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JOURNAL OF CANCER RESEARCH AND CLINICAL ONCOLOGY · 2020 ·Vol. 146 ·期 4 ·875-882 · IF 3.656

Precise therapeutic effect of self-assembling gold nanocluster–PTEN complexes on an orthotropic model of liver cancer

Wang Maonan,Wang Lishan,Feng Huan,Jiang Hui,Zhou Jiahua,Wang Xuemei

Purpose Presently, liver cancer is still one of the malignant tumors with high mortality. As far as the treatment of liver cancer is concerned, the most effective method is still liver transplantation. But every year, many liver cancer patients die from the lack of a proper liver transplant, or from waiting for a liver transplant. Therefore, it is very important to find new and effective treatment for patients with liver cancer. Methods Herein, the cell model and the orthotropic liver tumor mice model have been performed to verify the results of our treatment. We found that the in situ synthesized gold nanocluster–PTEN (GNC–PTEN) complexes can effectively target and realize the fluorescence imaging of the liver tumor. Results GNC–PTEN complexes could inhibit the proliferation, invasion, and metastasis of liver cancer cells. And the results also showed that GNC–PTEN complexes could be well targeted liver tumor at 6 h and the liver tumor in mice group treated with GNC–PTEN complexes almost disappeared. Conclusion This is a simply and effectively method to realize liver cancer imaging and inhibition. This may raise the possibility for the accurate image/diagnosis and simultaneously efficient treatment of liver cancer in the relevant clinic application.

CAS / MDL: 16903-35-8
研究领域: 肿瘤学 · 分子生物学 · 纳米医学
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ACS Applied Materials & Interfaces · 2019 · IF 8.456

Promoting Early Diagnosis and Precise Therapy of Hepatocellular Carcinoma by Glypican-3-Targeted Synergistic Chemo-Photothermal Theranostics

Weiwei Mu,Dandan Jiang,Shengjun Mu,Shuang Liang,Yongjun Liu,Na Zhang

The specific-targeting approach could promote the specificity of diagnosis and the accuracy of cancer treatment. The choice of a specific-targeting receptor is the key step in this approach. Glypican-3 (GPC3) is an oncofetal proteoglycan anchored on the cell membrane. It is overexpressed even in the early stage of hepatocellular carcinoma (HCC), whereas it shows almost no expression in the healthy adult liver. Therefore, GPC3 may be applied as a specific-targeting receptor for HCC theranostics. In this study, a GPC3 specific-targeting theranostics nanodevice, GPC3 targeting peptide (named G12)-modified liposomes co-loaded with sorafenib (SF) and IR780 iodide (IR780), was developed (GSI-Lip), which aims to realize early diagnosis and precise chemo-photothermal therapy of HCC. SF was the first-line chemotherapy drug for the treatment of HCC. IR780 was used for photothermal therapy and near-infrared fluorescence imaging. The evaluation of early diagnosis verified that early-stage tumors (3.45 ± 0.98 mm3, 2 days after 5 × 105 H22 cells’ inoculation in mice) could be clearly detected using GSI-Lip, which was significantly more sensitive than folic acid-modified liposomes (p < 0.01, 32.90 ± 10.01 mm3, 4 days after 1 × 106 H22 cells’ inoculation in mice). The study of the endocytic pathway indicated that specific G12/GPC3 recognition may induce caveolae-mediated endocytosis of GSI-Lip. Notably, the accumulation of GSI-Lip in tumors was significantly increased compared with that observed with folic acid-modified liposomes (p < 0.01). Specific-targeting endowed the precise antitumor effect of GSI-Lip. GSI-Lip showed a higher antitumor efficacy in comparison with folic acid-modified liposomes (inhibition rate: 90.52% vs 84.22%, respectively; p < 0.01). During a period of 21 days, the synergistic chemo-photothermal therapy (GSI-Lip + laser) exhibited a better antitumor effect versus GSI-Lip without laser (inhibition rate: 94.93% vs 90.52%, respectively; p < 0.01). Overall, GPC3-targeted GSI-Lip promoted the sensitivity and specificity of HCC early diagnosis and achieved synergistic efficacy of chemo-photothermal theranostics, which has potential clinical applications. Furthermore, the present study revealed that a more specific-targeting ligand could further improve the efficacy of theranostics against HCC.

研究领域: 肿瘤学 · 分子生物学 · 药剂学
✓ 已验证 DOI PubMed 高影响因子
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CARBOHYDRATE POLYMERS · 2016 · IF 4.219

Multi-functionalized hyaluronic acid nanogels crosslinked with carbon dots as dual receptor-mediated targeting tumor theranostics

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

Hyaluronic acid (HA)-based theranostic nanogels were designed for the tumor diagnosis and chemotherapy, by crosslinking the folate-terminated poly(ethylene glycol) modified hyaluronic acid (FA-PEG-HA) with carbon dots (CDs) for the first time. Due to the extraordinary fluorescence property of the integrated CDs, the theranostic nanogels could be used for the real-time and noninvasive location tracking to cancer cells. HA could load Doxorubicin (DOX) via electrostatic interaction with a drug-loading capacity (DLC) of 32.5%. The nanogels possessed an ideal release of DOX in the weak acid environment, while it was restrained in the neutral media, demonstrating the pH-responsive controlled release behavior. The cytotoxicity and cellular uptake results clearly illustrated that most DOX was released and accumulated in the cell nuclei and killed the cancer cells efficaciously, due to their dual receptor-mediated targeting characteristics.

CAS / MDL: 6066-82-6
研究领域: 生物材料学 · 肿瘤学 · 药剂学
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International Journal of Pharmaceutics-X · 2025 · IF 6.4

An aptamer-conjugated mesoporous polydopamine formulation for synergistic targeted and photothermal therapy of hepatocellular carcinoma

Yue Yang,Chonggao Wang,Shiwei Liu,Yewei Zhang

This study aimed to create multifunctional nanoparticles (NPs), specifically [email protected] (AMLC), for the purpose of developing effective strategies for treating hepatocellular carcinoma (HCC) through targeted therapy and photothermal therapy (PTT). The study involved synthesizing mesoporous polydopamine (MPDA)-NPs, loading lenvatinib (Len) and Cy5.5 via incubation, and modifying AS1411 aptamer onto MPDA via a covalent chemical reaction. The NPs were characterized using techniques such as ultra-micro spectrophotometry, Fourier transform infrared spectroscopy, and transmission electron microscopy. Target-specific uptake and cell-killing assays were utilized to evaluate AMLC-mediated synergistic therapy while using Western blotting and immunofluorescence to confirm the underlying mechanism. Consequently, the nanoparticles (NPs) were successfully synthesized, demonstrating excellent solvent solubility and stability, with controlled drug release achieved in acidic environments (maximum release efficiency≈80 %). In vitro and in vivo studies revealed that these NPs could more effectively target hepatocellular carcinoma (HCC) cells, enhancing the targeting capability of lenvatinib. Under near-infrared (NIR) laser irradiation, the targeted photothermal therapy (PTT) exhibited significantly improved anticancer efficacy, with AMCL+PTT treatment resulting in up to 76 % tumor volume reduction‌ ( P  < 0.01). The study demonstrates that AMLC, a multifunctional nano-delivery system, significantly enhances Lenvatinib's tumor-targeting capacity while exhibiting excellent biocompatibility. Combined with photothermal therapy (PTT), it demonstrates potent antitumor efficacy, showing promising clinical translation potential for hepatocellular carcinoma (HCC) therapy.

研究领域: 肿瘤学 · 纳米医学 · 药理学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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ACS Applied Materials & Interfaces · 2025 · IF 8.2

Intelligent Hierarchical Targeting Near-Infrared Persistent Luminescence Nanosystem for Improved Nuclear Delivery and Simultaneous Visualization/Therapy of EBV-Associated Cancer

Yunfei Zhu,Ya Wen,Yanping Xie,Guangfeng Chen,Siqi Hu,Yue Wu,Lijun Jiang,Bruno Viana,Cyrille Richard,Ka-Leung Wong,Ju Jiao,Jing Wang,Rui Zou

Epstein–Barr nuclear antigen 1 (EBNA1), a sequence-specific DNA binding protein of Epstein–Barr virus (EBV), is essential for viral genome replication and maintenance and is therefore an attractive target for the therapeutic intervention of EBV-associated cancers. Several EBNA1-specific inhibitors have demonstrated the ability to block EBNA1 function in vitro, but practical delivery strategies for these inhibitors in vivo are still lacking. Here, we report an intelligent hierarchical targeting theranostic nanosystem (denoted as mZGOCS@MnO2–P5) that integrates an azide (N3) terminal dual-targeting peptide (N3–P5), a tumor microenvironment-responsive degradable MnO2 nanosheet, and a mesoporous ZnGa2O4:Cr3+, Sn4+ near-infrared persistent luminescence (NIR-PL) nanosphere (mZGOCS). In our design, mZGOCS@MnO2–P5 enables primarily targeting of the EBV-specific oncoprotein LMP1 (an EBV-encoded transmembrane protein) via the LMP1 targeting motif within P5. Once internalized into cells, the MnO2 nanosheet would be degraded in the acidic and reducing tumor microenvironment, simultaneously releasing P5 and recovering the NIR-PL of ZnGa2O4:Cr3+, Sn4+ initially quenched by the MnO2 nanosheet, thereby providing an autofluorescence interference-free NIR-PL imaging signal for monitoring the delivery efficacy of P5. The released P5 can secondarily target EBNA1 via the EBNA1 binding motif, blocking its function and thus inhibiting the growth of EBV-positive tumors. The feasibility of our developed hierarchical targeting theranostic nanosystem is well demonstrated both in vitro and in vivo, highlighting the huge translational potential of mZGOCS@MnO2–P5 in EBV-associated cancer therapy.

研究领域: 肿瘤学 · 病毒学 · 纳米医学
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Cancer Nanotechnology · 2025 ·Vol. 16 ·期 1 ·1-20 · IF 4.8

Nanocomplex hyaluronic acid/ganciclovir@ZIF-8 for ganciclovir efficient delivery and targeted anti-KSHV treatment

Li Fangling,Liu Chengjing,Gu Wenyi,Xu Qianhe,Li Dongmei,Cao Dongdong,Liu Zhiyong

Kaposi's sarcoma-associated herpesvirus (KSHV) infection can cause a variety of tumors and is one of the leading causes of death in acquired immune deficiency syndrome (AIDS) patients. As a small molecule antiviral drug, ganciclovir (GCV) can be used for anti-KSHV treatment. However, GCV has non-specific action and toxic side effects in vivo, and how to make it safer and more effective against KSHV is still a great challenge. By encapsulating GCV into metal–organic skeleton material zeolitic imidazolate framework-8 (ZIF-8) and further modification of hyaluronic acid (HA), the nanomedical delivery system of GCV (HA/GCV@ZIF-8) has been developed for efficient GCV delivery and targeted anti-KSHV treatment. The modification of HA leads to the targeted binding of the nanocomplex with the overexpressed CD44 receptors in tumor cell membranes, resulting in the increased accumulation and cellular uptake of GCV. Exploiting the decomposition property of ZIF-8 under acidic conditions, the nanocomplex exhibits pH-responsive drug release in slightly acidic tumor environment. In addition, HA/GCV@ZIF-8 not only suppresses expression of KSHV pathogenic genes with less drug dose, but also inhibits the ability of cell proliferation and migration. In vivo anti-tumor results showed that HA/GCV@ZIF-8 accumulated in tumor cells and effectively inhibited tumor growth. The results open a gate for the targeted anti-KSHV treatment. Graphical

研究领域: 医学 · 药学 · 病毒学
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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2017 · IF 3.649

Glycyrrhetinic acid-modified TPGS polymeric micelles for hepatocellular carcinoma-targeted therapy

Xiumei Zhu,Altansukh Tsend-Ayush,Zhongyue Yuan,Jing Wen,Jiaxin Cai,Shifu Luo,Jianxu Yao,Junxing Bian,Linfang Yin,Jianping Zhou,Jing Yao

In this study, glycyrrhetinic acid (GA)-modified D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) polymeric micelles (TGA PMs) were developed for the delivery of etoposide (ETO) to hepatoma cells. GA was incorporated as a ligand because of its high affinity to the hepatocytes, while TPGS functioned as a P-gp inhibitor to reverse multidrug resistance. ETO-loaded TGA PMs (ETO-TGA PMs) displayed a mean particle size of 133.6   ±   1.2   nm with a low poly-dispersity index (0.224   ±   0.013) and negative zeta potential (−16.30   mV). The drug loading and entrapment efficiency of ETO-TGA PMs were 10.4% and 79.8%, respectively. ETO-TGA PMs also exhibited faster drug release behavior at pH 5.8 and relatively stable drug release at pH 7.4. Confocal laser scanning microscope (CLSM) observations and in vivo imaging studies revealed that TGA PMs displayed higher cellular uptake and selective accumulation at the tumor site, indicating good tumor targetability. Furthermore, ETO-TGA PMs displayed significant cytotoxicity towards HepG2 cells and higher anti-tumor efficacy (75.96%), compared to the control group. This could be due to TGA-mediated targeted drug delivery to the hepatocytes as well as P-gp inhibition. These findings suggest that TGA PMs have the potential to be used as a targeted drug delivery system for hepatic cancer therapy.

研究领域: 药剂学 · 肿瘤学 · 生物医学工程
✓ 已验证 DOI PubMed 高影响因子
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BIOMEDICINE & PHARMACOTHERAPY · 2018 · IF 3.457

RGD peptide-modified, paclitaxel prodrug-based, dual-drugs loaded, and redox-sensitive lipid-polymer nanoparticles for the enhanced lung cancer therapy

Guowen Wang,Zuyi Wang,Chuankui Li,Guixin Duan,Kangwu Wang,Qicai Li,Tao Tao

One approach to improve the targeted therapeutic efficiency of lung cancer is to deliver drugs using nano-scaled systems. In this study, RGD peptide-modified, paclitaxel (PTX) prodrug-based, dual-drugs loaded, and redox-sensitive lipid-polymer nanoparticles were developed and the in vitro and in vivo antitumor efficiency was evaluated in lung cancer cells and tumor bearing animal models. RGD-modified PTX and cisplatin (CDDP) loaded LPNs (RGD-ss-PTX/CDDP LPNs) have sizes around 190 nm, and zeta potentials of −35 mV. The half-maximal inhibitory concentration (IC50) values were 26.7 and 75.3 μg/mL for drugs loaded LPNs and free drugs combination, which indicates significantly higher antitumor activity of LPNs than free drugs. RGD-ss-PTX/CDDP LPNs also exhibited the best antitumor efficiency in vivo , which inhibited the tumor size of mice from 1486 mm 3 to 263 mm 3 . The results illustrated that the system could successfully load drugs and achieve synergistic combination lung cancer treatment efficiency with lower systemic toxicity compared with free drugs counterparts. The resulting system could be facilitated as a promising targeted nanomedicine for the treatment of lung cancer.

研究领域: 药学 · 肿瘤学 · 生物医学工程
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Frontiers in Molecular Biosciences · 2022 · IF 6.113

Aspirin Repurposing in Folate-Decorated Nanoparticles: Another Way to Target Breast Cancer

Kanwal Fariha,Ma Mingming,Rehman Muhammad Fayyaz ur,Khan Fahim-ullah,Elizur Shai E.,Batool Aima Iram,Wang Chi Chiu,Tabassum Tahira,Lu Changrui,Wang Yao

Breast cancer affects more than 1 million women per year worldwide. Through this study, we developed a nanoparticle-based drug delivery system to target breast cancer cells. Aspirin has been found to inhibit thromboembolic diseases with its tumor-preventing activity. As a consequence, it relieves disease symptoms and severity. Here, mesoporous silica nanoparticles (MNPs) have been used to deliver aspirin to the tumor location. MNP-based aspirin in folic acid (F)-conjugated polydopamine (MNP-Asp-PD-PG-F) vehicles are prepared for targeted breast cancer therapy. The vehicle hinges on MNP altered with polymer polyethylene glycol (PG), polydopamine (PD), and F. The delivery vehicle was studied for in vitro drug release, cytotoxicity, and breast cancer cell proliferation. F-conjugated drug delivery vehicles let MNPs achieve an elevated targeting efficacy, ideal for cancer therapy. It was also observed that compared to free aspirin, our drug delivery system (MNP-Asp-PD-PG-F) has a higher cytotoxic and antiproliferative effect on breast cancer cells. The drug delivery system can be proposed as a targeted breast cancer therapy that could be further focused on other targeted cancer therapies. Delivering aspirin by the PD-PG-F system on the tumor sites promises a therapeutic potential for breast cancer treatment.

研究领域: 药学 · 肿瘤学 · 纳米医学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF CONTROLLED RELEASE · 2022 · IF 11.467

Bio-inspired engineered ferritin-albumin nanocomplexes for targeted ferroptosis therapy

Chencheng Xue,Hui Zhang,Xuan Wang,Haoyu Du,Lu Lu,Yang Fei,Yanan Li,Yuchen Zhang,Menghuan Li,Zhong Luo

Nanotechnology-enabled ferroptosis therapy is an emerging paradigm for tumor treatment, but amplifying ferroptotic damage in tumor cells in a safe and selective manner is still challenging, which severely hinders its clinical translation. In this study, we constructed a bio-inspired protein nanocomplex based on natural-occurring bovine serum albumin (BSA) and ferritin for efficient tumor elimination via cooperatively enhanced ferroptosis therapy. The long-circulating BSA molecules provided multiple anchoring points for the efficient loading of the GPX4-inhibiting ferroptosis inducer (1S, 3R) RAS-selective lethal 3 (RSL3), which was further complexed with ferritin via acidity-responsive glutaraldehyde linkers. The ferritin moieties may not only bind to transferrin receptor 1 overexpressed on tumor cell membrane for targeted endocytic uptake but also be degraded in lysosomes to induce iron overload, which could substantially promote the lipid peroxidation in tumor cells and cooperate with the glutathione peroxidase 4 (GPX4)-inhibiting capability of RSL3 to induce pronounced ferroptosis. The in vitro and in vivo results collectively demonstrated that the albumin-ferritin-based nanocomplex could present superior antitumor effects with no obvious adverse effects, which may open new avenues for the clinical translation of ferroptosis-dependent therapeutic modalities.

研究领域: 肿瘤学 · 纳米医学 · 生物材料学
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JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY · 2014 ·Vol. 302 ·期 1 ·123-130 · IF 1.415

Preparation and the biodistribution study of [131I]-5,10,15,20-tetrakis(4-hydroxyphenyl)porphyrin and 5-(4-aminophenyl)-10,15,20-triphenylporphyrin

Sun Zhi-Zhong,Wei Hong-Yuan,Wang Guan-Quan,Zhou Zhi-Jun,He Jia-Heng,Wang Jing,Luo Shun-Zhong

[ 131 I]-5,10,15,20-tetrakis(4-hydroxyphenyl)porphyrin and [ 131 I]-5-(4-aminophenyl)-10,15,20-triphenylporphyrin ( 131 I-TPPOH and 131 I-TPPNH 2 ) were prepared and their biodistribution properties were evaluated in normal Kunming (KM) mice and SMMC-7721 tumor-bearing BALB/c mice. The optimized labeling yields were 98 and 96 % for 131 I-TPPOH and 131 I-TPPNH 2 , respectively. They were stable in vitro saline and in vivo. Both compounds had a specific affinity to liver and lung, and mainly metabolized through liver. They showed a time-dependent accumulation and retainable characteristics in SMMC-7721 tumor. These results supported their potential value for targeted tumor therapy agents.

研究领域: 放射医学 · 肿瘤学 · 药理学
✓ 已验证 DOI 高影响因子
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JOURNAL OF BIOTECHNOLOGY · 2025 · IF 3.9

Functional nucleic acid-powered hybrid nanocarriers for synchronized targeted delivery of dual-solubility therapeutics

Xin Liu,Mengqiu Sun,Lu Dai,Yusheng Li,Rui Song,Hong Bian,Hao Zhang

Combination chemotherapy presents a promising approach to overcome multidrug resistance in cancer treatment. However, conventional delivery systems struggle to achieve synchronized co-delivery of hydrophilic and hydrophobic therapeutics with tumor-specific targeting and controlled release. Here, we developed a multifunctional nanocarrier integrating poly (lactic-co-glycolic acid) nanoparticles with polydopamine and programmable nucleic acids. Within this system, the hydrophobic core encapsulates lipophilic drugs, while the surface nucleic acid architecture enables hydrophilic drug loading via molecular intercalation. Furthermore, tumor-targeting aptamers guide selective cellular uptake, and a tumor microenvironment-responsive mechanism ensures spatiotemporally controlled drug release. As demonstrated experimentally, this unified platform demonstrates promising antitumor activity with potential advantages in drug delivery efficiency. By combining targeted delivery, differential drug loading, and stimuli-triggered release, the design establishes a modular framework for precision combination therapies, thereby advancing adaptable nanomedicine in oncology.

研究领域: 肿瘤学 · 生物医学工程 · 药理学 · 分子生物学
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