化疗与光动力疗法(PDT)的协同效应是提高肿瘤治疗效果的有效途径。然而，大多数协同治疗药物的水溶性和稳定性较差，因此难以在避免严重副作用的同时实现高疗效。本文成功合成了一种名为cRGDfk-CCPT-mCe6的独特的蒲公英样纳米药物，利用载Ce6的亲水性β-环糊精(β-CD)掺杂的脂质体作为核心(花托)，并以β-CD修饰的喜树碱(CPT)前药作为飘散的蒲公英种子。通过分子间β-CD与CPT之间的主/客体相互作用，将β-CD修饰的CPT前药依次引入到核心囊泡中，并进一步引入cRGDfk肽作为最外层(花柱)，以增强其进入癌细胞的内稳定性。CPT通过谷胱甘肽(GSH)可裂解的二硫键与β-CD相互作用，在富含谷胱甘肽的癌细胞中释放药物，就像蒲公英种子在风中散布一样。GSH的消耗进一步通过Ce6与光辐射的联合作用破坏了癌细胞的细胞内氧化还原稳态，从而实现了协同抗肿瘤效应，导致癌细胞死亡。因此，这种纳米药物提供了一种简便而多才多艺的抗肿瘤策略，以及持久的抗癌效果。版权所有©2023 Elsevier Inc.。保留所有权利。

The synergistic effect of chemotherapy and photo-dynamic therapy (PDT) is an effective way to improve the efficiency of tumor treatment. However, most synergistic therapeutic drugs have poor water solubility and stability, so it is difficult to achieve high therapeutic effects while avoiding the severe side effects. Herein, a unique dandelion-like nanomedicine (named as cRGDfk-CCPT-mCe6) was successfully synthesized using Ce6-loaded amphiphilic β-cyclodextrins (β-CD) doped lipid-based vesicles as the core (receptacle) and β-CD modified camptothecin (CPT) pro-drug as the flyable dandelion seeds. The β-CD modified CPT pro-drug was introduced into the core vesicles in succession via host-guest interaction between inter-molecular β-CD and CPT, and cRGDfk peptides were further introduced as the outermost layer (stigma) to enhance the internalization into cancer cells. CPT interacted with β-CD through glutathione (GSH)-cleavable disulfide bonds, which led to drug release in glutathione-rich cancer cells, just as spread of dandelion seeds in the wind. GSH consumption further disrupted the intracellular redox homeostasis of cancer cells through combined action of Ce6 with light irradiation and the synergistic anti-tumor effect was thus achieved, resulting in apoptosis of cancer cells. Therefore, the nanomedicine provides a facile and versatile anti-tumor strategy, as well as a persistent anti-cancer effects.Copyright © 2023 Elsevier Inc. All rights reserved.