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MATERIALS & DESIGN · 2016 · IF 3.997

Fluorescent amphiphilic copolymer-based tumor theranostics for facile DOX-loading and tumor microenvironment-triggered release

Xu Jia,Kun Tian,Xubo Zhao,Tingting Zhou,Mingliang Pei,Peng Liu

Novel reduction/pH dual-stimuli responsive fluorescent amphiphilic copolymer PEG-Cys-P(DEAEMA-co-Rh6GEAm) with detachable poly(ethylene glycol) (PEG) corona through bio-reducible disulfide linkage and pendent cationic groups was synthesized via reversible addition-fragmentation chain transfer (RAFT) polymerization for tumor theranostic application. The doxorubicin (DOX)-loaded micelles could be easily fabricated via facile micellization in the presence of DOX in water, with a high drug-loading capacity (DLC) of 39.2%. They exhibited fast release ratio with the synergetic effect of reductive agent and pH in the simulated tumor micro-environment, while the leakage can be efficiently avoided in the physiological media. Furthermore, the fluorescence intensity of the copolymer possessed a reversibly transformation in different pH media, indicating the potential application for intracellular fluorescence imaging of tumors.

研究领域: 生物材料学 · 肿瘤治疗学 · 药剂学
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Materials Today Bio · 2023 · IF 8.2

Emulsifying Lipiodol with pH-Sensitive DOX@HmA nanoparticles for hepatocellular carcinoma TACE treatment eliminate metastasis

Qing Shi,Xingxing Zhang,Minmin Wu,Yuhan Xia,Yating Pan,Jialu Weng,Na Li,Xingjie Zan,Jinglin Xia

Lipiodol-based transcatheter arterial chemoembolization (TACE) is currently the predominant and first-line treatment option recommended by the global standard for unresectable hepatocellular carcinoma (HCC). However, the unstable emulsion of Lipiodol causes a substantial proportion of chemotherapy drugs to enter the circulation system, leading to poor accumulation in cancer tissues and unexpected side effects of chemotherapy drugs. Herein, we emulsified Lipiodol with a pH-sensitive drug delivery system assembled from hexahistidine and zinc ions (HmA) with a super-high loading capacity of doxorubicin (DOX) and a promising ability to penetrate bio-barriers for the effective treatment of HCC by TACE. In vitro tests showed that DOX@HmA was comparable to free DOX in killing HCC cells. Impressively, during the in vivo TACE treatment, the anti-tumor efficacy of DOX@HmA was significantly greater than that of free DOX, indicating that DOX@HmA increased the accumulation of DOX in tumor. Emulsifying Lipiodol with pH-sensitive DOX@HmA significantly inhibited cell regeneration and tumor angiogenesis and decreased the systemic side effects of chemotherapy, especially by suppressing pulmonary metastasis in liver VX2 tumors in rabbits by inhibiting epithelial–mesenchymal transition (EMT). Emulsifying tumor microenvironment-responsive drug delivery systems (DDSs) with Lipiodol could be a new strategy for clinical TACE chemotherapy with potentially enhanced HCC treatment.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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FITOTERAPIA · 2021 · IF 2.882

Stigmastane-type steroid saponins from the leaves of Vernonia amygdalina Del

Meng-Ling Zhao,Shu-Jun Shan,Rong Tao,Le-Tian Cui,Qiu-Rong Li,Jun Luo,Yi Li

Vernoramyosides A-F ( 1 – 6 ), six new Δ 7,9(11) stigmastane-type steroid saponins , along with four known analogues ( 7 – 10 ) were isolated from the leaves of Vernonia amygdalina Delile (Compositae). Their structures were determined by the combination of NMR, ECD and HR-ESI-MS data. These compounds all possessed highly oxidized side chain and a γ-lactam or α , β -unsaturated five-membered lactone ring. All isolates were screened for their activities in reversing resistance in MCF/DOX cells.

研究领域: 植物化学 · 药物化学 · 天然产物研究
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CARBON · 2017 · IF 6.337

A chemo/photo- co-therapeutic system for enhanced multidrug resistant cancer treatment using multifunctional mesoporous carbon nanoparticles coated with poly (curcumin-dithiodipropionic acid)

Fangzhou Li,Yun Wang,Zhipeng Zhang,Yuanyuan Shen,Shengrong Guo

It is still a tremendous challenge to combat multidrug resistant (MDR) cancer up to now, due to cancer resistance to chemotherapeutic agents. Herein, we put a new strategy for effective treatment of MDR cancer by improving chemotherapeutic efficacy via chemosensitizer in combination with phototherapy. Our previous work has demonstrated poly (ethylene glycol) - poly (curcumin-dithiodipropionic acid) (PEG-PCDA) is a good pre-chemosensitizer and enhances the sensitivity of MDR cancer cells to doxorubicin (DOX). In this study, we firstly synthesized mesoporous carbon nanoparticles (MCNs) having excellent photothermal and photodynamic effects, which could load a high dose of hydrophobic drug and presented pH -responsive drug release characteristics. On this basis, we developed a multifunctional MCN based drug delivery system to take chemo/photo- co-therapy against MDR human breast cancer MCF-7/ADR cells. The MCN based drug delivery system loaded 36.4% DOX and was coated with 23.2% PEG-PCDA, which could take photothermal and photodynamic effects under near-infrared (NIR) irradiation and trigger drug release by pH, glutathione (GSH), and/or NIR irradiation, termed as PEG-PCDA/DOX@MCNs. Once the PEG-PCDA/DOX@MCNs had been delivered into MCF-7/ADR cells, DOX release was triggered by degradation of PEG-PCDA via GSH and weak acidic pH, and in combination with MCN yielded photothermal and photodynamic effects under NIR irradiation, PEG-PCDA/DOX@MCNs could reduce premature drug release and then enhance anti-MDR cancer efficacy.

CAS / MDL: 108-95-2
研究领域: 肿瘤学 · 纳米医学 · 药物递送系统
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MATERIALS & DESIGN · 2023 · IF 8.4

Controllable growth of drug-encapsulated metal-organic framework (MOF) on porphyrinic MOF for PDT/chemo-combined therapy

Bei Liu,Zechao Liu,Xijian Lu,Peng Wu,Zhaogang Sun,Hongqian Chu,Hongshang Peng

To improve the therapeutic effect of tumors, developing well-defined hybrid metal-organic frameworks (MOFs) through MOF-on-MOF growth has attracted much attention. In this work, an in situ growth strategy was reported to assemble doxorubicin (DOX)-encapsulated zeolitic imidazolate frameworks (ZIF-8) on the surface of Zr(IV)-based porphyrinic MOFs. Such an approach offers a high controllability in the thickness of the ZIF-8 layer without any requirement of surface modifications on porphyrinic MOFs. Impressively, the acidic pH-response degradation of ZIF-8 promoted the release of DOX in the acidic tumor microenvironment. Upon light irradiation, porphyrinic MOFs can harvest photons to produce plentiful singlet oxygen, thus leading to amplified chemo/PDT therapeutic efficacy. This work paves the way to utilize the hybrid engineering of MOFs for synergistic cancer therapy.

CAS / MDL: 65-85-0 67-56-1
研究领域: 材料科学 · 癌症治疗 · 纳米医学
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COLLOIDS AND SURFACES B-BIOINTERFACES · 2017 · IF 3.887

Precise ratiometric loading of PTX and DOX based on redox-sensitive mixed micelles for cancer therapy

Dujuan Zhao,Jilian Wu,Chuanxiang Li,Huiyuan Zhang,Zhonghao Li,Yuxia Luan

PTX and DOX have different anticancer mechanisms. The combination of the two anticancer drugs could synergically enhance their anticancer effect, but simultaneously accompanied by severe side effects. In the present study, we constructed a mixed micelle system based on redox-sensitive mPEG-SS-PTX and mPEG-SS-DOX conjugate. The drug delivery system has a fixed and high drug loading content of 24.2% (PTX   ∼   14.8% and DOX   ∼   9.4%) with a precise ratio of PTX and DOX to realize the synchronized and controlled release. The mixed micelle has an average size of 93.3   nm with a narrow distribution, suitable for passive targeting to tumor tissues by the EPR effect. In vitro release profile and in vitro anticancer results show the mixed micelles have obvious redox-sensitive release properties in reducing environment and have a significant cytotoxicity to A549 and B16 cells. Importantly, in vivo study shows the mixed micelles have no obvious side effect on mice compared to free PTX/DOX samples during the treatment. Therefore, the constructed redox-sensitive mixed micelle is a promising drug delivery system for cancer therapy.

研究领域: 药学 · 癌症研究 · 纳米技术 · 药物递送系统
✓ 已验证 DOI PubMed 高影响因子
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Nano Today · 2026 · IF 10.7

Deep tumor penetration of supramolecular Fmoc-Glyco/ Fmoc-diphenylalanine-DOX drug loaded nanorods for targeted chemotherapy

Yan Zhang,Lingxin Peng,Baotong Ye,Guodong Lu,Sichen Li,Jingjing Zhou,Mihail Barboiu,Jinghua Chen

Nanoparticles (NPs) have been extensively investigated in modern cancer chemotherapy for their advantages in targeted drug delivery, enhanced efficacy and reduced toxicity. However, clinical evidence continues to indicate modest therapeutic efficacy of these nanomedicines, largely attributed to insufficient drug accumulation and poor tissue penetration in tumors. In the current study, we discovered that synergetic and precise control over nanoparticle shape and surface functionalization improves tumor penetration and enhances chemotherapy outcomes. Specifically, supramolecular nanospheres/nanorods self-assembled from scaffolding Fmoc-FF, hepatocyte targeting Fmoc-monosaccharides and the anti-tumor drug doxorubicin (DOX) have been associated via the synergetic control of their nanostructured morphologies and the surface presentation of bioactive signals. These pH-sensitive self-assembled nanoparticles enable controlled nanostructure shape and multivalent carbohydrate-functionalized surfaces, allowing activation in the acidic tumor microenvironment for triggered drug release. In vitro experiments demonstrated that the galactose-modified nanorod FGal 1–2 , measuring approximately 250 nm in length and of 25 nm in diameter, displayed the highest toxicity towards HepG2 cells and significantly enhanced cellular uptake. Additionally, nanorod FGal 1–2 demonstrated the deepest penetration (> 80 μm) in a 3D tumor spheroid model, surpassing the nanosphere FGal 1–1 and longer nanorod FGal 1–3 . Moreover, in vivo animal studies further revealed higher tumor accumulation of nanorod FGal 1–2 compared to the corresponding nanosphere, along with the strongest tumor inhibition, markedly reduced cardiotoxicity of DOX, and an 85% reduction in tumor volume. This work offers new insights into the design of nanoparticles with functional/morphological effects in their properties for advanced anti-tumor drug delivery.

CAS / MDL: 109-63-7 1122-58-3
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ENVIRONMENTAL RESEARCH · 2021 · IF 6.498

Enhanced photodegradation of doxycycline (DOX) in the sustainable NiFe2O4/MWCNTs/BiOI system under UV light irradiation

Xueqian Yan,Jin Qian,Xiangjun Pei,Lihong Zhou,Rui Ma,Mingkuan Zhang,Yufei Du,Linqin Bai

In this study, a magnetic NiFe 2 O 4 /MWCNTs/BiOI composite were fabricated and applied for enhanced and sustainable photocatalytic degradation of doxycycline (DOX) under UV light irradiation. The as-synthesized material was characterized by a series of techniques and its photocatalytic property was assessed via a couple of batch tests. With the pH at 3.0 and NiFe 2 O 4 /MWCNTs/BiOI loading of 1.5 g L −1 , the DOX degradation (at 45 mg L −1 ) efficiency could achieve 92.18% with the reaction rate constant k of 0.0072 min −1 . The high mineralization of DOX suggests the strong oxidation of both the parent pollutant and the intermediary products in the ternary catalyst system. DRS spectra indicated that compared with BiOI , the introduction of NiFe 2 O 4 and MWCNTs reduces the band gap energy of the NiFe 2 O 4 /MWCNTs/BiOI. The quenching test illustrates that h + , OH and O 2 − all functioned in the developed photocatalytic system, where O 2 − and h + play the dominant roles in DOX degradation. The more efficient electron-h + separation and more oxidizing species induced by UV light resulted in the significant improvement of DOX abatement in the developed coupling system compared with that on either BiOI or NiFe 2 O 4 /MWCNTs. The magnetic property of NiFe 2 O 4 /MWCNTs/BiOI enables its easy separation of the solid catalyst from the reaction solution and the sustainable application in the photocatalysis . Based on the intermediates of DOX decomposition identified by UPLC-MS, the possible degradation routes were proposed accordingly.

研究领域: 环境化学 · 材料科学 · 光催化 · 水污染治理 · 纳米复合材料 · 药物降解
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JOURNAL OF BIOMATERIALS SCIENCE-POLYMER EDITION · 2026 · IF 3.5

Sono-dynamic synergy of DOX-MBs achieves real-time imaging-guided drug delivery for breast cancer

Panhui Huang,Jieqiong Wang,Zhiyong Lu,Fei Yan,Wenjun Yu,Wei Li,Qiong Luo

Doxorubicin (DOX) is a widely used first-line chemotherapeutic drug with potent anti-tumor activity, yet severe off-target cardiotoxicity and hepatotoxicity severely restrict its clinical application. This study aimed to construct an ultrasound-responsive PLGA microbubble delivery system to realize tumor-specific controlled DOX release under low-intensity focused ultrasound (US), integrate real-time ultrasonic tumor imaging, and simultaneously reduce systemic side effects of free DOX. DOX-loaded PLGA microbubbles (DOX-MBs) were fabricated and evaluated for ultrasound contrast enhancement and US-triggered intracellular DOX release. In vitro and in vivo experiments were performed to evaluate tumor cell apoptosis induction, anti-metastatic capacity, as well as cardiac and hepatic toxic side effects of this theranostic platform. The DOX-MB system enabled real-time ultrasound visualization of tumor lesions. US exposure disrupted the microbubbles and promoted intracellular DOX release. Compared with free DOX, this platform significantly elevated tumor cell apoptosis, suppressed tumor distant metastasis, and effectively alleviated DOX-induced cardiotoxicity and hepatotoxicity in vivo. The developed US-activated DOX-loaded PLGA microbubbles integrate diagnostic ultrasound imaging and tumor-targeted chemotherapy with reduced organ toxicity. This work provides a facile and novel design strategy for imaging-guided, ultrasound-triggered tumor theranostic microplatforms.

✓ 已验证 DOI 高影响因子
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Frontiers in Pharmacology · 2025 · IF 4.8

EGCG and DOX dual-drug-loaded enzyme-responsive nanovesicles boost mitochondrial-mediated ICD for improved immunotherapy

Mengxue Zhou,Ying Wang,Hongchun Cui,Huan Geng,Lifo Ruan,Yanni Zhao,Chuang Zhou,Weidong Dai,Jun Chen,Jizhong Yu,Haipeng Lv,Zhi Lin

Enhancing cancer immunotherapy using methods that induce immunogenic cell death (ICD) can significantly improve its effectiveness and profoundly influence its role as a highly efficient cancer treatment strategy. However, the limited penetration of cytotoxic T cells into tumors, owing to dense tumor fibrosis, remains a significant barrier to immunotherapy. A tumor microenvironment-sensitive intelligent dual-drug delivery system was developed to simultaneously deliver epigallocatechin-3-gallate (EGCG) and doxorubicin (DOX) to mitochondria. EGCG enhanced the mitochondria-targeted action of DOX and increased damage to the mitochondrial electron transport chain which facilitated capturing electrons in the mitochondrial matrix of DOX. Subsequently, DOX molecules form a semiquinone intermediate and electrons are transferred to oxygen to generate reactive oxygen species (ROS) that induce mitochondrial apoptosis. These results indicate that EGCG amplifies the combined effects of chemo/chemodynamic therapy of DOX, demonstrating a pronounced synergistic ICD effect that recruits CD8+ T cells to the tumor microenvironment (TME). In addition, EGCG promotes T-cell infiltration into tumor tissues by inhibiting the transforming growth factor-β signaling pathway, thereby significantly enhancing antitumor efficacy. This study advances the efficacy of immunotherapy through bidirectional synergy, which not only enhances intrinsic tumor immunogenicity but also overcomes the extrinsic physical barriers of tumors, providing a new direction for the development of broadly applicable immunotherapies.

研究领域: 肿瘤学 · 药理学 · 生物医学工程 · 免疫学
✓ 已验证 DOI PubMed 高影响因子
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SOFT MATERIALS · 2019 · IF 0.973

Folic acid-modified β-cyclodextrin nanoparticles as drug delivery to load DOX for liver cancer therapeutics

Wenbo Fan,Yuedi Xu,Zheng Li,Qiang Li

To get the safe and effective therapy for liver cancer, multifunctional nanoparticulate systems with therapeutic efficacy for biomedical application are progressing quite rapidly. The aim of the present research is to determine the potential of doxorubicin (DOX)-loaded folic acid–polyethylene glycol–β-cyclodextrin (FA–PEG–β-CD) nanoparticles (NPs) as drug-delivery system for liver cancer therapy. The targeting delivery of FA–PEG–β-CD was synthesized from FA and β-CD with PEG as a linker, which then loaded antitumor drug DOX to get the FA–PEG–β-CD/DOX NPs. The physicochemical characterizations including flourier transform infrared, 1H nuclear magnetic resonance, transmission electron microscope and dynamic light scattering, drug-loading content, drug encapsulation efficiency, blood compatibility, and in-vitro drug release were investigated. Finally, the in-vitro antitumor activity was estimated by HepG2 cells. The size of FA–PEG–β-CD NPs was about 20–80 nm, while FA–PEG–β-CD/DOX NPs was 30–60 nm. And the FA–PEG–β-CD/DOX NPs have drug-loading efficiency (11.9%) and encapsulation efficiency (95.2%). The in-vitro drug release results showed that the FA–PEG–β-CD NPs could not merely improve the solubility of hydrophobic drugs but also control the drug release. Blood compatibility assays revealed that DOX-loaded NPs did not induce blood hemolysis. In summary, the drug delivery of FA–PEG–β-CD NPs is suitable to carry the drug to the tumor tissues and release the drug effectively, and FA–PEG–β-CD/DOX NPs may be a potential platform for improving the treatment of liver cancer.

研究领域: 药剂学 · 肿瘤学 · 生物医学工程
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Polymer Chemistry · 2016 ·Vol. 7 ·期 9 ·1719-1729 · IF 5.687

Preparation of pH and redox dual-sensitive core crosslinked micelles for overcoming drug resistance of DOX

Xiao-Qing Yi,Quan Zhang,Dan Zhao,Jia-Qi Xu,Zhen-Lin Zhong,Ren-Xi Zhuo,Feng Li

In this paper, we first synthesized an amphiphilic block copolymer poly(ethylene glycol)-poly(2,4,6-trimethoxybenzylidene-pentaerythritol carbonate-co-5-methyl-5-propargyl-1,3-dioxan-2-one), i.e., PEG-P(TMBPEC-co-MPMC), with pendant reactive alkynyl groups as well as pH-sensitive acetal groups. Next, core crosslinked (CCL) micelles were prepared by the introduction of 1,6-diazidohexane and bis(azidoethyl)disulfide into micelles via azide–alkyne click chemistry, which were denoted as CCL/CC and CCL/SS, respectively. The CCL micelles had superior stability and drug loading efficiency to the uncrosslinked (UCL) micelles. In comparison with free DOX, drug-loaded CCL micelles exhibited lower cell viability in MCF-7/ADR cells due to their “stealth” endocytosis effect that might be beneficial for overcoming delivery barriers of drug resistance. More interestingly, as compared with CCL/CC micelles, CCL/SS micelles were found to further enhance cytotoxicity in MCF-7/ADR cells because of their better on-demand drug release capability of pH and redox dual-sensitive CCL/SS micelles. These results suggest that the self-assembled pH and redox dual-sensitive CCL/SS micelles have promising applications to overcome multi-drug resistance in tumor treatments.

研究领域: 药学 · 纳米技术 · 药物递送系统 · 癌症研究
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