A hypoxia-responsive prodrug for specific drug release and synergistic chemo-photodynamic cancer therapy

IF 4.2 3区工程技术 Q2 CHEMISTRY, APPLIED

Dyes and Pigments Pub Date : 2026-06-01 Epub Date: 2026-01-22 DOI:10.1016/j.dyepig.2026.113602

Zhen-Kun Sun , Feng-Yan Yao , Wen-Qiang Wu , Yong-Jun Tao , Tian-Jiao Gao , Jian-Yong Liu , Lijing Zheng

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引用次数: 0

Abstract

Hypoxia within solid tumors significantly impairs the efficacy of photodynamic therapy (PDT), which relies on oxygen to generate cytotoxic reactive oxygen species (ROS). In this study, we turn this limitation into a therapeutic advantage by developing a hypoxia-activatable prodrug, BAP, which integrates a boron dipyrromethene (BODIPY)-based photosensitizer with paclitaxel (PTX) via a reductively cleavable azobenzene linker. Upon light irradiation, this photosensitizing prodrug mediates photodynamic action that consumes local oxygen, thereby aggravating tumor hypoxia. This heightened hypoxic state facilitates rapid cleavage of the azobenzene linker, resulting in the release of PTX specifically within tumors. As a consequence, tumor cells that survive PDT are effectively eliminated. Both in vitro and in vivo evaluations demonstrated the superior antitumor performance of BAP, which operates through a synergistic mechanism combining BODIPY-driven PDT and hypoxia-triggered chemotherapy. This study presents a novel strategy that not only addresses the challenge of hypoxia in PDT but also leverages it to achieve controlled combination therapy, offering a promising platform for synergistic cancer treatment.

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一种缺氧反应前药，用于特异性药物释放和协同化学-光动力癌症治疗

实体瘤内缺氧会显著损害光动力治疗（PDT）的疗效，光动力治疗依赖于氧气产生细胞毒性活性氧（ROS）。在这项研究中，我们通过开发一种可缺氧激活的前药BAP，将这一局限性转化为治疗优势，BAP通过还原可切割的偶氮苯连接剂将基于硼二吡啶（BODIPY）的光敏剂与紫杉醇（PTX）结合。在光照射下，这种光敏前药介导光动力作用，消耗局部氧气，从而加重肿瘤缺氧。这种高缺氧状态促进了偶氮苯连接体的快速裂解，导致PTX在肿瘤内特异性释放。因此，在PDT中存活的肿瘤细胞被有效地消灭。体外和体内评价均表明BAP具有较好的抗肿瘤性能，其作用机制是由bodipy驱动的PDT和缺氧触发的化疗相结合的协同机制。本研究提出了一种新的策略，不仅解决了PDT中缺氧的挑战，而且利用它来实现控制联合治疗，为协同癌症治疗提供了一个有希望的平台。

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来源期刊

Dyes and Pigments 工程技术-材料科学：纺织

CiteScore

8.20

自引率

13.30%

发文量

933

审稿时长

33 days

期刊介绍： Dyes and Pigments covers the scientific and technical aspects of the chemistry and physics of dyes, pigments and their intermediates. Emphasis is placed on the properties of the colouring matters themselves rather than on their applications or the system in which they may be applied. Thus the journal accepts research and review papers on the synthesis of dyes, pigments and intermediates, their physical or chemical properties, e.g. spectroscopic, surface, solution or solid state characteristics, the physical aspects of their preparation, e.g. precipitation, nucleation and growth, crystal formation, liquid crystalline characteristics, their photochemical, ecological or biological properties and the relationship between colour and chemical constitution. However, papers are considered which deal with the more fundamental aspects of colourant application and of the interactions of colourants with substrates or media. The journal will interest a wide variety of workers in a range of disciplines whose work involves dyes, pigments and their intermediates, and provides a platform for investigators with common interests but diverse fields of activity such as cosmetics, reprographics, dye and pigment synthesis, medical research, polymers, etc.