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JOURNAL OF NANOPARTICLE RESEARCH · 2018 ·Vol. 20 ·期 11 ·1-10 · IF 2.127

Aptamer-conjugated multi-walled carbon nanotubes as a new targeted ultrasound contrast agent for the diagnosis of prostate cancer

Gu Fenfen,Hu Chuling,Xia Qingming,Gong Chunai,Gao Shen,Chen Zhongjian

Early diagnosis is primarily important for the therapeutic and prognostic outcomes of malignancies including prostate cancer (PCa). However, the visuality and veracity of ultrasound imaging for the diagnosis and prognostic prediction of PCa remains poor at present. In this study, we developed a new nanoultrasound contrast agent by modifying multi-walled carbon nanotubes (MWCNTs) with polyethylene glycol (PEG) and anti-PSMA aptamer. The result showed that the modified MWCNTs offered better visuality and veracity and were able to target PCa cells more effectively as compared with the traditional contrast agent. The zeta potential was about − 38 mv. The length of this contrast agent was about 400 nm and the diameter of it was about 30 nm. The zeta potential, TEM, and FT-IR all proved the successful preparation of the agent. The vitro cytological study revealed good cell uptake and biocompatibility of the new contrast agent. The minimum detection concentration in vitro is 10 μg/ml. The earliest stage of the detection was under the parameters of frequency = 6.0 MHz and medical index = 0.06. Both in vitro and in vivo ultrasound imaging demonstrated that the new nanoultrasound contrast agent had a good development effect, distribution, and metabolism, and may prove to be a good targeted ultrasound contrast agent, especially for PCa.

研究领域: 医学影像 · 纳米技术 · 癌症诊断 · 生物医学工程
✓ 已验证 DOI PubMed 高影响因子
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Journal of Biophotonics · 2021 ·Vol. 14 ·期 11 ·e202100117 · IF 3.207

Near-infrared emissive polymer-coated IR-820 nanoparticles assisted photothermal therapy for cervical cancer cells

Lijun Zhu,Jianjun Chen,Ting Yan,Gulinigaer Alimu,Xueliang Zhang,Shuang Chen,Mutalifu Aimaiti,Rong Ma,Nuernisha Alifu

Photothermal therapy (PTT) has attracted wide attention due to its noninvasiveness and its thermal ablation ability. As photothermal agents are crucial factor in PTT, those with the characteristics of biocompatibility, non-toxicity and high photothermal stability have attracted great interest. In this work, new indocyanine green (IR-820) was utilized as a photothermal agent and near-infrared (NIR) fluorescence imaging nanoprobe. To improve the biocompatibility, poly(styrene-co-maleic anhydride) (PSMA) was utilized to encapsulate the IR-820 molecules to form novel IR-820@PSMA nanoparticles (NPs). Then, the optical and thermal properties of IR-820@PSMA NPs were studied in detail. The IR-820@PSMA NPs showed excellent photothermal stability and biocompatibility. The cellular uptaking ability of the IR-820@PSMA NPs was further confirmed in HeLa cells by the NIR fluorescent confocal microscopic imaging technique. The IR-820@PSMA NPs assisted PTT of living HeLa cells was conducted under 793 nm laser excitation, and a high PTT efficiency of 73.3% was obtained.

CAS / MDL: 109-99-9 172616-80-7
研究领域: 生物医学工程 · 肿瘤学 · 材料科学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF POWER SOURCES · 2024 · IF 8.1

Voltage-assisted 3D printing of polymer composite dielectric films with low energy loss and high energy storage density

Jian Wang,Biyun Peng,Yifei Zhang,Honghong Gong,Baohui Wang,Wentao Wu,Lijun He,Sen Liang,Yunchuan Xie

PVDF-based polymers have garnered significant attention in the field of high-power density electrostatic capacitors due to their exceptional dielectric strength . However, their practical applications are constrained by low charge-discharge efficiency ( η ) and energy storage density ( U e ), which stem from high ferroelectric relaxation and low breakdown strength ( E b ). Here, a hydrogenated glassy polymer poly(styrene-methyl methacrylate-methylallyl alcohol) (PSMA) is designed and synthesized to be homogeneously distributed in PVDF through voltage-assisted 3D printing-hot pressing, resulting in a flexible composite film . The findings demonstrate that PSMA, rich in hydrogen bonds and high modulus strength, effectively mitigates the ferroelectric phase transition of PVDF to enhance η . Additionally, the voltage-assisted 3D printing process induces an entropy gain mechanism, facilitating the uniform distribution of the two phases and enhancing the interfacial properties for enhancing E b . Remarkably, the study achieves prominent growth in energy storage performance, with U e and η reaching 18.1 J/cm 3 and 80 % at 525 MV/m, respectively. These remarkable results highlight the potential of 3D printing technology in enhancing the energy storage performance of PVDF-based dielectrics.

研究领域: 材料科学 · 电气工程
✓ 已验证 DOI 高影响因子
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Exploration · 2026 · IF 30.4

PSMA-Targeting Macrophage Membrane-Coated Nanoparticles for Precision Diagnosis and Combination Therapy of Prostate Cancer

Keying Zhang,Bo Gao,Jingwei Wang,Yu Li,Chao Xu,Fa Yang,Shaojie Liu,Hongji Li,Chao Zhang,Xiangliang Meng,Zhaokun Shi,Rui Zhang,Ruili Zhang,Zhongliang Wang,Weihong Wen,Qiang Zhang,Yuankang Zou,Donghui Han,Huijie Bian,Weijun Qin

Prostate cancer (PCa) is the most frequently diagnosed cancer in males. Advanced PCa is invasive and may spread rapidly. Current strategies could not fulfill the requirement for clinical application; thus, novel therapeutic strategies are still urgently needed. Nanoparticles are a promising strategy for targeted drug delivery and cancer treatment; however, the strong exogeneity and weak targeting limit their further application. Here, we developed a novel macrophage membrane-coated nanoparticle that has transmembrane-expressed gy-1, a single-chain antibody fragment (scFv) against prostate-specific membrane antigen (PSMA), to endow the immune evasion and targeting property, which we named P-MMCNPs. The Fe 3 O 4 @Au nanoparticles were used as the core of P-MMCNPs, which confer P-MMCNPs with the properties of multimodal imaging and photothermal therapy (PTT). Anti-tumor cytotoxic drug maytansine (DM1) was loaded into the nanoparticles to obtain cytotoxicity. P-MMCNPs were shown to have immune evasion capacity and prolonged circulation time and can be specifically distributed in PSMA-positive tumors, thus enabling targeted imaging and targeted drug delivery. The macrophage membrane-coated nanoparticles combined to inhibit tumor growth in vivo when loaded with DM1 and treated with PTT. Additionally, we found that P-MMCNPs alone could inhibit tumor growth, which may be caused by cytokine neutralization by the macrophage membrane. Our work demonstrates that the innovative P-MMCNPs serve as a versatile platform. This platform improves PCa-targeted diagnostic and therapeutic efficacy while avoiding side effects. Moreover, it holds promise for expanding into the diagnosis and treatment of other diseases, with potential for clinical translation. Additionally, it offers novel insights into nanomedicine-based combination therapy.

CAS / MDL: 16961-25-4
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International Journal of Nanomedicine · 2023 · IF 8

In vitro and in vivo Evaluation of Folic Acid Modified DOX-Loaded 32P-nHA Nanoparticles in Prostate Cancer Therapy

Hao Deng,Yumei Wang,Yue Zhou,Dongliang Zhai,Jie Chen,Shilei Hao,Xiaoliang Chen

Background Prostate cancer (PCa) ranks second in the incidence of all malignancies in male worldwide. The presence of multi-organ metastases and tumor heterogeneity often leads to unsatisfactory outcomes of conventional radiotherapy treatments. This study aimed to develop a novel folate-targeted nanohydroxyapatite (nHA) coupling to deliver adriamycin (Doxorubicin, DOX), 32P, and 99mTc simultaneously for the diagnosis and treatment of prostate-specific membrane antigen (PSMA) positive prostate cancer.Methods The spherical nHA was prepared by the biomimetic method and characterized. Folic acid (FA) was coupled to nHA with polyethylene glycol (PEG), and the grafting ratio of PEG-nHA and FA-PEG-nHA was determined by the thermogravimetric analysis (TGA) method. In addition, 32P, 99mTc, and DOX were loaded on nHA by physisorption. And the labeling rate and stability of radionuclides were measured by a γ-counter. The loading and release of DOX at different pH were determined by the dialysis method. Targeting of FA-PEG-nHA loaded with 99mTc was verified by in vivo SPECT imaging. In vitro anti-tumor effect of 32P/DOX-FA-PEG-nHA was assessed with apoptosis assay. The safety of the nano-drugs was verified by histopathological analysis.Results The SEM images showed that the synthesized nHA was spherical with uniform particle size (average diameter of about 100nm). The grafting ratio is about 10% for PEG and about 20% for FA. The drug loading and the delayed release of DOX at different pH confirmed its long-term therapeutic ability. The labeling of 32P and 99mTc was stable and the labeling rate was great. SPECT showed that FA-PEG-nHA showed well in vivo tumor targeting and less damage to normal tissues.Conclusion FA-targeted nHA loaded with 32P, 99mTc, and DOX may be a new diagnostic and therapeutic strategy for targeting PSMA-positive prostate cancer tumors, which may achieve better therapeutic results while circumventing the severe toxic side effects of conventional chemotherapeutic agents.

CAS / MDL: 538-75-0 6066-82-6
研究领域: 肿瘤学 · 药剂学 · 核医学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Materials Science & Engineering C-Materials for Biological Applications · 2018 · IF 5.08

Development of PSMA-targeted and core-crosslinked glycol chitosan micelles for docetaxel delivery in prostate cancer therapy

Xiang Feng,Yunfeng Zhou,Xin Xie,Ming Li,Hao Huang,Liangliang Wang,Xiao Xu,Jingmou Yu

In this study, prostate-specific membrane antigen (PSMA)-targeted and core-crosslinked micelles were developed based on prostate cancer-binding peptide (PCP) modified glycol chitosan-lipoic acid (PGC-LA) conjugate. The degree of substitution was 5.2 PCP groups and 10.7 lipoic acid groups per 100 sugar residues of glycol chitosan in PGC-LA copolymer. Docetaxel (DTX) was chosen as a model anti-tumor drug. The DTX-loaded micelles were prepared by an o/w method, and core-crosslinked micelles were further constructed by using a catalytic amount of dithiothreitol. The mean diameter of DTX-loaded core-crosslinked PGC-LA (DTX-PGC-LA/cc) micelles was 397 nm determined by dynamic light scattering (DLS). In vitro DTX released from core-crosslinked micelles was slower than that from non-crosslinked counterpart. Blank micelles exhibited good biocompatibility. Additionally, cellular uptake and cytotoxcity of PCP-modified micelles were higher than those of micelles without PCP in PSMA-positive LNCaP cells. Importantly, DTX-PGC-LA/cc demonstrated the stronger anti-tumor efficacy against LNCaP tumor xenograft models than DTX injection and other DTX-loaded micelles. Taken together, this study provides a potential way in developing actively targeted and core-crosslinked micelles for hydrophobic drug delivery in 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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MOLECULAR PHARMACEUTICS · 2018 · IF 4.556

Prostate-Specific Membrane Antigen Targeted Therapy of Prostate Cancer Using a DUPA–Paclitaxel Conjugate

Qingzhi Lv,Jincheng Yang,Ruoshi Zhang,Zimeng Yang,Zhengtao Yang,Yongjun Wang,Youjun Xu,Zhonggui He

Prostate cancer (PCa) is the most prevalent cancer among men in the United States and remains the second-leading cause of cancer mortality in men. Paclitaxel (PTX) is the first line chemotherapy for PCa treatment, but its therapeutic efficacy is greatly restricted by the nonspecific distribution in vivo. Prostate-specific membrane antigen (PSMA) is overexpressed on the surface of most PCa cells, and its expression level increases with cancer aggressiveness, while being present at low levels in normal cells. The high expression level of PSMA in PCa cells offers an opportunity for target delivery of nonspecific cytotoxic drugs to PCa cells, thus improving therapeutic efficacy and reducing toxicity. PSMA has high affinity for DUPA, a glutamate urea ligand. Herein, a novel DUPA–PTX conjugate is developed using DUPA as the targeting ligand to deliver PTX specifically for treatment of PSMA expressing PCa. The targeting ligand DUPA enhances the transport capability and selectivity of PTX to tumor cells via PSMA mediated endocytosis. Besides, DUPA is conjugated with PTX via a disulfide bond, which facilitates the rapid and differential drug release in tumor cells. The DUPA–PTX conjugate exhibits potent cytotoxicity in PSMA expressing cell lines and induces a complete cessation of tumor growth with no obvious toxicity. Our findings give new insight into the PSMA-targeted delivery of chemotherapeutics and provide an opportunity for the development of novel active targeting drug delivery systems for PCa therapy.

CAS / MDL: 1122-58-3 148893-10-1
研究领域: 肿瘤学 · 药学 · 分子生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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International Journal of Nanomedicine · 2020 · IF 5.115

PSMA-Targeting Reduction-Cleavable Hyperbranched Polyamide-Amine Gene Delivery System to Treat the Bone Metastases of Prostate Cancer

Yongheng Ye,Lingli Zhang,Yuhu Dai,Zhi Wang,Cuie Li,Yue Peng,Dong Ma,Peiheng He

Objective This study aimed to develop aptamer-anchored hyperbranched poly(amido amine) (HPAA) for the systemic delivery of miRNA-133a-3p and to evaluate its therapeutic potential against bone metastasis of prostate cancer in vivo and in vitro. Methods A glutathione (GSH)-responsive cationic HPAA was prepared by the Michael addition reaction. Furthermore, HPAA-PEG was produced by PEGylation, and then the aptamer targeted to prostate-specific membrane antigen (PSMA) was conjugated to the HPAA-PEG. The obtained HPAA-PEG-APT could form nanocomplexes with miRNA-133a-3p through electrostatic adsorption. Results The results of immunocytochemistry indicated that the complexes could target PSMA-expressing LNCaP cells. The ability of HPAA-PEG-APT to facilitate the delivery of miRNA-133a-3p into LNCaP cells was proven, and HPAA-PEG-APT/ miRNA-133a-3p demonstrated enhanced antitumor activity, lower cytotoxicity and better biocompatibility in vitro. Moreover, in a mouse tibial injection tumor model, the intravenous injection of the HPAA-PEG-APT/ miRNA-133a-3p complex significantly inhibited cancer growth and extended the survival time. Conclusion This study provided an aptamer-anchored HPAA-loaded gene system to deliver miRNA-133a-3p for better therapeutic efficacy of bone metastasis of prostate cancer.

研究领域: 肿瘤学 · 药学 · 分子生物学 · 生物医学工程
✓ 已验证 DOI PubMed 高影响因子
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JOURNAL OF BIOMATERIALS SCIENCE-POLYMER EDITION · 2024 · IF 3.6

Au/Doc/Quer@PDA/A10-3.2 Nanoparticles for targeted treatment of docetaxel-resistant prostate cancer

Junjie Ye,Qi Wu,Qingfen Ji,Shengjie You,Song Gao,Guanan Zhao,Qiangqiang Xu,Ken Liu,Peng Li

Docetaxel (Doc), as a first-line chemotherapy drug for prostate cancer (PC), often loses its therapeutic efficacy due to acquired resistance and lack of targeting specificity. Therefore, there is a need to develop a novel drug that can overcome Doc resistance and enhance its targeting ability to inhibit PC progression. In this study, we prepared Au/Doc/Quer@PDA/A10-3.2 nanoparticles (NPs) composite drug by encapsulating Doc and quercetin (Quer) within polydopamine (PDA)-coated Au NPs and further modifying them with RNA oligonucleotide aptamer A10-3.2. A10-3.2 was used for specific targeting of prostate-specific membrane antigen (PSMA)-positive PC cells (LNCaP). Quer was employed to reverse the resistance of Doc-resistant cell line (LNCaP/R) to Doc. Physical characterization using ultraviolet-visible spectroscopy (UV-vis), transmission electron microscopy (TEM), dynamic light scattering (DLS), X-ray photoelectron spectroscopy (XPS), and Fourier-transform infrared spectroscopy (FTIR) confirmed the successful preparation of Au/Doc/Quer@PDA/A10-3.2 NPs. Fluorescence imaging and flow cytometry experiments demonstrated the targeting ability of Au/Doc/Quer@PDA/A10-3.2 NPs towards PSMA-positive LNCaP/R cells. Cell proliferation, apoptosis, invasion, and migration experiments revealed that Quer reversed the resistance of LNCaP/R cells to Doc. Immunoblotting experiments further confirmed the mechanism behind sensitization of chemotherapy by Quer. Finally, we evaluated the therapeutic efficacy of Au/Doc/Quer@PDA/A10-3.2 NPs in a mouse model of PC. In conclusion, this study synthesized and validated a novel nano-composite drug (Au/Doc/Quer@PDA/A10-3.2 NPs) for combating Doc-resistant PC, which could potentially be applied in clinical treatment of PC.

CAS / MDL: 62-31-7 68-04-2 77-86-1
研究领域: 癌症研究 · 纳米技术 · 药学 · 分子生物学
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Research · 2026 · IF 12.9

Magnetically navigated and PSMA/STEAP1 dual-targeted nanoliposomes for NIR-II/MRI imaging with photothermal-chemo-immunotherapy for prostate cancer

Jian-Xuan Sun,Ye An,Si-Han Zhang,Jin-Zhou Xu,Abudureyimu Maimaiti,Jing-Yu Xu,Yi-Fan Huang,Yu-Xuan yang,Mei-Cheng Liu,Shao-Gang wang,Qi-Dong Xia

Precision theranostics for castration-resistant prostate cancer remain a major challenge because of tumor heterogeneity, drug toxicity, and resistance to conventional therapies. Here, we report a multifunctional theranostic nanoplatform that integrates multimodal imaging guidance, dual-targeted delivery, photothermal therapy, and immune activation for the precision treatment of prostate cancer. By encapsulating aggregation-induced emission luminogens and magnetic nanoparticles, this system achieves superior second near-infrared fluorescence and magnetic resonance imaging fusion for deep-tissue visualization. The dual-targeting strategy, which integrates magnetic navigation with simultaneous engagement of six-transmembrane epithelial antigen of the prostate 1 and prostate specific membrane antigen (PSMA), effectively addresses tumor heterogeneity by enabling externally guided and biologically specific delivery to both PSMA+ and PSMA− prostate cancer cells. Upon targeted delivery, the synergistic combination of photothermal therapy and chemotherapy achieves potent tumor growth inhibition, activates CD8+ T cells and macrophages to promote robust antitumor immune responses, and elicits durable immunological memory to prevent tumor recurrence. In vitro and in vivo studies demonstrate superior tumor targeting specificity, enhanced imaging contrast, and minimal off-target toxicity. This study provides novel insights into the construction of a multifunctional theranostic nanoplatform in precision oncology, with promising translational potential for clinical management of castration-resistant prostate cancer.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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EJNMMI Research · 2024 ·Vol. 14 ·期 1 ·1-13 · IF 3.1

Exploring the impact of PEGylation on pharmacokinetics: a size-dependent effect of polyethylene glycol on prostate-specific membrane antigen inhibitors

Liu Yang,Xia Li,Li Haiyang,Cai Ping,Tang Sufan,Feng Yue,Liu Guangfu,Chen Yue,Liu Nan,Zhang Wei,Zhou Zhijun

Background Prostate cancer is the second most frequent cancer and the fifth leading cause of cancer-related deaths in men. Prostate-specific membrane antigen (PSMA) as a target has gained increasing attention. This research aims to investigate and understand how altering size of PEG impacts the in vitro and in vivo behavior and performance of PSMA inhibitors, with a specific focus on their pharmacokinetic characteristics and targeting properties. Results Two 68 Ga-labeled PSMA-targeted radiotracers were developed, namely [ 68 Ga]Ga-PP4-WD and [ 68 Ga]Ga-PP8-WD, with varying sizes of polyethylene glycol (PEG). [ 68 Ga]Ga-PP4-WD and [ 68 Ga]Ga-PP8-WD had excellent affinity for PSMA with IC50 being 8.06 ± 0.91, 6.13 ± 0.79 nM, respectively. Both tracers enabled clear visualization of LNCaP tumors in PET images with excellent tumor-to-background contrast. They also revealed highly efficient uptake and internalization into LNCaP cells, increasing over time. The biodistribution studies demonstrated that both radioligands exhibited significant and specific uptake into LNCaP tumors. Furthermore, they were rapidly cleared through the renal pathway, as evidenced by [ 68 Ga]Ga-PP4-WD and [ 68 Ga]Ga-PP8-WD showing a tenfold and a fivefold less in renal uptake, respectively, compared to [ 68 Ga]Ga-Flu-1 in 30 min. Both in vitro and in vivo experiments demonstrated that PEG size significantly impacted tumor-targeting and pharmacokinetic properties. Conclusions These radiotracers have demonstrated their effectiveness in significantly reducing kidney uptake while maintaining the absorbed dose in tumors. Both radiotracers exhibited strong binding and internalization characteristics in vitro, displayed high specificity and affinity for PSMA in vivo .

研究领域: 医学肿瘤学 · 分子成像 · 药理学 · 生物化学 · 核医学
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MOLECULAR PHARMACEUTICS · 2023 · IF 4.9

Preclinical Evaluation of a Fibroblast Activation Protein and a Prostate-Specific Membrane Antigen Dual-Targeted Probe for Noninvasive Prostate Cancer Imaging

Pei Wang,Shuailiang Wang,Futao Liu,Ya’nan Ren,Qian Guo,Qian Zhang,XingGuo Hou,Yuan Yao,Hua Zhu,Zhi Yang

Prostate-specific membrane antigen (PSMA) is a prostate cancer target that plays a crucial role in prostate cancer diagnosis and therapy. Herein, a novel dual-targeted imaging probe, [68Ga]Ga-FAPI-PSMA, was prepared by radiolabeling conjugated DOTA-FAPI-PSMA with the short half-life radionuclide gallium-68 (68Ga), which is dedicated to prostate cancer diagnostic imaging. In vitro, [68Ga]Ga-FAPI-PSMA had higher affinity for the PSMA and FAP high-expressing cell lines 22Rv1 and U87 MG with IC50 values of 4.73 and 2.10 nM, respectively, than in the corresponding negative expression cell lines PC3 and A549, and significant differences in cell uptake were also observed. In vivo, [68Ga]Ga-FAPI-PSMA was rapidly cleared from the body, and the estimated radiation dose was relatively low compared with several other FAPI probes. In 22Rv1 and U87 MG tumor xenografts, [68Ga]Ga-FAPI-PSMA rapidly accumulated in tumors after administration, and the best images can be obtained at 1 h postinjection. In conclusion, the dual-targeted probe [68Ga]Ga-FAPI-PSMA was successfully prepared for in vivo prostate cancer PET/CT imaging.

CAS / MDL: 76-05-1
研究领域: 放射学 · 肿瘤学 · 分子影像 · 核医学
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