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IR780
CHEMICAL ENGINEERING JOURNAL · 2019 · IF 8.355

Low side-effect and heat-shock protein-inhibited chemo-phototherapy nanoplatform via co-assembling strategy of biotin-tailored IR780 and quercetin

Hailong Tian,Jing Zhang,Huiyuan Zhang,Yue Jiang,Aixin Song,Yuxia Luan

The side effects of anticancer drugs and tumor tolerance from heat shock protein expression are still a bottleneck for the current chemo-phototherapy. Although quercetin (Qu) is a naturally low-side effect anticancer drug and heat shock protein inhibitor for tailoring phototherapy, it is largely restricted by poor water solubility. Moreover, the near-infrared dye IR780-iodide (IR780), as a promising phototherapy agent, is also restricted from clinical applications due to its poor water solubility. Herein, we rationally designed a robust low side-effect and heat-shock protein-inhibited chemo-phototherapy nanoplatform via co-assembly of biotin-tailored IR780 (B780) and quercetin, defined as B780/Qu nanoparticles (B780/Qu NPs), which efficiently solved the poor water solubility of both IR780 and Qu. Moreover, the B780 endowed B780/Qu NPs with superior active tumor-targeted property and pH-responsive drug delivery. Thanks to the combination of chemo-phototherapy, the B780/Qu NPs with near infrared (NIR) laser irradiation exhibited excellent anti-tumor efficacy. Therefore, our B780/Qu NPs are very promising as an efficient low side-effect and heat-shock protein-inhibited chemo-phototherapy nanoplatform against tumors.

研究领域: 肿瘤学 · 药剂学 · 生物医学工程
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Nanoscale Advances · 2025 · IF 4.6

BSA@IR780-Loaded Mesoporous Polydopamine Nanoparticles with Enhanced Photostability for Multimodal Imaging and Photothermal Therapy of Tumors

Shuaibo Yang,Yanzhao Diao,Lifeng Hang,Hong Qu,Laiping Fang,Wei Guo,Hua Wen,KuokWai IU,Guihua Jiang,Lianyi Shao,Quan Li

Multifunctional phototherapy that integrates diagnostic and therapeutic modalities holds the potential to revolutionize cancer treatment. The near-infrared cyanine dye IR780 is known for its high spatial resolution imaging capabilities. When conjugated with bovine serum albumin (BSA), it effectively mitigates common challenges such as photobleaching and fluorescence quenching, making it widely used in tumor imaging. However, its limited photothermal conversion efficiency hinders its broader application in tumor therapy. To overcome these limitations, this study presents the design and development of an imaging-guided multifunctional nanoplatform: mesoporous polydopamine (MPDA)-BSA@IR780. Our findings demonstrate that MPDA, as a carrier, significantly improves the photostability of BSA@IR780. Furthermore, MPDA's superior photothermal properties enhance the photothermal efficacy of the platform, enabling MPDA-BSA@IR780 to function as a dual photothermal therapy (PTT) agent. In addition to its therapeutic potential, MPDA-BSA@IR780 serves as both a photoacoustic (PA) and fluorescence (FL) imaging probe, effectively guiding treatment decisions. Cellular assays reveal that MPDA-BSA@IR780 exhibits a robust photothermal effect, supporting promising therapeutic outcomes. In vivo studies further demonstrate that, following laser irradiation, MPDA-BSA@IR780 achieves near-complete tumor ablation without inducing significant toxicity, while also exhibiting excellent biocompatibility. In conclusion, this study introduces a safe and effective photothermal nanoparticle platform for tumor imaging, diagnosis, and treatment, providing a promising strategy for future biomedical applications.

CAS / MDL: 62-31-7
研究领域: 癌症研究 · 纳米技术 · 诊疗学 · 生物医学工程
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Journal of Materials Chemistry B · 2021 ·Vol. 9 ·期 48 ·9932-9945 · IF 6.331

Design and construction of IR780- and EGCG-based and mitochondrial targeting nanoparticles and their application in tumor chemo-phototherapy

Jiahe Bao,Yinan Zhao,Jing Xu,Yuanqiang Guo

An integration combination of phototherapy and chemotherapy to treat carcinoma, solving the inner limitation of individual-modal chemical agent-based therapy or phototherapy, emerges to be a strategy with high prospects for achieving synergistic curative effects. The dye IR780-iodide (IR780) close to infrared radiation is a phototherapy agent with high prospects. However, it is limited in its clinical applications due to poor solubility in water. While epigallocatechin-3-gallate (EGCG), naturally resourced green tea polyphenol, has been extensively proven with intrinsic antitumor activity, but it is largely restricted by its low bioavailability in vivo. Hence, novel multiple-function nanoparticles comprising hyaluronic acid (HA) and IR780 were proposed to deliver EGCG, defined as EGCG@THSI nano-scale particles (EGCG@THSI NPs), thereby rapidly solving limitations of EGCG and IR780. Amphiphilic nano-scale carrier was prepared by triphenylphosphine (TPP), hyaluronic acid (HA), cystamine, and IR780, termed as TPP–HA–SS–IR780, and EGCG was loaded into the amphiphilic copolymer by self-assembly. TPP–HA–SS–IR780 endowed the as-synthesized EGCG@THSI NPs with excellent TPP-mediated mitochondrial-targeted and glutathione-triggered rapid drug release properties. As impacted by the integration of phototherapy and chemotherapy, the EGCG@THSI NPs under NIR laser irradiation showed a prominent anti-tumor effect. Taken together, this study presented a multiple-function nano-scale carrier platform with high prospects in improving the therapeutic efficacy of anti-carcinoma drugs.

CAS / MDL: 1122-58-3 6066-82-6
研究领域: 药学 · 纳米技术 · 肿瘤学 · 生物医学工程
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ADVANCED FUNCTIONAL MATERIALS · 2021 ·Vol. 31 ·期 24 ·2100954 · IF 18.808

IR780-Loaded Hyaluronic Acid@Gossypol–Fe(III)–EGCG Infinite Coordination Polymer Nanoparticles for Highly Efficient Tumor Photothermal/Coordinated Dual Drugs Synergistic Therapy

Siyuan Luo,Ya Wang,Shihong Shen,Peng Tang,Zeying Liu,Shuai Zhang,Daocheng Wu

A novel strategy called “two-stage dual-synergistic tumor therapy (TDTT),” which combines photothermal therapy with infinite coordination polymers (ICPs) chemotherapy at the first stage in the short term and two drugs of ICPs synergistic chemotherapy (coordinated dual drugs chemotherapy) at the second stage in the long term, is proposed. This strategy is achieved by preparing IR780-loaded hyaluronic acid (HA) encapsulated gossypol–Fe(III)–epigallocatechin gallate (EGCG) ICP nanoparticles (HA@IRGFE ICP NPs), which have IR780 inclusions, a natural gossypol, and EGCG coordinated with Fe 3+ framework, and a HA shell. It is found that the HA@IRGFE ICP NPs’ diameter is 120.0 ± 39.5 nm and has tumor-targeting ability and can be rapidly released in tumor environment. Their photothermal conversion efficiency is greatly improved to 47.8%, and the total combination index of TDTT is 0.38, which indicates an excellent synergistic therapy result. These HA@IRGFE ICP NPs show low toxicity with a high tolerated dose (30.0 mg kg −1 ), a high tumor inhibition rate of 98.7%, and a very low tumor recurrence rate over 60 days (12.5%) with TDTT strategy, indicating their great potential applications in the field of tumor therapy.

CAS / MDL: 989-51-5
研究领域: 生物医学工程 · 纳米医学 · 肿瘤学
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Journal of Materials Chemistry B · 2023 · IF 7

Protein-coated cobalt oxide-hydroxide nanospheres deliver photosensitizer IR780 iodide for near-infrared light-triggered photodynamic/photothermal/chemodynamic therapy against colon cancer

Han Hu,Shijie Yao,Qi Xu,Xing Cai,Zhimin Mo,Zhe Yang,Wen-Qiu Chen,Qianyuan He,Xiaofang Dai,Zushun Xu

Phototherapy has garnered worldwide attention for its minimal invasiveness, controllability, and spatial selectivity in treating cancer. One promising approach involves the use of near-infrared dye IR780, which demonstrates both photodynamic therapy (PDT) and photothermal therapy (PTT) effects under 808 nm laser irradiation. However, this hydrophobic dye's toxicity and limited tumor targeting severely hamper its suitability for cancer applications. Herein, a biocompatible nanoplatform CoOOH-IR780@BSA (CoIRB) has been developed to efficiently deliver IR780 and provide multi-mode treatments for colon tumors. Due to the nanocarrier coating, CoIRB nanoparticles demonstrated reliable dispersion and stability, and their biotoxicity was substantially reduced for safer blood circulation, which overcame the biological barrier of IR780. The nanoplatform has also shown considerable results in phototherapy in vivo and in vitro experiments, with successful inhibition of MC38 tumor growth through intravenous administration. Additionally, the introduction of cobalt ions could induce Fenton-like reactions to activate the production of toxic hydroxyl radicals (·OH), exerting an assistive chemodynamic therapy (CDT) effect. Notably, these nanodrugs also exhibited potential as scavengers of reductive glutathione (GSH) and hydrogen sulfide (H2S) leading to amplifying oxidative damage of reactive oxygen species (ROS). Overall, the versatile therapeutic platform, CoIRB, has opened up considerable prospects as a biotherapeutic option for combining PDT/PTT/CDT against colon cancer.

研究领域: 纳米技术 · 癌症治疗 · 光疗 · 生物医学工程
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ACS Applied Bio Materials · 2019 · IF 0

Combating Multidrug Resistance through an NIR-Triggered Cyanine-Containing Amphiphilic Block Copolymer

Jia Tian,Chao Xiao,Baoxuan Huang,Xiaoze Jiang,Hongliang Cao,Feng Liu,Weian Zhang

Nowadays, multidrug resistance is the main challenge during cancer chemotherapy. Photochemical internalization (PCI) has been demonstrated to be a unique and promising approach to overcome multidrug resistance with light-harnessed activation. Here, an amphiphilic pH-responsive block copolymer with IR780 at the junction point [PEG-IR780-PDEAEMA; PEG, poly(ethylene glycol); PDEAEMA, poly((diethylamino)ethyl methacrylate)] has been designed as a perfect drug release platform as well as a functional macromolecular photosensitizer of PCI. PEG-IR780-PDEAEMA was synthesized by the combination of RAFT polymerization and click chemistry and further self-assembled into spherical micelles in aqueous solution. Notably, IR780 moieties were dispersed regularly around the core of the spherical micelles, which led to the diminishment of the aggregation-caused quenching effect of photosensitizers and high singlet oxygen quantum yield. Confocal laser scanning microscopy results showed that a high amount of doxorubicin (DOX) was translocated into the nucleus with NIR light irradiation through the PCI effect. Moreover, DOX-loaded PEG-IR780-PDEAEMA micelles showed much higher phototoxicity under short-time NIR light irradiation than their dark toxicity. Therefore, this DOX-loaded drug release platform based on pH-sensitive IR780-containing block copolymers has the potential to offer an efficient strategy for addressing drug resistance.

研究领域: 癌症研究 · 聚合物化学 · 药物科学 · 生物医学工程
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Biomaterials Science · 2018 ·Vol. 6 ·期 9 ·2460-2471 · IF 5.831

Construction of perfluorohexane/IR780@liposome coating on Ti for rapid bacteria killing under permeable near infrared light

Xiuhua Wang,Lei Tan,Xiangmei Liu,Zhenduo Cui,Xianjin Yang,Kelvin W. K. Yeung,Paul K. Chu,Shuilin Wu

Near infrared (NIR) light induced photodynamic antibacterial therapy (PDAT) is a promising antibacterial technique in rapid in situ disinfection of bacterially infected artificial implants due to its penetration ability into tissues. However, the lower oxygen content in vivo may restrict the yields of reactive oxygen species (ROS), thus reducing the antibacterial efficacy of PADT significantly. Herein, liposome encapsulated photosensitizers (PS), IR780 and perfluorohexane (PFH), have been constructed on the surface of Ti implants via a covalent linkage to overcome this issue. Thanks to the high oxygen capacity of PFH, more ROS can be generated during NIR irradiation regardless of the low content of oxygen in vivo. As a result, in vitro tests demonstrated that 15 minutes of 808 nm near-infrared irradiation could achieve a high antibacterial efficacy of 99.62% and 99.63% on the implant surface against Escherichia coli and Staphylococcus aureus, respectively. By contrast, the PDAT system without PFH modification shows a lower antibacterial efficacy (only 66.54% and 48.04%, respectively). In addition, this enhanced PDAT system also possesses great biocompatibility based on the in vitro and in vivo subcutaneous assays. This surface system makes it possible for rapid bacteria-killing in artificial implants that have been implanted in vivo under local conditions with lower oxygen content.

研究领域: 生物医学工程 · 材料科学 · 微生物学
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Arabian Journal of Chemistry · 2023 · IF 6

Biotin-modified hyaluronic acid double-target nanoparticles for quercetin and IR780 delivery: Fabrication, characterization, and biological properties

Linan Zhou,Ying Li,Zhen Lin,Xiaotang Gong,Jing Xu,Yuanqiang Guo

Currently, the use of nanotechnology to repurpose traditional drugs has emerged as a promising strategy for cancer treatment. Quercetin (Qu), a chemotherapy molecule, has excellent antitumor activity, and IR780, a photosensitizer, possesses sound tumor phototherapy effects. However, both compounds have poor water solubility and other drawbacks that hinder their extensive clinical applications. To effectively utilize two molecules in the fight against cancer, a new multifunctional chemical-phototherapy nanoplatform with tumor target and glutathione (GSH) response was designed. By modifying HA, the amphiphilic molecule carrying biotin and IR780 was obtained, which self-assembled to load the antitumor active molecule Qu, namely Qu@BHSI. In addition to addressing the hydrophobic issue of Qu and IR780, the prepared nanoparticles can rapidly release Qu with high concentrations of GSH present and generate heat and cytotoxic reactive oxygen species (ROS) under near-infrared light. The biological function research showed that Qu@BHSI nanoparticles had the ability to suppress the growth of A549 cells, induce cell apoptosis, stimulate ROS production in zebrafish, and inhibit angiogenesis in transgenic zebrafish. The construction of nanosystems provides new or alternative strategies and approaches for effectively repurposing classical drug molecules including photosensitizers and chemotherapy drugs.

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MOLECULAR PHARMACEUTICS · 2025 · IF 4.5

Metal-Polyphenol Self-Assembled Nanophotothermal Agent for Precise Mitochondrial Targeted Photothermal Therapy

Jun Zhou,Wensong Wang,Yong Li,Qianqian Liu,Fan Liu,Qiao Zhang,Yunfei Zhang,Can Jiang,Si Chen,Fei-Peng Du,Jinxuan Fan

Nanocarriers have been extensively utilized to improve the stability of photothermal agents in vivo, enhance delivery efficiency, and reduce drug side effects. However, challenges, such as the low safety of carrier materials, insufficient loading of therapeutic agents, and complex preparation procedures, still persist. In this study, the photothermal agent IR780 was encapsulated in network TA-Fe3+ (TF) which was self-assembled by tannic acid (TA) and Fe3+ to synthesize an acid-responsive multifunctional nanophotothermal agent TF@IR780 (TR). In the slightly acidic tumor microenvironment (TME), network shell TF is degraded, and the internal photothermal agent IR780 is exposed. On the one hand, the TF network can improve the solubility and stability of photothermal agent IR780 in vivo and significantly increase the uptake efficiency in tumor cells. On the other hand, Fe3+ exhibits magnetic resonance imaging (MRI) functionality, which combined with the fluorescence imaging of IR780 endows TR with multimodal imaging capabilities. In addition, TR is easy to release photosensitizers through acid response in the low pH environment of TME, and achieves precise damage to mitochondria through mitochondrial anchoring and light regulation. This overcomes the drawbacks of traditional tumor treatment methods, such as poor specificity, and demonstrates efficient and controllable antitumor activity.

CAS / MDL: 10025-77-1 1401-55-4
研究领域: 纳米医学 · 肿瘤学 · 生物材料学
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International Journal of Nanomedicine · 2025 · IF 6.5

Reduction-Responsive Nanoparticles Self-Assembled from Sericin-ss-Doxorubicin Conjugate for Hydrophobic IR780 Delivery with Integration of Antitumor Chemo-Phototherapy

Lulu Zhang,Haiyang Liu,Jin Ren,Junyi Shao,Yanrong Cao,Shuangshuang Wang,Changchun Peng,Shengwen Shao,Haixia Ge,Jingmou Yu

Background Stimuli-responsive polymer-drug nanoparticles have emerged as a versatile and effective platform for delivering drugs in the treatment of malignant tumors. The integration of chemo-phototherapy has gained increasing prominence due to its remarkable synergistic antitumor effects.Methods Hydrophilic sericin (Ser) was linked to antitumor drug doxorubicin (DOX) via a disulfide bond. The obtained Ser-ss-DOX conjugate was characterized by Fourier-transform infrared spectroscopy (FTIR), proton nuclear magnetic resonance (1H NMR) and dynamic light scattering (DLS). The near-infrared (NIR) fluorescent dye IR780 was encapsulated into Ser-ss-DOX by a dialysis method. The physical state of IR780 within Ser-ss-DOX/IR780 nanoparticles was analyzed by differential scanning calorimetry (DSC). The photothermal properties and drug release behavior of IR780-loaded nanoparticles were systematically investigated. Cellular uptake and reactive oxygen species (ROS) generation capacity and in vitro cytotoxicity of IR780-containing nanoparticles were studied in 4T1 breast cancer cells. In addition, 3D multicellular tumor spheroid model was conducted to investigate the antitumor activity of the nanoparticles.Results The Ser-ss-DOX conjugate was successfully synthesized. Ser-ss-DOX and Ser-ss-DOX/IR780 nanoparticles were spherical in shape, and their particle sizes measured by DLS were 326 and 190 nm, respectively. IR780 was in an amorphous state within the Ser-ss-DOX/IR780 nanoparticles. The loading contents of DOX and IR780 were 8.26% and 2.78%, respectively. Ser-ss-DOX/IR780 exhibited ideal photothermal properties in vitro and reduction-sensitive drug release in a high glutathione (GSH) environment. Ser-ss-DOX/IR780 displayed higher cellular uptake in 4T1 cells than Ser-ss-DOX and free DOX. Under 808 nm laser irradiation, Ser-ss-DOX/IR780 showed a strong capacity to generate ROS. Importantly, Ser-ss-DOX/IR780 with laser irradiation effectively inhibited the growth of 4T1 cells and 3D multicellular tumor spheroids.Conclusion This work demonstrated that Ser-ss-DOX/IR780 integrated dual functionalities of chemotherapy and phototherapy, thereby enabling substantial potential for application in tumor treatment.

研究领域: 纳米医学 · 癌症治疗 · 药物递送系统 · 生物材料 · 光热治疗 · 刺激响应材料
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ACS Applied Materials & Interfaces · 2019 · IF 8.456

An Oxygen Self-sufficient Fluorinated Nanoplatform for Relieved Tumor Hypoxia and Enhanced Photodynamic Therapy of Cancers

Shengnan Ma,Jie Zhou,Yuxin Zhang,Bo Yang,Yiyan He,Chen Tian,Xianghui Xu,Zhongwei Gu

The efficacy of photodynamic therapy (PDT) in the solid tumor is hampered by many challenges, including its oxygen self-consuming nature, insufficient oxygen levels within the hypoxic tumor microenvironment, and limited penetration of photosensitizers within tumors. Herein, we develop the IR780@O2-SFNs/iRGD as an oxygen self-sufficient and tumor-penetrating nanoplatform, which consists of IR780-loaded pH-sensitive fluorocarbon-functionalized nanoparticles (SFNs) and iRGD as a tumor targeting peptide that can penetrate deeper within the tumor. Because of the high oxygen affinity and outstanding permeability of the obtained nanoplatform, oxygen and IR780 which are encapsulated in the same core can play their roles to the utmost, resulting in remarkably accelerated singlet oxygen production, as demonstrated in vitro by the 3D multicellular spheroids and in vivo by tumor tissues. More interestingly, a single-dose intravenous administration of IR780@O2-SFNs/iRGD into mice bearing orthotopic breast cancer could selectively accumulate at the tumor site, highly alleviate the tumor hypoxia, significantly inhibit the primary tumor growth, and reduce the lung and liver metastasis, enabling the improved photodynamic therapeutic performance. Thus, this work paves an effective way to improve PDT efficacy through increasing tumor oxygenation and selective delivery of photosensitizers to the deep and hypoxic tumor.

CAS / MDL: 106-31-0
研究领域: 肿瘤学 · 纳米医学 · 治疗学 · 生物医学工程
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COLLOIDS AND SURFACES B-BIOINTERFACES · 2020 · IF 4.389

Rational design of an oxygen-enriching nanoemulsion for enhanced near-infrared laser activatable photodynamic therapy against hypoxic tumors

Liang Hong,Jia-Lin Wang,Jun-Xian Geng,Yi-Hua Zhao,Gao-Xin Zhou,Jia Zhang,Li-Wei Liu,Jun-Le Qu

Photodynamic therapy (PDT) has emerged as one of the most promising modalities to treat cancers. However, the hypoxic microenvironment in tumors severely limits the efficiency of PDT. IR780 is a near-infrared light activatable photosensitizer for PDT. It has attracted intensive attention owing to its intriguing properties such as mitochondria-targeting ability and fluorescence imaging capability. Nevertheless, its application in tumor treatment is hampered by its low aqueous solubility and poor stability. To address these obstacles, here we designed a novel hierarchical nanoplatform containing a uniquely stable high loading capacity oxygen carrier (perfluoropolyether, in short, PFPE) and IR780. This nanoplatform (IR780-P/W NE, in abbreviation for IR780-PFPE-in-water nanoemulsion) has no detectable dark cytotoxicity. It not only improves the aqueous solubility and stability of IR780, but also transports oxygen to relieve hypoxia and boosts the efficiency of near-infrared light triggered PDT via augmentation of reactive oxygen species generation. Particularly, the innovative nanosized oxygen carrier developed in this research, P/W NE, is a potential universal platform for loading hydrophobic photosensitizers (including but not limited to IR780), sonosensitizers, or radiosensitizers, and simultaneously improving the therapeutic efficacy. Our results highlight the intriguing potential of the developed nanoemulsions for mitigating tumor hypoxia and enhancing the efficiencies of oxygen-dependent therapies including PDT, sonodynamic therapy, radiotherapy, and so on.

研究领域: 癌症治疗 · 纳米医学 · 药剂学
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