Pharmaceutics
·
2024
·Vol. 16
·期 6
·744
·
IF 4.9
Qianqian Long,Xinmin Zhao,Lili Gao,Mengyuan Liu,Feng Pan,Xihui Gao,Changyou Zhan,Yang Chen,Jialei Wang,Jun Qian
Background:Nanoparticles conjugated with fluorescent probes have versatile applications, serving not only for targeted fluorescent imaging but also for evaluating the in vivo profiles of designed nanoparticles. However, the relationship between fluorophore density and nanoparticle behavior remains unexplored.Methods:The IR783-modified liposomes (IR783-sLip) were prepared through a modified ethanol injection and extrusion method. The cellular uptake efficiency of IR783-sLip was characterized by flow cytometry and fluorescence microscope imaging. The effects of IR783 density on liposomal in vivo behavior were investigated by pharmacokinetic studies, biodistribution studies, and in vivo imaging. The constitution of protein corona was analyzed by the Western blot assay.Results:Dense IR783 modification improved cellular uptake of liposomes in vitro but hindered their blood retention and tumor imaging performance in vivo. We found a correlation between IR783 density and protein corona absorption, particularly IgM, which significantly impacted the liposome performance. Meanwhile, we observed that increasing IR783 density did not consistently improve the effectiveness of tumor imaging.Conclusions:Increasing the density of modified IR783 on liposomes is not always beneficial for tumor near-infrared (NIR) imaging yield. It is not advisable to prematurely evaluate novel nanomaterials through fluorescence dye conjugation without carefully optimizing the density of the modifications.
研究领域:
药剂学
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生物医学工程
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分子影像学
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产品关联
DOI
PubMed
高影响因子
Advanced Science
·
2025
·
IF 14.1
Jinzhao Liu,Meicen Wu,Qingyang Lyu,Chang Yang,Ni Fan,Kang Chen,Weiping Wang
Immune evasion and metastasis are the leading causes of poor prognosis in triple-negative breast cancer treatment. Since current standard immunotherapies have limited efficacy due to immunologically cold microenvironment, it is crucial to explore new strategies to sensitize anticancer immune response. In this study, it is found that incorporating β -lapachone-based oxidation therapy with CUDC101-initiated epigenetic regulation results in synergistic antitumor effects and potent immune activation. To co-deliver these two hydrophobic drugs, IR783 with cyanine structure serves as the stabilizer to form a nanoformulation based on small molecule self-assembly. Such IR783-stabilized nanodrugs can not only lead to cancer cell apoptosis through HDAC inhibition-enhanced oxidation therapy but also cooperatively induce immunogenic cell death and promote pro-inflammatory cytokine gene expression to reshape immunosuppressive microenvironment. Besides, nanodrugs can inhibit both primary and distant tumor growth effectively by elevating systemic anticancer immunity. This study provides a promising approach to synergize oxidation therapy with epigenetic modulation for safe and efficient breast cancer immunotherapy.
研究领域:
肿瘤学
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免疫学
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药剂学
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产品关联
DOI
PubMed
高影响因子
ACS Omega
·
2025
·
IF 4.3
Yuxiang Gao,Rong Ma,Lijun Zhu,Zhong Du,Jiabao Xiong,Chi Zhang,Xueliang Zhang,Cailing Ma,Nuernisha Alifu
Near-infrared-II (NIR-II, 900–1700 nm) fluorescence imaging as one of the emerging imaging methods has shown the advantages of excellent spatial resolution and sensitivity. In order to obtain high-quality NIR-II fluorescence images and effective treatment results, it is essential to develop theranostic fluorescent nanoprobes with good tumor targeting and treatment capabilities. Herein, we designed and synthesized novel NIR-II fluorescent theranostic nanoprobes based on the organic dye IR783. IR783 was further encapsulated into liposomes, along with the chemotherapeutic drug doxorubicin (DOX) and the cervical cancer-targeting peptide TMTP1 (NVVRQ), to construct integrated nanoprobes for imaging and treatment. The constructed IR-DT nanoprobes, with its good tumor targeting ability, exhibit excellent imaging performance and significant therapeutic effects. With its powerful imaging capabilities, the IR-DT nanoprobes can achieve high-resolution fluorescence imaging of blood vessels, tumor lesions, and sentinel lymph nodes and could dynamically monitor the dissolution of carotid artery thrombi. The treatment results demonstrate that the nanoprobes possess significant advantages in both tumor-targeting capability and therapeutic efficacy. These findings suggest that it holds great potential to be developed into a theranostic nanoprobe for cervical cancer.
研究领域:
生物医学工程
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分子影像学
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癌症治疗
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF LUMINESCENCE
·
2026
·
IF 3.8
Chenchen Nie,Shanshu Yan,Gaoyuan Xing,Kaixin Ji,Xing Yang,Jianfeng Tang,Jiucun Chen,Yanan Zhao,Jie Hu,Jing Liu
Precise regulation of endogenous reactive oxygen species (ROS) is critical for maintaining physiological homeostasis, while dysregulated ROS levels are implicated in diverse pathologies. In vivo monitoring of this key signaling molecule represents an urgent priority, yet poses significant challenges due to the limitations of conventional ROS probes reliant on ultraviolet-visible excitation for high-fidelity biological imaging. To address this constraint, we engineered a luminescent nanoprobe by conjugating IR783 with upconversion nanoparticles (UCNPs), enabling H 2 O 2 detection via upconversion luminescence. The detection mechanism involves ROS-triggered cleavage of IR783, inducing nanostructure disassembly and subsequent restoration of upconversion luminescence. This design yields a concentration-dependent luminescence turn-on response, where upconversion luminescence intensity escalates proportionally with H 2 O 2 levels. The UCNPs-IR783 nanoprobe exhibits minimal cross-reactivity with biomolecules and low cytotoxicity, enabling effective visualization of both intrinsic and extrinsic reactive oxygen species within Hepa1-6 and RAW264.7 cellular models. Furthermore, investigations in murine subjects validate its applicability for ROS detection specifically within the tumor microenvironment.
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DOI
高影响因子
ACTA PHARMACOLOGICA SINICA
·
2021
·Vol. 43
·期 7
·1843-1856
·
IF 6.15
Huang Qiu-ju,Liao Guo-chao,Zhuang Xue-rong,Yang Meng-lan,Yao Jing-jing,Deng Jian-hua,Zhang Yan-min,Wang Ying,Qi Xiao-xiao,Pan Dong-feng,Guan Yang,Huang Zhi-ying,Zhang Feng-xue,Liu Zhong-qiu,Lu Lin-lin
Ras has long been viewed as a promising target for cancer therapy. Farnesylthiosalicylic acid (FTS), as the only Ras inhibitor has ever entered phase II clinical trials, has yielded disappointing results due to its strong hydrophobicity, poor tumor-targeting capacity, and low therapeutic efficiency. Thus, enhancing hydrophilicity and tumor-targeting capacity of FTS for improving its therapeutic efficacy is of great significance. In this study we conjugated FTS with a cancer-targeting small molecule dye IR783 and characterized the anticancer properties of the conjugate FTS-IR783. We showed that IR783 conjugation greatly improved the hydrophilicity, tumor-targeting and therapeutic potential of FTS. After a single oral administration in Balb/c mice, the relative bioavailability of FTS-IR783 was increased by 90.7% compared with FTS. We demonstrated that organic anion transporting polypeptide (OATP) and endocytosis synergistically drove the uptake of the FTS-IR783 conjugate in breast cancer MDA-MB-231 cells, resulting in superior tumor-targeting ability of the conjugate both in vitro and in vivo. We further revealed that FTS-IR783 conjugate could bind with and directly activate AMPK rather than affecting Ras, and subsequently regulate the TSC2/mTOR signaling pathway, thus achieving 2–10-fold increased anti-cancer therapeutic efficacy against 6 human breast cancer cell lines compared to FTS both in vivo and in vitro. Overall, our data highlights a promising approach for the modification of the anti-tumor drug FTS using IR783 and makes it possible to return FTS back to the clinic with a better efficacy.
研究领域:
药理学
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肿瘤学
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分子生物学
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DOI
PubMed
高影响因子
MATERIALS & DESIGN
·
2023
·
IF 8.4
Mingzhi Zhu,Pei Wang,Biaoqi Chen,Linrong Shi,Ruimin Long,Shibin Wang,Yuangang Liu
Such is the hypoxia in solid tumor that Ⅱ-type photodynamic therapy (PDT) has not yet achieved significantly satisfactory consequences. Despite the rapid advancement in nanotechnology-based PDT for alleviating the hypoxic tumor microenvironment, several challenges persist. These include inefficient passive oxygen-supply mechanisms, low stability of oxygen-delivery nanosystems, and the complexity of their modification processes. To address these issues, we developed integrative nanoformulations (HHI NPs) by sequentially inserting biomacromolecule hemoglobin (Hb) and IR783 (photosensitizer) into hollow mesoporous Prussian blue (HPB NPs) through a straightforward and gentle diffusion method. Intriguingly, the resulting hybrid nanocomposites based on hollow mesoporous structure provided stability of biomacromolecule Hb, ensuring active and efficient oxygen delivery. In these nanosystems, HHI NPs equipped with high oxygen-carrying Hb efficiently generated reactive oxygen species over HepG2 cells cultured in hypoxic condition under NIR irradiation. Additionally, HPB NPs served not only as nanocarriers but also as photothermal agents exhibiting excellent photothermal conversion effects. which were beneficial for photothermal therapy (PTT) of cancer. HHI NPs co-loaded with Hb and IR783 not only actively relieved the hypoxic TME through the stable protection of the hollow structure from HPB NPs, but also achieve the significant synergistic therapy by combining PDT and PTT for tumor treatment.
研究领域:
纳米技术
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癌症治疗
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生物医学工程
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药学
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产品关联
DOI
高影响因子
Nature Communications
·
2025
·Vol. 16
·期 1
·1-9
·
IF 15.7
Zhang Yiyan,Zhao Tianyu,Deng Yuming,Liu Xinyue,Zhang Xiaorong,Zhu Tong,Ågren Hans,Chen Guanying
Lead halide perovskites serve as an important class of photoelectrical materials in modern technological applications, such as light emitting diodes, photodetectors, and solar cells. However, the inability to respond to near infrared light poses a tight constraint on their performances. This study reports a class of broadband near infrared-responsive inorganic lead halide perovskite nanocrystals, which emit a palette of tunable upconversion luminescence via organic dye-lanthanide tandem sensitization. The coordination of dyes (IR783) to the surface of ytterbium-doped cesium lead halide nanocrystals entails an intense and broad spectral response range of near infrared light (600-860 nm). Sub-10 Wcm −2 light irradiance at 804 nm induced ultrabright exciton luminescence (tunable from 520 to 625 nm), about 27,500 folds brighter than the one without dye sensitization, with upconversion brightness reaching 3.22 M −1 cm −1 . Transient absorption spectra revealed an ultrafast triplet energy transfer process (9.28 × 10 8 s −1 ) from dyes to ytterbium dopants with near-unity efficiency (98.4%), followed by cooperative sensitization that excites delocalized excitons. These broadband near infrared-responsive inorganic perovskite nanocrystals have implications for applications ranging from solar cells to near infrared imaging and sensing.
研究领域:
材料科学
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光电子学
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纳米技术
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光子学
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能量转换
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产品关联
DOI
PubMed
高影响因子
BIOMATERIALS
·
2021
·
IF 12.479
Lu Lu,Kui Wang,Chuanchuan Lin,Weihu Yang,Qiaojian Duan,Ke Li,Kaiyong Cai
The blood−brain barrier (BBB) is one of the major limitations of glioblastoma therapy in the clinic. Nanodrugs have shown great potential for glioblastoma therapy. Herein, we purposefully developed a multicomponent self-assembly nanocomplex with very high drug loading content for curing orthotopic glioblastoma with synergistic chemo-photothermal therapy. The nanocomplex consisted of self-assembled pH-responsive nanodrugs derived from amino acid-conjugated camptothecin (CPT) and canine dyes (IR783) coated with peptide Angiopep-2-conjugated copolymer of Ang-PEG-g-PLL. Specifically, the carrier-free nanocomplex exhibited a high drug loading content (up to 62%), good biocompatibility , and effective glioma accumulation ability. Moreover, the nanocomplex displayed good stability and pH-responsive behavior ex vivo . Both in vitro and in vivo results revealed that the nanocomplex could effectively cross the BBB and target glioma cells. Furthermore, the combination of chemotherapy and photothermal therapy of the nanocomplex achieved a better therapeutic effect, longer survival time, and minimized toxic side effects in orthotopic glioblastoma tumor-bearing nude mice . Overall, we modified the chemotherapeutic drug CPT so that it could self-assemble with other molecules into nanoparticles , which providing an alternative for the preparation of the carrier-free nanodrugs. The results highlighted the potential of self-assembly nanodrugs as a novel platform for effective glioblastoma therapy.
研究领域:
纳米技术
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药学
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癌症治疗
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生物医学工程
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神经科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）