JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
·
2018
·Vol. 62
·期 1
·43-51
·
IF 1.423
Qin Xu,Shumao Zhang,Yan Zhao,Yue Feng,Lin Liu,Liang Cai,Wei Zhang,Zhanwen Huang,Hongyuan Wei,Liangang Zhuo,Yue Chen
The purposes of this study were as follows: (1) to radiolabel ibandronic acid (IBA, a third-generation bisphosphonate) with 177 Lu, investigating optimal labeling conditions, and (2) to analyze biodistribution and imaging properties of intravenous 177 Lu-ibandronate ( 177 Lu-IBA) administered in animals. 177 Lu-labeled methylene diphosphonate ( 177 Lu-MDP) served as a comparator agent. Differing proportions of IBA solution and 177 LuCl 3 solution were combined to determine an optimal ratio for radiolabeling purposes, varying pH, temperature, and time to establish ideal reactivity conditions. Radiochemical purity of the labeled compounds was then assessed by paper chromatography. In vitro and in vivo stabilities were also measured at specific time intervals. In Kunming mice, biodistributions of 177 Lu-IBA and 177 Lu-MDP and respective agent activities in various organs were monitored by gamma counter, and we performed single photon computed tomography/computed tomography (SPECT/CT) imaging of 177 Lu-IBA in normal New Zealand White rabbits. Radiolabeling yields for 177 Lu-IBA proved to be >97% within 30 minutes at 90°C, and its radiochemical purity ensured stability in vitro and in vivo. Furthermore, we found that 177 Lu-IBA is readily soluble in water, showing higher skeletal uptake than 177 Lu-MDP but lower uptake by liver and spleen. The image quality of 177 Lu-IBA was so clear that even after 6 days, analysis was still feasible.
研究领域:
核医学
·
药理学
·
分子影像学
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DOI
PubMed
高影响因子
JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
·
2023
·Vol. 332
·期 6
·2093-2102
·
IF 1.6
Li Kehong,Fan Wenqi,Yan Jingxuan,Wang Jing,Zhao Peng,Liao Wei,Yang Yuchuan,Yang Xia,Wei Hongyuan,Chen Yue
Differences in cellular radiosensitivity and the binding affinity of radiopharmaceuticals could directly affect the radiotherapeutic effects. In this study, we investigated the radionuclide ( 177 Lu) induced radiosensitivity of serval non-small-cell lung cancer cells (NSCLCs) as well as the binding affinity of cetuximab to those cells. The apoptosis of NSCLCs caused by 177 Lu was related to the DNA double-strand damage and was cell-type dependent. We also proved that the introduction of 177 Lu to the antibody could enhance its cytotoxic effect on NSCLCs. The [ 177 Lu]Lu-DOTA-cetuximab could accumulate in the HCC827 tumor xenografts with excellent stability according to in vivo SPECT/CT imaging and the biodistribution results. The [ 177 Lu]Lu-DOTA-cetuximab showed high potential to be used for targeting diagnosis and radiotherapy in lung cancers.
研究领域:
肿瘤学
·
放射生物学
·
核医学
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产品关联
DOI
高影响因子
ACS Nano
·
2024
·
IF 15.8
Yueping Li,Shanshan Shan,Ruru Zhang,Chaoping Sun,Xuelan Hu,Jiada Fan,Yi Wang,Ruixue Duan,Mingyuan Gao
Efforts on bladder cancer treatment have been shifting from extensive surgery to organ preservation in the past decade. To this end, we herein develop a multifunctional nanoagent for bladder cancer downstaging and bladder-preserving therapy by integrating mucosa penetration, reduced off-target effects, and internal irradiation therapy into a nanodrug. Specifically, an iron oxide nanoparticle was used as a carrier that was coated with hyaluronic acid (HA) for facilitating mucosa penetration. Dibenzocyclooctyne (DBCO) was introduced into the HA coating layer to react through bioorthogonal reaction with azide as an artificial receptor of bladder cancer cells, to improve the cellular internalization of the nanoprobe labeled with 177Lu. Through magnetic resonance imaging, the targeted imaging of both nonmuscle-invasive bladder cancer (NMIBC) and muscle-invasive bladder cancer (MIBC) was realized after intravesical instillation of the multifunctional probe, both NMIBC and MIBC were found downstaged, and the metastasis was inhibited, which demonstrates the potential of the multifunctional nanoprobe for bladder preservation in bladder cancer treatment.
研究领域:
肿瘤学
·
放射医学
·
纳米医学
·
分子影像学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
CARBON
·
2024
·
IF 10.5
Guoquan Ma,Haiyue Peng,Xisheng Fan,Yang Li,Jing Gao,Yingjiang Hu,Bo Li,Yuanyou Yang,Jingsong Zhang,Lijian Ma,Ning Liu,Jiali Liao,Feize Li
Porous carbon materials stemming from covalent organic frameworks (COFs) have emerged as pivotal candidates in various fields. However, no COF or relevant derivative has stepped into the recovery of no-carrier added (NCA) 177 Lu, one of the most important radionuclides in modern medicine, from irradiated target. In this work, shape-persistent COF-derived carbon microsphere (COF-CMS) was successfully synthesized via self-templated carbonization and subsequently functionalized with active component 2-ethylhexyl phosphoric acid mono-2-ethylhexyl ester (P507). The prepared functional COF-CMS@P507 has shown high selectivity and fast adsorption kinetics for Yb 3+ /Lu 3+ in static batch adsorption and great potential in dynamic column separation of Lu 3+ from Yb 3+ . More importantly, based on plenty of tracer experiments and practical investigations, a separation process flow was established to realize the isolation of 177 Lu from an irradiated 176 Yb target. Consequently, 177 Lu product can be effectively obtained in preferable recovery (86%) with high radinuclidic and chemical purity (≥99.99%). The present study provides a new idea for NCA 177 Lu production, which is also valuable for the development of lanthanide separation and functional COFs.
研究领域:
放射医学
·
材料科学
·
核化学
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产品关联
DOI
高影响因子
JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
·
2021
·Vol. 330
·期 3
·997-1005
·
IF 1.371
Yang Yuchuan,Wang Jing,Liu Wei,Deng Hao,Zhao Peng,Liao Wei,Wang Guanquan,Wei Hongyuan,Zhuo Liangang,Yang Xia
Death receptor 5 (DR5) is overexpressed in many tumors. Combination of the anti-DR5 antibody with radionuclides such as lutetium-177 ( 177 Lu) could enhance apoptosis and decrease the possibility of drug-induced resistance. In this study, a humanized anti-DR5 monoclonal antibody CTB006 was labeled with zirconium-89 ( 89 Zr) and 177 Lu to improve its efficiency for diagnosis and radiotherapy, respectively. The radiolabeled antibodies showed high tumor uptake in colon205 xenografts according to the results of micro-PET imaging and biodistribution. The 177 Lu-DOTA-CTB006 could inhibit tumor growth significantly.
研究领域:
肿瘤学
·
核医学
·
分子影像学
✓ 已验证
DOI
高影响因子
Separations
·
2025
·Vol. 12
·期 8
·215
·
IF 2.7
Jiuquan Qi,Qianwen Chen,Chuanying Liu,Chengliang Xiao,Shuainan Ni
Due to the nearly identical chemical properties of Lu and Yb, the production of no-carrier-added (NCA)177Lu faces significant challenges in their separation. Achieving efficient and streamlined separation of Lu and Yb is crucial for the production of NCA177Lu. This study systematically investigated the separation performance of the commercial Rext-P350 extraction resin for Lu and Yb. Static adsorption experiments revealed that, at a solid–liquid ratio of 8 g/L, both Lu3+and Yb3+were nearly completely adsorbed, with saturation adsorption capacities of 25.8 mg/g and 21.5 mg/g, respectively. An increase in the nitric acid concentration in the aqueous phase significantly inhibited adsorption, but the separation factor for Lu3+/Yb3+remained above 1.88. The adsorption kinetics followed a pseudo-second-order model (R2> 0.99), with equilibrium reached within 15 min, demonstrating fast adsorption kinetics. Characterization by SEM, FT-IR, and XPS confirmed the chemical coordination between the resin and Lu3+/Yb3+. Dynamic chromatographic separation experiments showed that the Rext-P350 resin exhibited significantly better separation performance for Lu3+/Yb3+compared to 2-ethylhexylphosphoric acid mono-2-ethylhexyl ester (P507) extraction resin. Leveraging the excellent performance of Rext-P350 resin, a two-stage continuous extraction chromatography process was designed, achieving efficient separation of 0.045 mg of Lu3+from 200 mg of Yb3+with a Lu3+purity of 90.9% and a yield of 98.4%. This study provides a feasible separation technique for the purification of NCA177Lu.
研究领域:
核化学
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放射性同位素生产
·
分离科学
·
无机化学
·
核医学
✓ 已验证
DOI
高影响因子
ACS Applied Materials & Interfaces
·
2023
·
IF 9.5
Ranxi Liang,Feize Li,Xijian Chen,Fuyuan Tan,Tu Lan,Jijun Yang,Jiali Liao,Yuanyou Yang,Ning Liu
Nano-metal–organic frameworks (nano-MOFs) labeled with radionuclides have shown great potential in the anticancer field. In this work, we proposed to combine fluorescence imaging (FI) with nuclear imaging to systematically evaluate the tumor inhibition of new nanomedicines from living cancer cells to the whole body, guiding the design and application of a high-performance anticancer radiopharmaceutical to glioma. An Fe-based nano-MOF vector, MIL-101(Fe)/PEG-FA, was decorated with fluorescent sulfo-cyanine7 (Cy7) to investigate the binding affinity of the targeting nanocarriers toward glioma cells in vitro, as well as possible administration modes for in vivo cancer therapy. Then, lutetium-177 (177Lu)-labeled MIL-101(Fe)/PEG-FA was prepared for high-sensitive imaging and targeted radiotherapy of glioma in vivo. It has been demonstrated that the obtained 177Lu-labeled MIL-101(Fe)/PEG-FA can work as a complementary probe to rectify the cancer binding affinity of the prepared nanocarrier given by fluorescence imaging, providing more precise biodistribution information. Besides, 177Lu-labeled MIL-101(Fe)/PEG-FA has excellent antitumor effect, leading to cell proliferation inhibition, upregulation of intracellular reactive oxygen species, tumor growth suppression, and immune response-related protein and cytokine upregulation. This work reveals that optical imaging and nuclear imaging can work complementarily as multimodal imaging in the design and evaluation of anticancer nanomedicine, offering a MIL-101(Fe)/PEG-FA-based pharmaceutical with potential in tumor endoradiotherapy.
研究领域:
纳米技术
·
放射学
·
肿瘤学
·
药学
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Precision Radiation Oncology
·
2026
·
IF 3.6
Xingliang Liu,Gang Wang,Zhenwen Zhao,Haoyu Wang,Hongyu Chen,Xiao Xu,Jingdong Li,Hongjuan Ma
Purpose Transarterial radioembolization (TARE) is an important locoregional therapy for hepatocellular carcinoma (HCC). However, clinically used yttrium-90 ( 90 Y) microspheres are non-biodegradable and provide limited imaging capability, while biodegradable polymeric microspheres prepared using conventional radiolabeling strategies often exhibit poor radionuclide stability. Experimental design We designed a biodegradable radiometal-chelating microsphere based on amidoxime-functionalized polylactic acid microspheres (PLA-g-PAO-Ms) engineered via electron beam-induced graft polymerization. Results The PLA-g-PAO-Ms exhibited a high Lu 3+ loading capacity (33.83 mg g −1 ) and underwent controlled biodegradation in vitro after approximately 20 d. Cell Counting Kit-8 (CCK-8) assays confirmed favorable cytocompatibility, with both LO2 and HepG2 cell viabilities exceeding 90% after 72 h, showing no significant difference from the control group ( p > 0.05); by contrast, free Lu 3+ (50 mg·L −1 ) significantly reduced HepG2 viability to 51.4% ( p < 0.001). In a rat orthotopic liver tumor model, the intra-arterial administration of 177 Lu-labeled PLA-g-PAO-Ms ( 177 Lu-PLA-g-PAO-Ms) resulted in pronounced tumor suppression with sustained in vivo radionuclide retention for at least 14 d. Biodistribution analysis revealed selective tumor accumulation of 8.79 ± 1.74 %ID g −1 , significantly higher than that in normal liver ( 1 ± 0.54 %ID g −1 ) and other organs ( P < 0.001 ), whereas free 177 LuCl 3 showed minimal tumor uptake ( 0.30 ± 0.28 %ID g −1 ) with predominant non-target organ accumulation. Conclusion These findings suggest that PLA-g-PAO-Ms provide a biodegradable microsphere system capable of stable radiometal incorporation and effective tumor suppression following intra-arterial administration, offering a promising approach for interventional radionuclide therapy for HCC.
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DOI
高影响因子
JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
·
2025
·
IF 1.6
Li Yuan-Yuan,Yu Jia-Yan,Wang Tao,Wang Jing,Zhao Peng,Yang Xia,Wei Hong-Yuan,Chen Yue
Fab fragments obtained via enzymatic digestion of full-length antibodies or by gene recombination technology have smaller molecular weight and greater penetration ability. Those advantages make it uniquely suited to deliver radionuclides. In this study, we prepared a Fab fragment from the anti-EGFR antibody Cetuximab and labeled it with 177 Lu. The binding activity in vitro and biodistribution in vivo of [ 177 Lu]Lu-DOTA-Fab-Cetuximab were investigated. The [ 177 Lu]Lu-labeled Fab fragment showed improved tumor penetration and faster blood clearance compared to the full-length antibody.
研究领域:
医学
·
肿瘤学
·
核医学
✓ 已验证
产品关联
DOI
高影响因子
BIOCONJUGATE CHEMISTRY
·
2025
·
IF 3.9
Jing Wang,Chengxue He,Rui Guo,Li Wen,Jinping Tao,Huimao Zhang,HaiFeng Huang,Hua Zhu,Zhi Yang,Xianteng Yang
Malignant glioma highly expresses carbonic anhydrase IX (CAIX). This study aimed to develop [177Lu]Lu-XYIMSR-01, a small-molecule therapeutic agent CAIX, to assess its potential for treating malignant glioma. [177Lu]Lu-XYIMSR-01 was synthesized by radiolabeling DOTA-XYIMSR-01 with 177Lu. In vitro assays were conducted to evaluate the affinity for U87MG tumor cells. The probe was injected via the tail vein into subcutaneous and orthotopic U87MG models for micro-SPECT/CT imaging. The survival rates of tumor-bearing mice were assessed after [177Lu]Lu-XYIMSR-01 injection by intratumoral in orthotopic models, including untreated controls and those treated with Temozolomide or combination therapy. After purification, the radiochemical yield of [177Lu]Lu-XYIMSR-01 was 86.47 ± 2.42%, with a radiochemical purity (RCP) of 99%. Its cell uptake in U87MG cells was 3.70 ± 0.57 ‰ AD/105 cells, significantly higher than that in HCT116 cells (0.68 ± 0.16 ‰ AD/105 cells, P = 0.001). In the biodistribution study, [177Lu]Lu-XYIMSR-01 uptake in U87MG tumors was 6.19 ± 1.37%ID/g, with a tumor/muscle ratio of 20.14 ± 3.24. In the orthotopic glioma model, local injection combined with Temozolomide significantly improved survival and inhibited tumor growth. The results indicate that [177Lu]Lu-XYIMSR-01 is a promising therapeutic molecular probe for targeting CAIX, and its combination with Temozolomide significantly enhances treatment outcomes for malignant glioma.
研究领域:
肿瘤学
·
分子影像学
·
核医学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ACS Omega
·
2026
·
IF 5.2
Huanyu Chen,Yuduo Wan,Wanlu Feng,Changjiang Wang,Yang Wang,Yue Chen,Takron Chantadee,Zibo Li,Li Wang
Nectin-4, a cell adhesion molecule frequently overexpressed in non-small cell lung cancer (NSCLC), has emerged as a promising target for theranostic applications due to its involvement in tumor progression and association with poor prognosis. This study aimed to develop radiolabeled agents based on bicyclic peptides for both imaging and targeted therapy for Nectin-4 positive tumors. We designed and synthesized 68Ga-labeled probes ([68Ga]Ga-3 and [68Ga]Ga-5) for PET imaging and 177Lu-labeled agents ([177Lu]Lu-6) for targeted radionuclide therapy. Radiochemical yields and purity were optimized, and the agents were evaluated for cellular uptake, internalization, and biodistribution in Nectin-4-expressing cell lines (H1975, ABC-1, HEK293nectin4) and xenograft models. Target specificity was confirmed through blocking studies with the Nectin-4 specific inhibitor peptide N188. The 68Ga-labeled probes exhibited high radiochemical yields (78–81%) and purity (>95%), with specific uptake observed in Nectin-4-positive cells (e.g., 69.20 ± 2.31%ID/106 cells for [68Ga]Ga-3 at 120 min) and tumors. Blocking studies resulted in significant reductions in uptake, with 39-fold and 22-fold decreases for [68Ga]Ga-3 and [68Ga]Ga-5, respectively, confirming Nectin-4 specificity. [177Lu]Lu-6 showed superior tumor retention (13% uptake) and internalization (3.5%) compared to [177Lu]Lu-FAP-2286/N188, with sustained tumor growth suppression in xenograft models. PET/SPECT imaging revealed high tumor-to-background ratios and favorable pharmacokinetics, highlighting the potential of these agents for clinical application.
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
·
2026
·
IF 1.7
Yu Jiayan,Wang Tao,Li Jiajia,He Zhiyou,Wang Jing,Zhao Peng,Chen Yue,Yang Xia
Antibody-targeted radioimmunotherapy holds significant potential for solid tumor treatment. However, intact antibodies (IgG) and fragments (F(ab’) 2 ) may exhibit distinct pharmacokinetic and radiation delivery properties due to differences in molecular size and Fc functionality. TROP2 is highly overexpressed in most malignant tumors but minimally expressed in normal tissues. Therefore, the anti-TROP2 antibody was selected as the targeting agent in this study. We prepared the F(ab’) 2 antibody fragments of anti-TROP2 antibody and systematically compared the in vitro and in vivo behaviors of [ 177 Lu]Lu-DOTA-anti-TROP2 antibody and [ 177 Lu]Lu-DOTA-anti-TROP2-F(ab’) 2 antibody fragments to optimize radioligand therapy strategies. Cell binding assays were conducted to evaluate their TROP2 antigen binding affinity. In vivo distributions in tumors and normal organs were investigated through Micro-SPECT/CT imaging and biodistribution studies using tumor-bearing mice. The results demonstrated that, compared to the anti-TROP2 antibody, the anti-TROP2-F(ab’) 2 antibody fragments exhibited superior blood clearance kinetics as well as lower accumulation in liver and spleen. This could reduce the radiation side effects of [ 177 Lu]Lu-DOTA-anti-TROP2-F(ab’) 2 antibody fragments on bone marrow or other full-antibody target normal organs. However, cutting Fc from the full anti-TROP2 antibody increased renal accumulation and exhibited shedding phenomena following tumor targeting.
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DOI
高影响因子
危险品化学品经营许可证（带存储）