camptothecin (CPT) prodrug delivery system (CTS-S-CPT@IR 780 NPs) in which CPT was conjugated to chitosan was developed. The synthesized CTS-S-CPT conjugate self-assembled to form NPs loading IR 780 in solution. Sonodynamic therapy (SDT) at the tumor site can activate the sonosensitizer IR 780 to release large amounts of ROS and heat, inducing apoptosis. ROS can also cleave carbon‒sulfur bonds and release the chemotherapeutic drug CPT. ROS-responsive CTS-S-CPT@IR 780 NPs activated by combination chemotherapy/SDT were successfully prepared for tumor-targeted drug delivery and can effectively inhibit tumor growth in vivo and in vitro with lower toxic side effects, and localized, controllable, and on-demand release drug. This prodrug approach has spawned hope for overcoming such treatment dilemmas.
黑色素瘤是一种由黑素细胞病变引起的严重爆发性疾病,其特征为侵袭性肿瘤,已成为全球发展最快的癌症之一,其发病率和死亡率的增长幅度高于其他类型的癌症。寻找有效的药物已成为合作研究中的一个重要课题。许多化合物由于物理化学性质不佳,特别是低溶解度、高清除率和毒副作用,已被从临床应用中淘汰。在本研究中,开发了一种活性氧(ROS)响应型喜树碱(CPT)前药递送系统(CTS-S-CPT@IR 780 NPs),其中CPT与壳聚糖偶联。合成的CTS-S-CPT偶联物在溶液中自组装形成负载IR 780的纳米颗粒。肿瘤部位的声动力疗法(SDT)可激活声敏剂IR 780释放大量ROS和热量,诱导细胞凋亡。ROS还可裂解碳-硫键并释放化疗药物CPT。成功制备了通过联合化疗/SDT激活的ROS响应型CTS-S-CPT@IR 780 NPs用于肿瘤靶向给药,可有效抑制体内外肿瘤生长,且毒副作用较低,能实现药物的局部、可控和按需释放。这种前药方法为克服此类治疗难题带来了希望。