MOLECULAR PHARMACEUTICS
·
2024
·
IF 4.5
Zuojie Li,Yuhao Jiang,Qing Ruan,Guangxing Yin,Peiwen Han,Xiaojiang Duan,Junbo Zhang
The specific expression of prostate-specific membrane antigen (PSMA) makes it an ideal target for the diagnosis and treatment of prostate cancer. Currently, many 99mTc-labeled PSMA-targeted tracers have been developed. However, the high renal uptake of these 99mTc-labeled tracers is a common problem that limits their clinical application. In this work, the ligand (EUKPG) using DPro-Gly as the linker was synthesized and three 99mTc-labeled complexes ([99mTc]Tc-EUKPG-EDDA, [99mTc]Tc-EUKPG-TPPTS, [99mTc]Tc-EUKPG-TPPMS) with different coligands were prepared and evaluated. Among them, [99mTc]Tc-EUKPG-EDDA showed the most favorable pharmacokinetic properties, with significantly reduced uptake in the kidney (14.04 ± 0.23% ID/g), rapid clearance and low uptake in nontarget organs, thus making it to exhibit high tumor-to-background ratios (tumor/blood: 7.47, tumor/muscle: 12.65). Affinity studies have shown that it has high specificity for PSMA both in vivo and in vitro. Therefore, [99mTc]Tc-EUKPG-EDDA has great potential as a promising molecular tracer to target PSMA for tumor imaging.
研究领域:
医学影像学
·
肿瘤学
·
放射化学
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DOI
PubMed
高影响因子
JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
·
2018
·Vol. 319
·期 1
·69-73
·
IF 1.181
Duan Xiaoyan,Li Jianbo,Lu Xiaoling
In the field of nanotechnology, DNA-based nanoscale materials have facilitated the construction of DNA polyhedrons with different shapes and sizes by using predictable base pairing and highly tunable conformation. In this study DNA bipyramid nanostructures with one arm chain (T20-DBNs) were successfully prepared in a single annealing procedure. 99m Tc-A20 ssDNA was obtained by radiolabeled DTPA-A20 with 99m Tc, and then 99m Tc-DTPA-DBNs were obtained by hybridizing T20-DBNs with 99m Tc-A20 ssDNA. We focused on studying a method of 99m Tc radiolabeling DNA nanostructures with DTPA as a chelate, and hoped to develop a new SPECT molecular imaging probe based on DNA nanostructures.
研究领域:
纳米技术
·
放射医学
·
分子影像学
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产品关联
DOI
高影响因子
CERAMICS INTERNATIONAL
·
2025
·
IF 5.6
Yue Ji,Tian Tian,Pengju Chen,Yuan Zhao,Hao Wu,Yan Wu,Hiroshi Watabe,Wenlong Li,Yuezhou Wei,Xiangbiao Yin
99m Tc is one of the most widely used radioisotopes in nuclear medicine for diagnostic applications, with its supply critically dependent on the beta (β)-decay of the parent nuclide 99 Mo. To address this dependency, the cold sintering process has been introduced as a novel and facile technique to fabricate high-density MoO 3 ceramic targets for efficient 99 Mo production. It was explored in detail for the effects of transient liquid solutions, sintering temperature, uniaxial pressure, holding time, and additive formulation on the densification of raw MoO 3 powder. The results show that the typical transition solution of (NH 4 ) 6 Mo 7 O 24 ·4H 2 O and H 2 O mixture was most conducive to densifying MoO 3 material. The optimum conditions for cold sintering were under temperature of 200 °C, pressure of 500 MPa, holding time of 10 min, and transient aqueous solution of 10 wt.% (NH 4 ) 6 Mo 7 O 24 ·4H 2 O and 10 wt.% H 2 O. After further annealing cold-sintered MoO 3 at 600 °C, pure MoO 3 ceramic was obtained with the disappearance of the second phase. The pure MoO 3 ceramic target had a relative density of 95.48%, compressive strength of 118.01 MPa, and micro-Vickers hardness of 0.472 GPa. All these results suggested that cold sintering could be an energy-saving economical and efficient technique on the densification of MoO 3 for preparation its ceramic target, which are expected to inspire new insights to establish more practical technologies for 99 Mo and 99m Tc productions.
研究领域:
核医学
·
材料科学
·
放射性同位素生产
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产品关联
DOI
高影响因子
Nanomedicine
·
2024
·
IF 4.7
Yumei Wang,Yue Zhou,Dongliang Zhai,Hao Deng,Xiaoliang Chen
Aim: Nano-hydroxyapatite (nHA) is a good nanocarrier to load 223Ra, but the low specific activity (sp.act.) of 223Ra@nHA limits its application in medicine. Methods: We proposed a method for preparing nHA using PEG as a template, which significantly increases the sp.act of 223Ra@nHA and a new method to loaded 99mTc for in vivo tracking. Results: The nHA synthesized using PEG as a template was associated with higher sp.act for 223Ra in comparison to nHA with identical particle size and without PEG. The nHA load 99mTc-MDP was associated with higher labeling rate and stability in comparison to 99mTc. Conclusion: All these findings suggest that using PEG as a template and 99mTc-MDP could be the most effective of synthetic 223Ra/99mTc@nHA.
研究领域:
纳米技术
·
放射药学
·
癌症治疗
·
材料科学
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产品关联
DOI
PubMed
高影响因子
SEPARATION AND PURIFICATION TECHNOLOGY
·
2024
·
IF 8.1
Fan Zhang,Qi Zheng,Yachao Tan,Fan Wang,Khalid A.M. Salih,Ningchao Zheng,Mohammed F. Hamza,Shunyan Ning,Yuezhou Wei,Xiangbiao Yin
Currently, the primary approach for treating radioactive isotopes all over the world is a great challenge. The impact of this treatment is to transform liquid radioactive wastewater (present in huge volume) into low-volume solid radioactive waste. The current work presents synthesis and application of novel adsorbent using β-lactoglobulin fibrils (βFs) on SiO 2 particles and activated carbon particles (AC particles), which considered as facile and ecologically conscious. βFs were produced by denaturing inexpensive β-lactoglobulin. This method of filtering was used for radioactive waste, which differs from most prior adsorption techniques. Polyethyleneimine (PEI) was grafted onto protein fibrils using polydopamine (PDA). The produced material shows highly removal performance of TcO 4 - under both acidic and alkaline conditions (up to 99.76 %, with filtering time of just 5–6 min). This membrane exhibits a superior preference for TcO 4 - over certain common competing ions, including SO 4 2- , NO 3 – , and Cl - . The hybrid membrane achieves maximum adsorption performance for the substituted ion ReO 4 - of 533 mg/g, which is higher than the most commonly used fiber materials. Furthermore, βFs-PDA + PEI fibrils can efficiently treat up to 8000 kg of wastewater per kg and exhibit remarkable reusability performance. This membrane’s simple production, efficient performance, and excellent selectivity make it ideal to be implemented in both hospitals and nuclear power plants.
研究领域:
环境科学
·
核工程
·
材料科学
·
废物管理
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产品关联
DOI
高影响因子
MOLECULAR PHARMACEUTICS
·
2021
·
IF 4.939
Deliang Zhang,Rongqiang Zhuang,Jindian Li,Yuting Lv,Xia Yang,Weimin Pan,Xianzhong Zhang
Idiopathic pulmonary fibrosis (IPF) is a progressive fibrotic disease with poor prognosis. Evidence has shown that vimentin is a key regulator of lung fibrogenesis. 99mTc-labeled N-acetylglucosamine-polyethyleneimine (NAG-PEI), a vimentin-targeting radiotracer, was used for the early diagnosis of IPF, and NAG-PEI was also used as a therapeutic small interfering RNA (siRNA) delivery vector for the treatment of IPF in this study. Single-photon emission-computed tomography (SPECT) imaging of bleomycin (BM)- and silica-induced IPF mice with 99mTc-labeled NAG-PEI was performed to visualize pulmonary fibrosis and monitor the treatment efficiency of siRNA-loaded NAG-PEI, lipopolysaccharide (LPS, a tolerogenic adjuvant), or zymosan (ZYM, an immunostimulant). The lung uptakes of 99mTc-NAG-PEI in the BM- and silica-induced IPF mice were clearly and directly correlated with IPF progression. The lung uptake of 99mTc-NAG-PEI in the NAG-PEI/TGF-β1-siRNA treatment group or LPS treatment group was evidently lower than that in the control group, while the lung uptake of 99mTc-NAG-PEI was significantly higher in the ZYM treatment group compared to that in the control group. These results demonstrate that NAG-PEI is a potent MicroSPECT imaging-guided theranostic platform for IPF diagnosis and therapy.
研究领域:
肺病学
·
放射学
·
分子生物学
·
诊疗学
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产品关联
DOI
PubMed
高影响因子
Molecular Imaging
·
2016
·
IF 2.216
Pu Zhang,Zhide Guo,Deliang Zhang,Chang Liu,Guibing Chen,Rongqiang Zhuang,Manli Song,Hua Wu,Xianzhong Zhang
The aim of this study is to develop a copolymer-based single-photon emission computed tomography/magnetic resonance (SPECT/MR) dual-modality imaging agent that can be labeled with both technetium-99m (99mTc) and gadolinium (Gd) and target asialoglycoprotein receptor (ASGPR) via galactose. Monomers of N-p-vinylbenzyl-6-(2-(4-dimethylamino)benzaldehydehydrazono) nicotinate (VNI) for labeling of 99mTc, 5,8-bis(carboxymethyl)-3-oxo-11-(2-oxo-2-((4-vinylbenzyl)amino)ethyl)-1-(4-vinylphenzyl)-2,5,8,11-tetraazatridecan-13-oic acid (V2DTPA) for labeling of Gd, and vinylbenzyl-O-β-d-galactopyranosyl-d-gluconamide (VLA) for targeting ASGPR were synthesized, respectively. Then the copolymer P(VLA-co-VNI-co-V2DTPA) (pVLND2) was synthesized and characterized by gel permeation chromatography, dynamic light scattering, and high-performance liquid chromatography analysis. After labeling with 99mTc and Gd simultaneously, the radiochemical purity, toxicity, relaxivity (r1), and in vivo SPECT/MR imaging in mice were evaluated. Single-photon emission computed tomography/magnetic resonance imaging and biodistribution results showed that pVLND2 could target ASGPR well. The significantly improved signal to noise ratio was observed in mice liver during MR imaging. All the results suggest that this novel kind of copolymer has the potential to be further developed as a functional SPECT/MR imaging agent.
研究领域:
医学影像学
·
分子生物学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
·
2026
·
IF 1.6
Mao Yiyin,Zhou Peng,Jiang Juntao,Liu Yaling,Wang Hongyong,Han Guoqing,Wu Jun,Zou Pei,Lu Chunxiong
Programmed death-ligand 1 (PD-L1) represents a pivotal target for immune checkpoint blockade therapy. This study developed a novel PD-L1-targeting SPECT probe [ 99m Tc]Tc-G 3 C-2CBM based on dimeric 2-bromo-3-biphenyl (CBM) scaffold design. The probe was designed to enable bivalent interactions through dual CBM domains, exhibiting > 98% radiochemical yield and excellent in vitro stability. Cellular uptake studies revealed significantly higher accumulation in PD-L1-overexpressing A375-hPD-L1 cells compared to A375 cells (14.15 ± 2.11% vs. 5.89 ± 0.55% at 4 h; uptake ratio = 3.20). The probe displayed favorable binding affinity (K D = 36.54 ± 7.28 nM) and inhibitory potency (IC 50 = 69.62 ± 5.15 nM). In vivo SPECT imaging confirmed tumor-specific accumulation, though accompanied by notable hepatic uptake. These results demonstrate that CBM dimerization is a feasible approach for retaining PD-L1 binding and may provide a basis for the future development of multivalent radiotracers.
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DOI
高影响因子
JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
·
2024
·
IF 1.5
Xu Xiang,Mao Yiyin,Zhou Peng,Wu Yujing,Liu Yaling,Wang Hongyong,Lu Chunxiong,Zou Pei
In this study, a 99m Tc-labeled small molecule imaging probe [ 99m Tc]Tc-PG3C-CBM for PD-L1 imaging was designed. It showed a radiochemical yield of > 97% and good in vitro stability. Uptake in A375-hPD-L1 cells (17.07 ± 1.40%) was 4.5 times higher than in A375 cells (3.81 ± 0.19%). The probe demonstrated moderate PD-L1 affinity (K D : 11.6 ± 2.57 nM; IC 50 : 59.2 ± 2.40 nM). Additionally, SPECT/CT imaging and biodistribution results indicated that [ 99m Tc]Tc-PG3C-CBM was mainly metabolized by the liver and showed some accumulation at the tumor site. These results suggest that [ 99m Tc]Tc-PG3C-CBM could potentially target PD-L1 at tumor sites.
研究领域:
核医学
·
分子影像学
·
肿瘤学
✓ 已验证
DOI
高影响因子
International Journal of Nanomedicine
·
2023
·
IF 8
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.
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
MOLECULAR PHARMACEUTICS
·
2025
·
IF 4.5
Yujing Du,Xiaona Ren,Yao Wang,Yang Xu,Shida Duan,Yan Fan,Jianhua Zhang,Min-Fu Yang
Yttrium oxide (Y2O3), as a rare-earth oxide nanoparticle, has potential toxicity that remains unresolved. By bridging the gap between nanomaterial development and safety assessment, this work aimed to evaluate the biodistribution of Y2O3 using a novel radiolabeling approach with technetium-99m (99mTc) for real-time tracking. Different concentrations (0.4, 4, and 8 mg/mL) of Y2O3 were used for 99mTc labeling and were intravenously administered to mice. In vivo organ biodistribution was measured via dynamic planar imaging and micro single-photon emission computed tomography/computed tomography (micro-SPECT/CT). Biodistribution and inductively coupled plasma mass spectrometry (ICP-MS) were conducted to quantitative tissue uptake of 99mTc-Y2O3, and hematoxylin-eosin (H&E) staining were performed for histopathological evaluation. Different concentrations of 99mTc-Y2O3 were successfully synthesized with a high radiochemical purity and stability. In vivo imaging revealed different distribution patterns with 0.4, 4, and 8 mg/mL of 99mTc-Y2O3. Low-dose 99mTc-Y2O3 nanoparticles rapidly cleared from pulmonary circulation, shifting to predominant hepatic-splenic accumulation. In contrast, medium and high doses demonstrated prolonged lung retention with partial redistribution to the spleen and liver. These biodistribution patterns were validated by ICP-MS, which showed a strong correlation with the 99mTc-Y2O3 tracking. Histopathology revealed dose-related alveolar wall thickening and splenic white pulp expansion. This study demonstrated that 99mTc-Y2O3 could be a robust tool for nanoparticle in vivo tracking, providing the organ distribution information for long-term toxicity studies and chronic exposure effects.
研究领域:
纳米医学
·
放射性药物
·
毒理学
·
分子成像
·
纳米颗粒生物分布
✓ 已验证
DOI
PubMed
高影响因子
SEPARATION AND PURIFICATION TECHNOLOGY
·
2026
·
IF 9.1
Weiquan Liu,Qingru Zeng,Juan Liu,Zihang Yi,Mohammed F. Hamza,Yuezhou Wei,Lifeng Chen,Shunyan Ning
99m Tc, one of the most vital radioisotopes in nuclear medicine, is primarily supplied by molybdenum‑technetium ( 99 Mo/ 99m Tc) generators using alumina as the adsorbent. Nevertheless, this conventional technology poses challenges including the adsorbent's low Mo adsorption capacity, low distribution coefficient, and potential radioactive leakage. To address this challenge, a novel silica-based amine adsorbent (DDA/SiO 2 -P) was developed for the high adsorption capacity of Mo and efficiently separation of Mo and Tc. Given their similar chemical properties, rhenium (Re) was employed as a non-radioactive surrogate for technetium in this study. The adsorbent demonstrates exceptional performance with a Mo adsorption capacity of 119 mg/g, 170 mg/g, and 222 mg/g at 288 K, 308 K, and 318 K at pH = 2 respectively, achieving a remarkable separation factor ( SF Mo/Re ) of 3200. Furthermore, the adsorbent enables efficient elution of Re using 0.9 wt% NaCl solution. In a dynamic column experiment simulating generator operation, the recovery rate of Re reached 85.15% in the first ten collected fractions with the chemical purity of Re 99%, corresponding to a radiochemical purity of 99.9%. Additionally, the synthesis method for this adsorbent is straightforward and cost-effective, positioning it as a promising candidate for next-generation 99 Mo/ 99m Tc generators.
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产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）