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Materials Today Bio · 2025 · IF 10.2

Co-encapsulated Ce6 + CpG and biopeptide-modified liposomes for enhanced transdermal photo-immunotherapy of superficial tumors

Shaozhen Wang,Chen Yang,Yuanyuan Zhang,Yi Hu,Lan Xiao,Weiping Ding,Bensheng Qiu,Fenfen Li

Cancer immunotherapy encounters challenges of a low treatment response rate due to the tumor immunosuppressive microenvironment and immune-related adverse events caused by off-target immunotherapy agents delivered through systemic administration in clinical practice. Photodynamic therapy (PDT) offers a viable approach to improve the immunotherapy efficacy through inducing immunogenic tumor cell death and is particularly advantageous in superficial tumor treatment. Therefore, leveraging integrated nanomaterials for photo-immunotherapy appears to be an ideal strategy to improve therapeutic outcome. In this study, we develop a transdermal-enhancing peptide (TD)-modified cationic liposome that simultaneously encapsulated with photosensitizer chlorine 6 (Ce6) and immunoadjuvant CpG, denoted as Ce6/CpG@Lip-TD, to mediate photo-immunotherapy of superficial tumors via the skin. The functionalization of TD peptide and positively charged surface endow the liposomes enhanced skin penetration capability. The combination of Ce6 and CpG within the liposomes synergistically potentiates the photo-immunotherapy effect when exposed to laser irradiation. In both melanoma and breast cancer murine models, Ce6/CpG@Lip-TD demonstrated substantial tumor-suppressing properties, along with an augmented systemic immune response against distal tumors. As a topical therapeutic agent, Ce6/CpG@Lip-TD circumvents the regulatory challenges associated with the systemic delivery of nanomaterials and significantly reduces systemic side effects, holding great promise for rapid translation into clinical applications.

CAS / MDL: 148504-34-1
研究领域: 肿瘤学 · 纳米医学 · 免疫学
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MATERIALS & DESIGN · 2026 · IF 8.2

UCNPs@Ce6-based Near-Infrared photodynamic therapy triggers mitophagy-related apoptosis in esophageal squamous cell carcinoma

Wenqing Chen,Xiaohui Lin,Tianmei Zhang,Yu Luo,Zhimei Huang,Danlei Chen,Xingwu Zheng,Jian Wen

This upconversion nanoprobe shifts Er 3+ emission from 540 to 660 nm for efficient Ce6 excitation. • First report that Ce6-loaded upconversion nanoparticles are excellent biocompatible and target ESCC cells. • The UCNPs@Ce6 platform dually functions: with PDT, ROS‑mitophagy/apoptosis alone, autophagy‑mediated anti‑inflammation. Chlorin e6 (Ce6), an efficient photosensitizer, suffers from poor biocompatibility, and lanthanide-doped upconversion nanoparticles (UCNPs) possess unique optical properties, yet their roles in esophageal squamous cell carcinoma (ESCC) remain unclear. In this study, Ce6-loaded UCNPs (UCNPs@Ce6) with a core–shell-shell structure was designed and synthesized to overcome the limitation of conventional photodynamic therapy (PDT) that relies on shallow-penetrating light. In vitro, UCNPs@Ce6-PDT selectively inhibited ESCC cells without affecting normal esophageal epithelial cells. Mechanistically, PDT induced mitochondrial dysfunction, mitophagy, and apoptosis via the reactive oxygen species (ROS)-mitochondrial pathway, whereas UCNPs@Ce6 alone activated autophagy and inhibited pyroptosis/necroptosis-related inflammation. In vivo, the fluorescence image-guided tumor therapy achieved tumor growth inhibition (73.72% ± 2.88%) without obvious toxicity. Collectively, this nanoplatform provides a safe and effective strategy for targeted therapy of ESCC by combining PDT-triggered mitophagy-related apoptosis with autophagy-mediated anti-inflammatory responses. Download: Download high-res image (151KB) Download: Download full-size image

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Scientific Reports · 2016 ·Vol. 6 ·期 1 ·1-12 · IF 5.228

Superparamagnetic Fe3O4-PEG2K-FA@Ce6 Nanoprobes for in Vivo Dual-mode Imaging and Targeted Photodynamic Therapy

Yin Ting,Huang Peng,Gao Guo,Shapter Joseph G.,Shen Yulan,Sun Rongjin,Yue Caixia,Zhang Chunlei,Liu Yanlei,Zhou Sui,Cui Daxiang

The development of targeted nanoprobes is a promising approach to cancer diagnostics and therapy. In the present work, a novel multifunctional photo/magnet-diagnostic nanoprobe (MNPs-PEG 2K -FA@Ce6) has been developed. This nanoprobe is built using folic acid (FA), bifunctional polyethylene glycol (PEG 2K ) and photosensitizer chlorin e6 (Ce6). The MNPs-PEG 2K -FA@Ce6 nanoprobes are superparamagnetic, can be synthesized on a large scale by a one-pot hydrothermal process without further surface modification and are stable in an aqueous environment for eight months. Compared with free Ce6 nanoprobes in vitro studies, the MNPs-PEG 2K -FA@Ce6 nanoprobes significantly enhance cellular uptake efficiency and promote the effectiveness of photodynamic therapy (PDT) with the assistance of 633 nm laser irradiation. The unique nanoprobes show superior penetration and a retention time of more than six days with less accumulation in the liver allowing highly effective tumor recognition and monitoring. Additionally, there was little damage to healthy organs or tissues. These exciting new nanoprobes could be potential building blocks to develop new clinical therapies and translational medicine.

研究领域: 生物医学工程 · 癌症研究 · 分子影像学
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International Journal of Nanomedicine · 2023 · IF 8

808 nm Near-Infrared Light-Excited UCNPs@mSiO2-Ce6-GPC3 Nanocomposites For Photodynamic Therapy In Liver Cancer

Jiahe Hu,Jialan Shi,Yingqian Gao,Wei Yang,Ping Liu,Qinghao Liu,Fei He,Chunxu Wang,Tao Li,Rui Xie,Jiuxin Zhu,Piaoping Yang

Background It is important to explore effective treatment for liver cancer. Photodynamic therapy (PDT) is a novel technique to treat liver cancer, but its clinical application is obstructed by limited depth of visible light penetration into tissue. The near-infrared (NIR) photosensitizer is a potential solution to the limitations of PDT for deep tumor tissue treatment.Purpose We aimed to investigate 808 nm NIR light-excited UCNPs@mSiO2-Ce6-GPC3 nanocomposites for PDT in liver cancer.Methods In our study, 808 nm NIR light-excited upconversion nanoparticles (UCNPs) were simultaneously loaded with the photosensitizer chlorin e6 (Ce6) and the antibody glypican-3 (GPC3), which is overexpressed in hepatocellular carcinoma cells. The multitasking UCNPs@mSiO2-Ce6-GPC3 nanoparticles under 808 nm laser irradiation with enhanced depth of penetration would enable the effective targeting of PDT.Results We found that the UCNPs@mSiO2-Ce6-GPC3 nanoparticles had good biocompatibility, low toxicity, excellent cell imaging in HepG2 cancer cells and high anti-tumor effect in vitro and in vivo.Conclusion We believe that the utilization of 808 nm NIR excited UCNPs@mSiO2-Ce6-GPC3 nanoparticles for PDT is a safe and potential therapeutic option for liver cancer.

研究领域: 生物医学工程 · 癌症研究 · 纳米技术 · 治疗学
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ACS Applied Bio Materials · 2021 · IF 0

Photodynamic and Photothermal Ce6-Modified Gold Nanorod as a Potent Alternative Candidate for Improved Photoinactivation of Bacteria

Baoqu Zhang,Hongjun Yan,Zhouting Meng,Peiyuan Li,Xiantao Jiang,Zihua Wu,Jun-An Xiao,Wei Su

The global rise of antibiotic resistance of pathogenic bacteria has become an increasing medical and public concern, which is further urging the development of antimicrobial channels for treating infectious diseases. The combination of photodynamic therapy (PDT) with photothermal therapy (PTT) has been considered as a promising alternative way for the replacement of traditional antibiotic therapy. In this research, the newly fabricated Chlorin-e6 (Ce6) conjugated mesoporous silica-coated AuNRs, designated AuNR@SiO2-NH2-Ce6, exhibited synergistic photothermal effects and single oxygen localized generation property, and showed stronger photoinactivation for bacteria compared with Ce6. AuNR@SiO2-NH2-Ce6 can anchor to the cell membrane and accumulate in the interior of cells. Furthermore, the unique porous structure of AuNR@SiO2NH2 enabled Ce6 encapsulation in the mesopores and was subsequently released and activated by photothermic effect, allowing the generated single oxygen to penetrate into the cytoplasmic membrane or directly enter the interior of bacteria cells, thus overcoming the inherent defects of single oxygen. AuNR@SiO2-NH2-Ce6 not only damaged the integrity of the cell membrane of bacteria but also facilitated the cellular permeation and accumulation of external nanoagents in the bacteria upon light irradiation. In addition, AuNR@SiO2-NH2-Ce6 exhibited negligible cytotoxicity toward mammalian cells and hemolytic activity. Therefore, AuNR@SiO2-NH2-Ce6 may be highly promising candidates as topical antibacterial agents, and this study has wide implications on the design of next-generation antimicrobial agents.

研究领域: 生物医学工程 · 微生物学 · 纳米医学
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ACS Omega · 2023 · IF 4.1

Lutein-Based pH and Photo Dual-Responsive Novel Liposomes Coated with Ce6 and PTX for Tumor Therapy

Hong Shen,Changwei Zhang,Chengzhang Wang,Jianxin Jiang,Fengxia Tang,Chuan Li,Hua Yuan,Xiaoran Yang,Zhenkai Tong,Yi Huang

Liposomes are considered the best nanocarrier for delivering cancer drugs such as chlorin e6 (Ce6) and paclitaxel (PTX). However, the poor stability and non-selectivity release of liposomes may severely limit their further applications. In this study, based on the characteristics of lutein (L) photo-response and orthoester (OE) acid-response, stable and dual-responsive liposomes (Dr-lips) have been prepared. The Dr-lips exhibited a spherical shape with a uniform size of approximately 58.27 nm. Moreover, they displayed a zeta potential ranging from −45.45 to −28.25 mV and showed excellent storage stability, indicating stable colloidal properties. Additionally, they achieved high drug encapsulation rates, with 92.27% for PTX and 90.34% for Ce6, respectively. Meanwhile, under near-infrared (NIR) light at 660 nm, Ce6 plays a key role in accelerating the photodegradation rate of lutein and PEG-OE-L while also enhancing tissue penetration ability. Additionally, Dr-lips loaded with Ce6 and PTX not only displayed excellent pH and photo dual-responsiveness for targeted delivering and releasing but also showed remarkable reactive oxygen species (ROS) generation capacity and impressive anti-tumor activity in vitro. Therefore, it provides a novel strategy for optimizing stability and enhancing their targeted drug delivery of liposome.

研究领域: 药剂学 · 肿瘤学 · 生物医学工程
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Journal of Nanomaterials · 2022 · IF 3.791

Multiclawed SiO2 Nano-Antibacterial Agent Based on Charge Inversed Ce6 Ionic Liquid Polymers for Combating Oral Biofilm Infection

Ziyi Jiao,Yonggang Teng,Chunjing Zhan,Youbei Qiao,Yuying Ma,Chaoli Wang,Hong Wu

Photodynamic antimicrobial chemotherapy (PACT) is a promising therapy against biofilm infection. However, due to the saliva clearance and obstacle of biofilm, the photosensitizer is difficult to concentrate in the infection site; then, the PACT is less effective on oral biofilm infection. In this article, we report a special nano-antibacterial agent (SiO2-PCe6-IL) to solve the bottleneck problem of PACT in treatment of oral biofilm infections. The SiO2-PCe6-IL was composed of SiO2 and poly ionic liquid photosensitizer (PCe6-IL) and had tri-fold features of eliminate biofilm infection: high binding ability, breaking biofilm barriers, and enrichment photosensitizer in infection site. In oral biofilm, the SiO2-PCe6-IL changed to SiO2-PIL+ like claws of octopus that could hold tightly with biofilm. Then, the poly-dodecyl on the SiO2-PIL+ broke down the barrier of biofilm. The results of HR-MS and zeta potential indicated that SiO2-PCe6-IL could change to positive (SiO2-PIL+) in acidic environment. The interaction forces and morphology results proved that the SiO2-PIL+ had a higher affinity to biofilm and could destroy the biofilm structure. Then, the photosensitizer was enriched in biofilm at sites of infection. The in vitro and in vivo experiments showed that SiO2-PCe6-IL could effectively eradicate oral biofilm infections and control of dental caries.

研究领域: 医学 · 材料科学 · 生物学
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NANOTECHNOLOGY · 2025 ·Vol. 36 ·期 30 ·305101 · IF 2.8

Enhanced ferroptosis by light-triggered biomimetic nano-erythrocyte membranes for tumor synergistic therapy

Gaojian Liu,Wenjing Wen,Xuan Zhao,Yanan Jing,Hao Li,Xulong Fan,ZiXuan Huang,Gaofeng Liang

Breast cancer is the most prevalent fatal cancer among women worldwide and the leading cause of death for women. Ferroptosis is a form of programmed cell death that relies on iron and is non-apoptotic, triggered by the inhibition of the cellular antioxidant system. Photodynamic therapy (PDT) employs photosensitizers to produce reactive oxygen species (ROS), increasing oxidative stress in tumor cells. When combined with ferroptosis, PDT can work synergistically to regulate intracellular redox balance. In this study, we designed engineered nano-erythrocyte membranes for targeted delivery of Chlorin e6 (Ce6) and cisplatin (DDP) to enhance breast cancer treatment. By using mild ultrasound, Ce6 and DDP were co-loaded onto the nano-erythrocyte membranes, combining ferroptosis inducers and photosensitizers to combat breast cancer. To improve targeting capability towards breast cancer, RGD cyclic peptides were modified onto the nano-erythrocyte membranes through a thiol–maleimide coupling reaction. The RGD-modified nano-erythrocyte membranes co-loaded with Ce6 and DDP not only inherited the good stability and significant biocompatibility of red blood cell membranes but also promoted the uptake by breast cancer cells, effectively inducing ferroptosis in these cells. In conclusion, this multifunctional ‘natural’ nanodrug delivery system provides an effective and safe method for PDT combined with ferroptosis for breast cancer treatment.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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ACS Applied Bio Materials · 2021 · IF 0

pH/ROS Dual-Responsive Polymer–Drug-Based Nanocarriers: Click-Reaction Preparation and Fluorescence Imaging-Guided Chemotherapy and Photodynamic Therapy

Ning Zhang,Daquan Wang,Xunan Jing,Tingting Yang,Hongbo Yang,Lingjie Meng

In the past decades, polymer–drug conjugates of anticancer agents have gained much attention due to their enhanced aqueous solubility, improved pharmacokinetics, and better drug utilization than their conventional insoluble counterparts. Several polymer–drug conjugates have entered the third phase of clinical trials yet suffer from inherent deficiencies, including uncontrolled drug release and unclear degradation mechanisms. In this study, a pH/reactive oxygen species (ROS) dual-responsive PEG-doxorubicin (DOX) conjugate (denoted as TPD) was synthesized through acyl alkynyl-amine click reaction by PEG dipropiolate (PEGB), amine-terminated thioketal (TKL), and doxorubicin (DOX). Due to the generated ene-amine and thioketal in the backbone, the prepared amphiphilic TPD not only has a high drug loading ratio for photosensitizer chlorin e6 (Ce6) but also has the sensitivity to the acidic tumor microenvironment (TME) and ROS. Considering the complex conditions of TME, the prepared TPD@Ce6 nanoparticles (NPs) might respond to the relatively low pH and release Ce6 initially, and upon laser radiation, Ce6 produces abundant singlet oxygen (1O2) to achieve a programmable accelerated release of DOX and more Ce6 at the tumor site. In addition, the NIR fluorescence of DOX could monitor drug delivery and controlled release. The developed TPD@Ce6 NPs can realize the targeted tumor in combination therapy with negligible cytotoxicity on normal tissues.

研究领域: 药学 · 肿瘤学 · 生物材料学
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ACS Applied Materials & Interfaces · 2018 · IF 8.097

pH-Responsive Magnetic Mesoporous Silica-Based Nanoplatform for Synergistic Photodynamic Therapy/Chemotherapy

Xiang-long Tang,Feng Jing,Ben-lan Lin,Sheng Cui,Ru-tong Yu,Xiao-dong Shen,Ting-wei Wang

By overcoming drug resistance and subsequently enhancing the treatment, the combination therapy of photodynamic therapy (PDT) and chemotherapy has promising potential for cancer treatment. However, the major challenge is how to establish an advanced nanoplatform that can be efficiently guided to tumor sites and can then stably release both chemotherapy drugs and a photosensitizer simultaneously and precisely. In this study, which considered the possibility and targeting efficiency of a magnetic targeting strategy, a novel Fe3O4@mSiO2(DOX)@HSA(Ce6) nanoplatform was successfully built; this platform could be employed as an efficient synergistic antitumor nanoplatform with magnetic guidance for highly specific targeting and retention. Doxorubicin (DOX) molecules were loaded into mesoporous silica with high loading capability, and the mesoporous channels were blocked by a polydopamine coating. Human serum albumin (HSA) was conjugated to the outer surface to increase the biocompatibility and blood circulation time, as well as to provide a vehicle for loading photosensitizer chlorin e6 (Ce6). The sustained release of DOX under acidic conditions and the PDT induced by red light exerted a synergistic inhibitory effect on glioma cells. Our experiments demonstrated that the pH-responsive Fe3O4@mSiO2(DOX)@HSA(Ce6) nanoplatform was guided to the tumor region by magnetic targeting and that the nanoplatform suppressed glioma tumor growth efficiently, implying that the system is a highly promising photodynamic therapy/chemotherapy combination nanoplatform with synergistic effects for cancer treatment.

研究领域: 纳米技术 · 癌症研究 · 生物医学工程 · 药学
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CARBOHYDRATE POLYMERS · 2024 · IF 10.7

Fucoidan based Ce6-chloroquine self-assembled hydrogel as in situ vaccines to enhance tumor immunotherapy by autophagy inhibition and macrophage polarization

Teng Wang,Yu Wang,Bingjie Wang,Yanguo Su,Tianze Jiang,Tiantian Gan,Xia Zhao

Tumor vaccines have become a promising approach for cancer treatment by triggering antigen-specific responses against tumors. However, autophagy and immunosuppressive tumor microenvironment (TME) reduce antigen exposure and immunogenicity, which limit the effect of tumor vaccines. Here, we develop fucoidan (Fuc) based chlorin e6 (Ce6)-chloroquine (CQ) self-assembly hydrogels (CCFG) as in situ vaccines. Ce6 triggers immune response in situ by photodynamic therapy (PDT) induced immunogenic cell death (ICD) effect, which is further enhanced by macrophage polarization of Fuc and autophagy inhibition of CQ. In vivo studies show that CCFG effectively enhances antigen presentation under laser irradiation, which induces a powerful in situ vaccine effect and significantly inhibits tumor metastasis and recurrence. Our study provides a novel approach for enhancing tumor immunotherapy and inhibiting tumor recurrence and metastasis.

CAS / MDL: 54-05-7 19660-77-6
研究领域: 肿瘤学 · 免疫学 · 药学 · 生物医学工程
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CHEMICAL ENGINEERING JOURNAL · 2021 · IF 13.273

pH/near-infrared light dual activated Ce6-doped silicon nanoparticles with tumor chemo-photodynamic synergistic therapy for improving efficiency of monotherapy

Tonghao Ma,Qi Zhang,Qize Xuan,Jiafeng Zhuang,Wei Zhang,Hui Li,Chao Chen,Ping Wang

Currently, single chemotherapeutics or photosensitizers implemented in clinic present huge challenges in terms of unfavorable therapeutic efficacy, physiological instability and non-selective toxicity. In order to remedy the faultiness of insufficient efficiency of monotherapy, we herein synthesized an “all-in-one” targeting drug delivery system with multimodal therapy based on chemo-photodynamic synergistic therapy. Specifically, mesoporous silica nanorods were first synthesized through doping chlorin e6 (Ce6) in the sol–gel process, and then were used to load chemotherapy drug. After the amino groups and boronic acid groups were sequentially modified on the surface of nanoparticles, lactobionic acid (LA) was chosen as an intermediary to achieve simultaneous crosslinking of targeting agent LA and sealing agent sericin through pH responsive boronic ester linkage. The obtained ultimate nanocomposites possessed good biocompatibility, colloidal stability and hemocompatibility. Besides, in vitro endocytosis experiment performed with confocal laser scanning microscopy and flow cytometry testified the LA-mediated accurate tumor-specific targeting ability of synthesized nanocarriers. Moreover, a series of in vitro assays demonstrated that fabricated therapeutic nanoplatform could not only release loaded drugs in response to acidic environment to achieve chemotherapy, but also could generate singlet oxygen from photosensitizer Ce6 under external light stimulation to realize photodynamic therapy. Most interestingly, the combination therapy including photodynamic therapy and chemotherapy exhibited a synergistic effect against tumor cells in both in vivo and ex vivo experiments. Briefly, the drug delivery system reported here could attain effective chemo-photodynamic synergistic therapy to dispose of the insufficient lethality of monotherapy while guaranteeing the safety during in vivo application.

CAS / MDL: 25952-53-8 6066-82-6
研究领域: 纳米医学 · 肿瘤学 · 药物递送系统
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