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IR820
Biomaterials Science · 2018 ·Vol. 6 ·期 11 ·2925-2931 · IF 5.831

IR820 covalently linked with self-assembled polypeptide for photothermal therapy applications in cancer

Kaizong Huang,Mengyue Gao,Lin Fan,Yueyang Lai,Hongwei Fan,Zichun Hua

Owing to the unique advantages of high specificity and minimal invasiveness, photothermal therapy (PTT) has been evidenced with great potential in cancer treatment. However, most photothermal agents present a shortage of photobleaching and nonspecific biodistribution in clinical application. In this study, we conjugated a new Indocyanine Green Dye (IR820) with self-assembled polypeptide (ELP) via chemical bonding in an aqueous environment. This preparation method could effectively avoid damaging the polypeptide. ELP-IR820 was fabricated as nanoconjugates with diameters of approximately 50 nm. The use of ELP-IR820 notably enhanced photothermal-mediated cytotoxicity on CT-26 cancer cells. We demonstrate that the ELP-IR820 nanoparticles significantly improved drug accumulation in the tumor and photothermal effect in vivo compared to the free dye and monomer ELP-IR820. ELP-IR820 nanoparticle also exhibited outstanding ability to cause prominent tumor tissue growth inhibition via the photothermal effect. No noticeable toxicity was detected for all treatment groups. These investigations broaden the application of NIR dyes as a multimodal photothermal therapy platform.

研究领域: 癌症治疗 · 材料科学 · 纳米技术 · 生物医学工程
✓ 已验证 DOI PubMed 高影响因子
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JOURNAL OF NANOBIOTECHNOLOGY · 2020 ·Vol. 18 ·期 1 ·1-15 · IF 6.518

The microneedles carrying cisplatin and IR820 to perform synergistic chemo-photodynamic therapy against breast cancer

Fu Ji-jun,Li Chu-wen,Liu Yang,Chen Ming-yue,Zhang Qiang,Yu Xi-yong,Wu Bo,Li Jie-xia,Du Ling-ran,Dang Yuan-ye,Wu Dan,Wei Min-yan,Lin Zhi-qiang,Lei Xue-ping

Backgrounds Surgical resection and adjunct chemotherapy or radio-therapy has been applied for the therapy of superficial malignant tumor in clinics. Whereas, there are still some problems limit its clinical use, such as severe pains and side effect. Thus, it is urgent need to develop effective, minimally invasive and low toxicity therapy stagey for superficial malignant tumor. Topical drug administration such as microneedle patches shows the advantages of reduced systemic toxicity and nimble application and, as a result, a great potential to treat superficial tumors. Methods In this study, microneedle (MN) patches were fabricated to deliver photosensitizer IR820 and chemotherapy agent cisplatin (CDDP) for synergistic chemo-photodynamic therapy against breast cancer. Results The MN could be completely inserted into the skin and the compounds carrying tips could be embedded within the target issue for locoregional cancer treatment. The photodynamic therapeutic effects can be precisely controlled and switched on and off on demand simply by adjusting laser. The used base material vinylpyrrolidone—vinyl acetate copolymer (PVPVA) is soluble in both ethanol and water, facilitating the load of both water-soluble and water-insoluble drugs. Conclusions Thus, the developed MN patch offers an effective, user-friendly, controllable and low-toxicity option for patients requiring long-term and repeated cancer treatments.

研究领域: 肿瘤学 · 药学 · 生物医学工程
✓ 已验证 产品关联 DOI PubMed 高影响因子
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ACS Applied Materials & Interfaces · 2018 · IF 8.097

pH- and Enzyme-Sensitive IR820–Paclitaxel Conjugate Self-Assembled Nanovehicles for Near-Infrared Fluorescence Imaging-Guided Chemo–Photothermal Therapy

Di Zhang,Jing Zhang,Qian Li,Hailong Tian,Na Zhang,Zhonghao Li,Yuxia Luan

The short lifetime and easy quick elimination of the near-infrared (NIR) dye new indocyanine green (IR820) in the body restrict its practical application as a photothermal agent in cancer therapy. Meanwhile, the drawback of poor water solubility of the chemotherapeutic drug paclitaxel (PTX) largely restricts its clinical applications. Herein, we, for the first time, combined IR820 and PTX in an “all-in-one” fluorescence imaging-guided chemo–photothermal therapy (PTT) platform by a rational design of a novel pH- and enzyme-sensitive IR820–PTX conjugate assembly. Specifically, the IR820–PTX conjugate nanoparticles exhibit an extremely high therapeutic agent content (IR820 and PTX, 95.7%). Besides the good stability in bloodstream, the IR820–PTX nanoparticles can target tumors for high accumulation via the enhanced permeation and retention effect. Particularly, our IR820–PTX nanoparticles simultaneously solve the obstacles of PTX poor solubility and the short lifetime of IR820 for cancer therapy. The simultaneous release of the free drug and dye can efficiently kill tumor cells by the combination of PTT and chemotherapy via NIR irradiation. Furthermore, the combined therapy can be imaging-guided by measuring the NIR fluorescence imaging resulting from the IR820 component. Therefore, our rationally designed pH- and enzyme-sensitive IR820–PTX conjugate nanoparticles provide an alternative “all-in-one” option for an efficient combinational dual-therapy and imaging.

研究领域: 肿瘤学 · 药剂学 · 生物医学工程
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Small · 2018 ·Vol. 14 ·期 52 ·1802994 · IF 9.598

Rational Design of IR820- and Ce6-Based Versatile Micelle for Single NIR Laser–Induced Imaging and Dual-Modal Phototherapy

Xu Hu,Hailong Tian,Wei Jiang,Aixin Song,Zhonghao Li,Yuxia Luan

Phototherapy as a promising cancer diagnostic and therapeutic strategy has aroused extensive attention. However, single-wavelength near-infrared (NIR) light–triggered combinational treatment of photothermal therapy (PTT) and photodynamic therapy (PDT) is still a great challenge. Herein, a multifunctional micelle activated by a single-wavelength laser for simultaneous PTT and PDT as well as fluorescence imaging is developed. Briefly, new indocyanine green (IR820) is conjugated to d -α-tocopheryl polyethylene glycol 1000 succinate (TPGS) via the linker 6-aminocaproic acid, and then, chlorin e6 (Ce6) is encapsulated into the micelles formed by TPGS–IR820 conjugates to fabricate TPGS–IR820/Ce6 micelles. As the well-designed TPGS–IR820 conjugate shares a similar peak absorption wavelength with Ce6, this micelle can be applied with a single NIR laser (660 nm). The stable micelles exhibit excellent photothermal conversion efficiency in vitro and in vivo as well as high singlet oxygen generation capacity in tumor cells. After efficient cellular internalization, the as-prepared micelles display outstanding anticancer activity upon single NIR laser irradiation in vitro and in vivo. Furthermore, TPGS–IR820/Ce6 micelles show negligible systemic toxicity. The highly safe and effective TPGS–IR820/Ce6 micelles can offer an innovative strategy to construct single NIR light–induced PTT and PDT combined phototherapy nanoplatforms via suitable modification of organic phototherapeutic agents.

研究领域: 癌症研究 · 诊疗学 · 材料科学 · 生物医学工程
✓ 已验证 产品关联 DOI PubMed 高影响因子
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RSC Advances · 2022 ·Vol. 12 ·期 19 ·12136-12144 · IF 4.036

Rational synthesis of IR820–albumin complex for NIR-II fluorescence imaging-guided surgical treatment of tumors and gastrointestinal obstruction

Xinyu Feng,Yuan Cao,Pengrui Zhuang,Ran Cheng,Xuejun Zhang,Hong Liu,Guohe Wang,Shao-Kai Sun

IR820, an analog of FDA-approved indocyanine green, is a promising second near-infrared window (NIR-II) fluorescence probe with better NIR-II fluorescence stability and great clinical transformation potential. Moreover, its fluorescence can be further remarkably enhanced by the interaction with albumin. Therefore, it is significant to flexibly design IR820–albumin complex using endogenous or exogenetic albumin to meet the requirements of different biological applications. Herein, we show the rational synthesis of IR820–albumin complex for NIR-II fluorescence imaging-guided surgical treatment of tumors and gastrointestinal obstruction. We compared the NIR-II fluorescence imaging ability of IR820 pre-incubated with albumin or not to visualize tumors and the gastrointestinal tract in vivo and found that the formation of IR820–albumin was essential for the intense NIR-II fluorescence. For imaging-guided tumor treatment, after intravenous injection of free IR820, IR820–albumin complex can be formed in vivo due to the presence of plenty of albumin in the blood. For imaging-guided gastrointestinal obstruction removal, IR820–albumin complex should be synthesized in vitro before oral administration. NIR-II fluorescence imaging-guided surgeries were successfully realized in both tumor resection and gastrointestinal obstruction removal. Besides, toxicity assessments in vitro and in vivo confirmed the good biocompatibility of IR820. Our study provides a flexible paradigm for IR820-based NIR-II fluorescence imaging and surgical navigation towards different diseases.

CAS / MDL: 3599-32-4
研究领域: 生物医学工程 · 医学成像 · 外科手术 · 药学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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BIOMATERIALS · 2019 · IF 10.273

Fluorescence imaging guided CpG nanoparticles-loaded IR820-hydrogel for synergistic photothermal immunotherapy

Xia Dong,Jie Liang,Afeng Yang,Zhiyong Qian,Deling Kong,Feng Lv

As synergistic photothermal immunotherapy has developed as one of the most attractive strategies for cancer therapy, it is crucial to design an effective photothermal immunotherapy system to enhance the synergistic anti-tumor effect and reveal the essential role of each treatment. In this study, we designed CpG self-crosslinked nanoparticles-loaded IR820-conjugated hydrogel with dual self-fluorescence to exert the combined photothermal-immunotherapy. IR820-hydrogel can be effective for hyperthermia to eliminate the primary tumor based on its comprehensive coverage and generated photothermal-induced tumor antigens for assisted immunotherapy. CpG self-crosslinked nanoparticles improved the immune response of adjuvant against melanoma without extra nano-carriers. The synergistic photothermal immunotherapy was achieved by the merging of CpG self-crosslinked nanoparticles and IR820-hydrogel. A possible mechanism of combined antitumor effect was further revealed by analyzing immune cells including CD8 + T cells , DCs, B cells, Treg and MDSC in tumor microenvironment . The specific antitumor immunity was provoked to remove the tumor residues and ultimately the combined treatment mode achieved more effective systemic therapeutic effect than either photothermal therapy or immunotherapy alone. Furthermore, self-fluorescent IR820-hydrogel and CpG nanoparticles exerted the imaging-guided combined photothermal-immunotherapy by the dual fluorescence imaging method without additional fluorescent labeling . This visible combined photothermal-immunotherapy offers a potential for precise cancer treatment.

研究领域: 肿瘤学 · 生物医学工程 · 免疫学 · 诊疗学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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CHEMICAL ENGINEERING JOURNAL · 2020 · IF 10.652

A novel biocompatible PDA/IR820/DAP coating for antibiotic/photodynamic/photothermal triple therapy to inhibit and eliminate Staphylococcus aureus biofilm

Junkai Zeng,Yitong Wang,Zhenyu Sun,Haishuang Chang,Mi Cao,Jie Zhao,Kaili Lin,Youzhuan Xie

Surgical site infection (SSI) with instrumentation is an undesired and troublesome complication in orthopaedics. Surgical debridement is currently the main treatment option. However, the poor prognosis remains the major problem and over 40% of patients needed additional surgery to remove the implant. To eliminate SSI, antibacterial and biocompatible implants are urgently needed. Herein, a novel biocompatible polydopamine (PDA)-IR820-Daptomycin (DAP) coating with triple therapy functions was successfully fabricated to enhance the anti-infection ability and osteogenic property of titanium implants. In which, PDA served as a biocompatible binder to immobilize IR820 and DAP, and possessed photothermal and osteogenic properties. The releasing of DAP inhibited the growth of Staphylococcus aureus and damaged the bacterial membrane. Meanwhile, after 808 nm laser irradiation, the combination of hyperthermia generated by PDA and singlet oxygen ( 1 O 2 ) produced by IR820 eradicated the biofilm noninvasively. Furthermore, this coating successfully accelerated glutathione (GSH) oxidation and destroyed the bacterial membrane, reaching an anti-bacterial efficiency of 97.2% in vitro . Additionally, the coating significantly stimulated the proliferation and osteogenic differentiation of rat bone marrow stem cells (rBMSCs). In vivo, Ti-PDA-IR820-DAP reached an anti-bacterial efficiency of 97.9% in a S. aureus biofilm-infected rat model with 15 min of irradiation at 50 °C and drastically promoted the bone-implant osseointegration in a rat femur condyle defect model. The present study demonstrates that combining antibiotics and phototherapy represents a feasible way to treat bone-implant-associated infections.

研究领域: 生物医学工程 · 材料科学 · 传染病学 · 骨科
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DRUG DEVELOPMENT RESEARCH · 2022 ·Vol. 83 ·期 8 ·1923-1933 · IF 5.004

Conjugates of lactobionic acid and IR820: New photosensitizers for efficient photodynamic therapy of hepatoma cells

Xiaoyin Yuan,Yayu Tao,Wen Xiao,Kunda Du,Hang Hu,Defeng Xu,Qingbo Xu

New indocyanine green (IR820) is an indocyanine green analog which has attracted increasing attention in cancer phototherapy for the prominent absorbance at near-infrared region and improved stability. However, the lack of tumor targeting ability is still an obstacle that severely limits the application of IR820. Lactobionic acid (LA) is a ligand for the asialoglycoprotein receptors which are overexpressed on the membrane of hepatocellular carcinoma cells. In this work, three conjugates of LA and IR-820, namely LA-IR820, LA-SS-IR820, and LA-DEG-IR820, were developed for targeted photodynamic therapy of hepatocellular carcinoma (HCC). The in vitro photodynamic effect study shows that LA-IR820, LA-SS-IR820 and LA-DEG-IR820 exhibit similar singlet oxygen quantum yield as compared to free IR820. The cellular uptake study demonstrates that LA-IR820, LA-SS-IR820, and LA-DEG-IR820 exhibit enhanced cellular uptake amount as compared to free IR820 due to the ligand-receptor interactions between LA and asialoglycoprotein receptor overexpressed on the membrane of HepG2 cells. Among these three conjugates, LA-IR820 with hydrodynamic diameter of 154.6 ± 6.1 nm exhibits the highest cellular uptake amount. The cellular reactive oxygen species (ROS) generation study shows that LA-IR820, LA-SS-IR820 and LA-DEG-IR820 display enhanced cellular ROS level as compared to free IR820 and LA-IR820 exhibits the highest cellular ROS level upon 600 mW/cm 2 660 nm laser irradiation. As a result, LA-IR820, LA-SS-IR820 and LA-DEG-IR820 exhibit enhanced photocytotoxicity against HepG2 cells as compared to free IR820 and LA-IR820 exhibits the highest photocytotoxicity. LA-IR820, LA-SS-IR820, and LA-DEG-IR820 show significant potential for the targeted photodynamic therapy of HCC.

研究领域: 肿瘤学 · 光动力治疗 · 药物递送 · 分子成像 · 纳米医学
✓ 已验证 DOI 高影响因子
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JOURNAL OF ALLOYS AND COMPOUNDS · 2023 · IF 6.2

MoS2-based nanocomposites with high photothermal conversion efficiency for combinational photothermal/photodynamic tumor therapy

Jing Liu,Endian Cui,Qun Zhang,Denghui Xie

Photothermal conversion efficiency (PCE) plays a crucial role in tumor photothermal therapy (PTT). In this work, we developed a MoS 2 -based antitumor agent with enhanced photothermal conversion efficiency by size/morphology tailoring and IR820 loading for combinational photothermal/photodynamic therapy (PTT/PDT) of breast cancer. Among three MoS 2 -based nanomaterials, namely MoS 2 nanospheres (NSs), MoS 2 nanoflowers (NFs) and MoS 2 quantum dots (QDs), MoS 2 NSs possessed the highest PCE at 37.48%. In order to further improve the PCE, polyethyleneimine (PEI)-assisted photosensitizer IR820 decoration was carried out to prepare the MoS 2 @PEI@IR820 (MPI) nanocomposite. The introduced IR820 not only improves PCE of the MoS 2 nanomaterials to 47.08% by increasing the light absorption for enhancing PTT, but produces cytotoxic ROS for PDT, resulting in a combinational PTT/PDT with the multifunctional MPI. In addition, in vivo fluorescence (FL) bioimaging and infrared thermographic imaging have been achieved by the designed MPI nanoplatform, which has proven to be good biocompatibility, low toxicity and high PCE. This study provides a novel way for the design and construction of prominent theragnostic nanoagents for combinational PTT/PDT.

研究领域: 生物医学工程 · 纳米医学 · 肿瘤学
✓ 已验证 产品关联 DOI 高影响因子
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International Journal of Nanomedicine · 2026 · IF 8.7

Hollow Cu2-xSe/PDA/IR820 Composite Nanoparticles with pH Response for Multimodal Synergistic Treatment of Esophageal Cancer

Feixiao Ma,Anqi Ji,Beng Ma,Pingjuan Yang,Jiayi Li,Shuxin Liao,Haonan Yao,Xuanhu Xie,Zhiwei Wang,Linlin Shi,Shegan Gao,Xin Hou

Purpose Esophageal cancer (EC) ranks among the most prevalent and lethal malignancies worldwide, and conventional therapeutic modalities, including surgery, radiotherapy, and chemotherapy, are constrained by inherent limitations. Recent advances in nanomedicine have opened new avenues for EC treatment. To achieve efficient and precise tumor eradication, this study developed a pH-responsive composite nanoplatform featuring a hollow architecture to enable high-efficiency loading of photosensitizers and realize multimodal synergistic therapy against EC through the integration of photothermal therapy (PTT), photodynamic therapy (PDT), and chemodynamic therapy (CDT).Methods A pH-responsive Cu2-xSe/PDA/IR820 composite nanoplatform was constructed by coating hollow Cu2-xSe nanoparticles with polydopamine PDA and loading the near-infrared photosensitizer IR820. Morphology, crystalline phase, elemental composition, and surface chemistry were characterized by TEM, XRD, XPS, and FT-IR. Photothermal conversion efficiency was quantified under 808 nm laser irradiation. IR820 release kinetics were monitored under different pH conditions of 5.0, 6.0, and 7.0 to assess pH-responsive behavior. In vitro studies on KYSE-150 EC cells included viability by CCK-8 assay, apoptosis by flow cytometry, ROS generation by DCFH-DA probe, mitochondrial membrane potential by JC-1 staining, and cellular uptake analysis. In vivo antitumor efficacy and biosafety were evaluated in an AKR tumor-bearing C57BL/6J mouse model via intratumoral injection and 808 nm laser irradiation, followed by tumor volume measurement, histopathological analysis with H&E, Ki-67, and TUNEL staining, and systemic toxicity assessment.Results The hollow Cu2-xSe/PDA/IR820 nanoparticles exhibited a uniform size of approximately 164 nm, excellent colloidal stability, and a high photothermal conversion efficiency of 44.56% under 808 nm laser irradiation. IR820 release displayed pronounced pH sensitivity, with a cumulative release of 23.07% at pH 5.0 within 30 minutes. In vitro, the nanoplatform combined with laser irradiation reduced KYSE-150 cell viability to 1.2% at 100 μg/mL, with an IC50 value of 18.74 μg/mL, induced 28.57% apoptosis, elevated intracellular ROS levels, decreased mitochondrial membrane potential, and depleted glutathione to 335 μmol/gprot. In vivo fluorescence imaging confirmed effective tumor accumulation via the EPR effect, with peak signal at 24 hours post-injection. Combined PTT/PDT/CDT treatment significantly suppressed tumor growth, reducing final tumor volume to 17.8% of the control group, and induced extensive apoptosis and necrosis in tumor tissues. Systemic biosafety evaluations revealed no significant hematological or histopathological abnormalities.Conclusion Hollow Cu2-xSe/PDA/IR820 composite nanoparticles loaded with IR820 were successfully fabricated and demonstrated remarkable advantages in multimodal combination therapy against EC.

✓ 已验证 DOI PubMed 高影响因子
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BIOMATERIALS · 2016 · IF 8.387

Mild photothermal therapy/photodynamic therapy/chemotherapy of breast cancer by Lyp-1 modified Docetaxel/IR820 Co-loaded micelles

WenTing Li,JinRong Peng,LiWei Tan,Jing Wu,Kun Shi,Ying Qu,XiaWei Wei,ZhiYong Qian

Patients suffering from cancer have benefited from combination therapy. Nanocarriers are the ideal candidates for combination therapy. In this study, we constructed docetaxel (DTX) loaded micellar nanomedicines co-loaded with near infrared (NIR) dye-IR820 for photothermal therapy (PTT)/photodynamic therapy (PDT)/chemotherapy of breast cancer. Lyp-1, a tumor homing peptide, was introduced into the nanosystems to construct the active targeting nanomedicine. In order to deliver IR820 to the tumor site and overcome its short lifetime in vivo , a PEI derivative—PCL-g-PEI was introduced. IR820 with negative charge was formed stable static interaction with the amine groups, meanwhile, the absorption of IR820 in the NIR region was weakened. It indicated that the nanosystem constructed in this study may provide an alternative candidate for mild PTT. By the evaluation of the photothermal conversion in vivo , we can confirm that IR820 has been successfully delivered and effectively accumulated in the tumor site. Furthermore, the tumor cells targeting and anticancer performances of this nanosystem have been studied in vitro and in vivo . The results demonstrated Lyp-1 modification has enhanced the tumor targeting delivery of DTX and IR820. By combining PTT and PDT, DTX nanomedicine efficiently inhibited the growth and metastasis of breast cancer in mice. This nanosystem is a promising candidate for combination therapy of breast cancer.

研究领域: 肿瘤学 · 药学 · 纳米技术 · 治疗学
✓ 已验证 DOI PubMed 高影响因子
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Journal of Materials Chemistry B · 2020 ·Vol. 8 ·期 19 ·4331-4339 · IF 5.344

Rapidly dissolving microneedle patch for synergistic gene and photothermal therapy of subcutaneous tumor

Qinan Xu,Xinfang Li,Peng Zhang,Youxiang Wang

The synergistic combination of gene therapy and photothermal therapy (PTT) has been widely investigated as a promising strategy for cancer treatment. To deliver genes and photothermal agents simultaneously and accurately to a tumor site, a microneedle (MN) patch co-loaded with p53 DNA and IR820 was fabricated by a two-step casting method. Hyaluronic acid was chosen as a matrix and p53 DNA and IR820 were mainly loaded into the tips to enhance utilization and reduce waste. The MN patch could efficiently penetrate the stratum corneum, and dissolve rapidly to release p53 DNA and IR820 in the subcutaneous tumor site. Due to the efficient photothermal efficacy of IR820, the temperature of the tumor site where the MN patch was applied increased by 14.7 °C under near-infrared light irradiation. The MN patch showed excellent antitumor effects in vivo owing to the synergistic effect of gene therapy and PTT. Consequently, the p53 DNA/IR820 MN patch may be a promising synergistic strategy for subcutaneous tumor treatments.

研究领域: 生物医学工程 · 肿瘤学 · 纳米技术 · 药学
✓ 已验证 DOI PubMed 高影响因子
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