To enhance the phototheranostic performance, agents with high reactive oxygen species (ROS) generation, good tumor-targeting ability, and prolonged retention are urgently needed. However, symmetric donor–acceptor (D–A) type agents usually produce spherical nanoaggregates, leading to good tumor targeting but inferior retention. Rod-like nanoaggregates are desired to extend their retention in tumors; however, this remains a challenge. In particular, agents with dynamically changeable shapes that integrate merits of different morphologies are seldomly reported. Therefore, self-assembled organic nanoaggregates with smart shape tunability are designed here using an asymmetric D–A type TIBT. The photoluminescence quantum yield in solids is up to 52.24% for TIBT. TIBT also exhibits high ROS generation in corresponding nanoaggregates (TIBT-NCs). Moreover, dynamic self-assembly in shape changing from nanospheres to nanorods occurrs in TIBT-NCs, contributing to the enhancement of ROS quantum yield from 0.55 to 0.72. In addition, dynamic self-assembly can be observed for both in vitro and in vivo, conferring TIBT-NCs with strong tumor targeting and prolonged retention. Finally, efficient photodynamic therapy to inhibit tumor growth is achieved in TIBT-NCs, with an inhibition rate of 90%. This work demonstrates that asymmetric D–A type agents can play significant roles in forming self-assembled organic nanoaggregates, thus showing great potential in long-acting cancer therapy.

中文翻译：

---

少即是多：不对称 D-A 型制剂实现长效光动力治疗的动态自组装纳米聚集体

为了增强光治疗性能，迫切需要具有高活性氧（ROS）产生、良好的肿瘤靶向能力和长时间保留的药物。然而，对称供体-受体（D-A）型药物通常产生球形纳米聚集体，导致良好的肿瘤靶向性但保留效果较差。棒状纳米聚集体需要延长其在肿瘤中的保留时间；然而，这仍然是一个挑战。特别是，具有动态可变形状、整合不同形态优点的药剂很少被报道。因此，本文使用不对称 D-A 型 TIBT 设计了具有智能形状可调性的自组装有机纳米聚集体。 TIBT在固体中的光致发光量子产率高达52.24%。 TIBT 在相应的纳米聚集体 (TIBT-NC) 中也表现出高活性氧生成。此外，TIBT-NC 中发生了从纳米球到纳米棒形状变化的动态自组装，有助于将 ROS 量子产率从 0.55 提高到 0.72。此外，在体外和体内都可以观察到动态自组装，从而赋予 TIBT-NC 强大的肿瘤靶向性和长期保留能力。最终，在TIBT-NCs中实现了有效的光动力疗法抑制肿瘤生长，抑制率高达90%。这项工作表明，不对称D-A型药物在形成自组装有机纳米聚集体方面可以发挥重要作用，从而在长效癌症治疗中显示出巨大潜力。