光动力疗法（PDT）被批准用于治疗某些癌症和癌前病变。虽然早期的光敏剂 (PS) 已进入临床，但过去二十年的研究已导致第三代 PS 的发展，包括用于改善肿瘤递送和最小化全身或光毒性的光动力纳米药物。在 PDT 纳米粒子设计方面，我们正在见证从被动递送到主动递送的转变，以减少 PS 剂量来改善结果。肿瘤微环境（TME）由复杂且动态的景观组成，具有配体表面修饰的光动力纳米载体的无数潜在靶标。在此，我们回顾了通过主动靶向纳米颗粒（NP）到细胞内细胞器（如线粒体或溶酶体等）来临时进行PDT的方法，克服了PDT引起的缺氧造成的局限性，破坏了肿瘤组织中的血管网络——血管靶向PDT。 VTP）和针对光免疫疗法的免疫细胞。我们认为，协同前景将有助于应对深部肿瘤、转移或复发等挑战，并为患者带来强劲的 PDT 反应。© 2024 Wiley periodicals LLC。

Photodynamic therapy (PDT) is approved for the treatment of certain cancers and precancer lesions. While early Photosensitizers (PS) have found their way to the clinic, research in the last two decades has led to the development of third-generation PS, including photodynamic nanomedicine for improved tumor delivery and minimal systemic or phototoxicity. In terms of nanoparticle design for PDT, we are witnessing a shift from passive to active delivery for improved outcomes with reduced PS dosage. Tumor microenvironment (TME) comprises of a complex and dynamic landscape with myriad potential targets for photodynamic nanocarriers that are surface-modified with ligands. Herein, we review ways to improvise PDT by actively targeting nanoparticles (NPs) to intracellular organelles such as mitochondria or lysosomes and so forth, overcoming the limitations caused by PDT-induced hypoxia, disrupting the blood vascular networks in tumor tissues-vascular targeted PDT (VTP) and targeting immune cells for photoimmunotherapy. We propose that a synergistic outlook will help to address challenges such as deep-seated tumors, metastasis, or relapse and would lead to robust PDT response in patients.© 2024 Wiley Periodicals LLC.