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Carrier‐free nanodrugs that integrate chemodrugs and other therapeutic agents demonstrate good efficacy and minimized side effects, showing promise for combined therapy. However, a key challenge lies in enhancing the bioavailability and therapeutic potential of the nanodrugs through a controllable assembly process. Herein, a carrier‐free photothermal nanodrug (ZPQ NPs) is constructed through flavonol‐driven assembly with amine‐substituted perylene diimide for enhanced chemo‐photothermal combined cancer therapy. The flavonol, particularly quercetin, facilitates J‐aggregation of perylene diimide derivatives within the nanodrug and contributes to multiple improvements, including red‐shifted absorption, enhanced fluorescence intensity, improved photothermal conversion efficiency as well as excellent photostability. Moreover, the nanodrug also demonstrates enhanced cellular uptake and intracellular reactive oxygen species scavenging capability. The combination of quercetin and photothermal effect effectively kills cancer cells, as well as alleviates inflammation following photothermal therapy. Guided by in vivo fluorescence imaging, the application of ZPQ NPs results in complete tumor elimination and effectively inhibits tumor recurrence through chemo‐photothermal combined therapy. This work presents a straightforward strategy for constructing carrier‐free nanodrugs that exhibit simultaneous enhancements in both photophysical properties and biological activity. [ABSTRACT FROM AUTHOR]

Reactive oxygen species (ROS) have become an effective tool for tumor treatment. The combination of photodynamic therapy (PDT) and chemodynamic therapy (CDT) takes advantage of various ROS and enhances therapeutic effects. However, the activation of CDT usually occurs before PDT, which hinders the sustained maintenance of hydroxyl radicals (⋅OH) and reduces the treatment efficiency. Herein, we present a light‐triggered nano‐system based on molecular aggregation regulation for converting cancer therapy from PDT/photothermal therapy (PTT) to a long‐lasting CDT. The ordered J‐aggregation enhances the photodynamic properties of the cyanine moiety while simultaneously suppressing the chemodynamic capabilities of the copper‐porphyrin moiety. Upon light irradiation, Cu‐PCy JNPs demonstrate strong photodynamic and photothermal effects. Meanwhile, light triggers a rapid degradation of the cyanine backbone, leading to the destruction of the J‐aggregation. As a result, a long‐lasting CDT is sequentially activated, and the sustained generation of ⋅OH is observed for up to 48 hours, causing potent cellular oxidative stress and apoptosis. Due to their excellent tumor accumulation, Cu‐PCy JNPs exhibit effective in vivo tumor ablation through the converting therapy. This work provides a new approach for effectively prolonging the chemodynamic activity in ROS‐based cancer therapy. [ABSTRACT FROM AUTHOR]

Organic dyes hold great promise for application in photodynamic therapy (PDT). However, they currently face challenges such as inadequate photodynamic activity, limited tumor penetration, and constraints imposed by tumor hypoxia. Here, a facile and efficient strategy is presented for multi‐enhanced PDT through the fluorination of a squarylium indocyanine dye‐based photosensitizer (FCy). The amphiphilic FCy features perfluorooctane and PEG‐biotin moieties conjugated to a squarylium indocyanine core. In aqueous environments, FCy spontaneously self‐assembles into stable nano‐sized photosensitizers (FCy NPs), demonstrating a high oxygen loading ability attributable to the presence of perfluoroalkyl groups. Consequently, the aggregation of squarylium indocyanine dyes remarkably boosts the photodynamic effect, yielding a 15‐fold improvement in singlet oxygen quantum yield. Owing to the perfluoroalkyl group, FCy NPs exhibit increased endoplasmic reticulum (ER)‐ accumulating abilities, which further induce ER stress upon laser irradiation and enhance the PDT effect. Furthermore, the superior deep tumor penetration ability of FCy NPs is confirmed through both in vitro and in vivo studies. With efficient oxygen supply to the deep tumor regions, FCy NPs demonstrate potent imaging‐guided PDT against hypoxia tumors. The study substantiates the enhanced ER‐accumulating ability of the perfluoroalkyl group and presents a facile fluorination strategy for the multi‐enhancement of photosensitizers. [ABSTRACT FROM AUTHOR]

Photodynamic therapy (PDT) exhibits great potential for cancer therapy, but still suffers from nonspecific photosensitivity and poor penetration of photosensitizer. Herein, a smart perylene monoimide‐based nanocluster capable of enzyme‐triggered disassembly is reported as an activatable and deeply penetrable photosensitizer. A novel carboxylesterase (CE)‐responsive tetrachloroperylene monoimide (P1) was synthesized and assembled with folate‐decorated albumins into a nanocluster (FHP) with a diameter of circa 100 nm. Once P1 is hydrolyzed by the tumor‐specific CE, FHP disassembles into ultrasmall nanoparticles (ca. 10 nm), facilitating the deep tumor penetration of FHP. Furthermore, such enzyme‐triggered disassembly of FHP leads to enhanced fluorescence intensity (ca. 8‐fold) and elevated singlet oxygen generation ability (ca. 4‐fold), enabling in situ near‐infrared fluorescence imaging and promoted PDT. FHP permits remarkable tumor inhibition in vivo with minimal side effects through imaging‐guided, activatable, and deep PDT. This work confirms that this cascaded multifunctional control through enzyme‐triggered molecular disassembly is an effective strategy for precise cancer theranostics. [ABSTRACT FROM AUTHOR]

Abstract: Fluorescent dyes with multi‐functionality are of great interest for photo‐based cancer theranostics. However, their low singlet oxygen quantum yield impedes their potential applications for photodynamic therapy (PDT). Now, a molecular self‐assembly strategy is presented for a nanodrug with a remarkably enhanced photodynamic effect based on a dye‐chemodrug conjugate. The self‐assembled nanodrug possesses an increased intersystem crossing rate owing to the aggregation of dye, leading to a distinct singlet oxygen quantum yield (Φ(1O2)). Subsequently, upon red light irradiation, the generated singlet oxygen reduces the size of the nanodrug from 90 to 10 nm, which facilitates deep tumor penetration of the nanodrug and release of chemodrug. The nanodrug achieved in situ tumor imaging and potent tumor inhibition by deep chemo‐PDT. Our work verifies a facile and effective self‐assembly strategy to construct nanodrugs with enhanced performance for cancer theranostics. [ABSTRACT FROM AUTHOR]

Bacterial infections cause severe threats to human health. Silver nanoparticles (AgNPs) are promising antibacterial materials, but still confront poor colloidal stability and uncontrollable silver ion (Ag+) release. Here, a dye template strategy based on tunable perylenediimide (PDI) self-assembly is presented for constructing novel silver nanohybrids with visible-light photocatalysis enhanced antibacterial effect. Ultrasmall AgNPs are grown on diversiform topological PDI self-assembly-templates via in situ reduction to yield silver nanohybrids, achieving stable AgNPs dispersion. The developed fiber-like nanohybrids (BF@AgNPs) are endowed with photocatalytic ability by PDI nanofiber templates. Upon visible-light irradiation, BF@AgNPs generate reactive oxygen species via photocatalytic reaction, facilitating the AgNPs degradation to release Ag+ and concurrently exerting photocatalytic damage to bacteria. Consequently, the visible-light photocatalysis enhanced antibacterial effect of BF@AgNPs against Staphylococcus aureus and Escherichia coli is achieved via synergetic Ag+ release and photocatalytic performance. This work not only provides a versatile molecular assembly strategy for developing new powerful antibacterial materials, but also opens up a new way for dye functionalization. [Display omitted] • Tunable perylenediimide self-assemblies are used as templates to construct silver nanohybrids in situ. • BF@AgNPs can generate ROS via photocatalysis, facilitating Ag+ release upon visible-light irradiation. • BF@AgNPs exhibit enhanced antibacterial effect via synergetic Ag+ release and photocatalysis upon visible-light irradiation. [ABSTRACT FROM AUTHOR]