Near-infrared (NIR) light-activated phototherapy, such as photothermal therapy (PTT) and photodynamic therapy (PDT), has gained considerable attention due to the advantages of high efficiency and minimally invasiveness. However, the development of a single component therapeutic agent with clear structure and molecular weight that achieve photodynamic/photothermal synergistic therapy is still challenging. Herein, we design and synthesize a new smart photosensitizer (PRX) by conjugation of perylene diimide (PDI) and methylene violet (RAX). The typical donor-acceptor (D-A) structure of RAX facilitates the red-shift of absorption to the near-infrared (NIR) region. The amphiphilic PRX could self-assemble into monodispersed nanoparticles (PRX NPs) with enhanced and broadened absorption. Under a single 808 nm laser irradiation, PRX NPs could generate efficient reactive oxygen species (ROS) and heat simultaneously with the photothermal conversion efficiency as high as 59%. PRX NPs displays strong interaction with DNA and can damage plasmid DNA upon light irradiation. The biocompatibility and high phototoxicity of PRX NPs against A549 cells are further confirmed through MTT assay. Therefore, the as-prepared PRX NPs could be served as a promising antitumor nanoagent through photothermal/photodynamic combination manner.

近红外（NIR）光激活光疗，例如光热疗法（PTT）和光动力疗法（PDT），由于其高效和微创的优势而备受关注。然而，开发具有透明结构和分子量的单组分治疗剂以实现光动力/光热协同治疗仍然是具有挑战性的。本文中，我们通过design二酰亚胺（PDI）和亚甲基紫（RAX）的共轭设计和合成了一种新型的智能光敏剂（PRX）。RAX的典型供体-受体（DA）结构有助于吸收向近红外（NIR）区域的红移。两亲性PRX可以自组装成单分散的纳米粒子（PRX NPs），具有增强和扩大的吸收能力。在单次808 nm激光照射下，PRX NP可以同时产生有效的活性氧（ROS）和热量，光热转化效率高达59％。PRX NP与DNA表现出强烈的相互作用，并且在光照射下会损坏质粒DNA。通过MTT测定进一步证实了PRX NP对A549细胞的生物相容性和高光毒性。因此，所制备的PRX NPs可以通过光热/光动力结合的方式作为有希望的抗肿瘤纳米剂。