Contrast Media & Molecular Imaging
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2019
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IF 1.984
Yuxiao Xia,Li Zhang,Yanhong Zhao,Xiangdong Liu,Liang Cai,Lin Liu,Yue Chen,Wei Zhang
Objective. This work evaluated the potential of 68Ga-labelledNOTA-ICG (1,4,7-triazacyclononane-1,4,7-triacetic acid indocyanine green) for liver reserve imaging. Methods. To determine the optimal conditions for generating 68Ga-NOTA-ICG, various reaction parameters were implemented. Quality control analysis was performed using different chromatography techniques. The in vitro and in vivo stability was also measured at specific time points. The radioactivity ratio between n-octanol and water was determined to evaluate the water solubility of 68Ga-NOTA-ICG. The plasma-protein binding rate of the labelled compound was determined by the methanol method. The biodistribution and imaging findings were evaluated in normal animals at different time points after injection. A preliminary imaging evaluation was performed using an animal model of hepatic ischaemia-reperfusion injury, which was confirmed by pathology. Results. 68Ga-NOTA-ICG was prepared with very high radiochemical purity (>98%) by reacting at 90°C for 10 min at pH = 3.5∼4.0, with excellent stability in vivo and in vitro (>95% 3 h postpreparation). The in vitro plasma-protein binding rate of 68Ga-NOTA-ICG was 13.01 ± 0.7%, and it showed strong water solubility . We found that in addition to excretion through the biliary tract and intestines, 68Ga-NOTA-ICG can be excreted through the urinary tract. The image quality of 68Ga-NOTA-ICG was very high; imaging agent retained in the area of liver injury could clearly be observed. Conclusion. This is the first report on a 68Ga-labelled NOTA-ICG fragment for liver reserve function studies. This complex has promise as a candidate agent for liver reserve imaging.
研究领域:
医学影像学
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核医学
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药理学
✓ 已验证
DOI
PubMed
高影响因子
ACS Applied Materials & Interfaces
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2018
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IF 8.097
Dongban Duan,Hui Liu,Yang Xu,Yuxiang Han,Mengxin Xu,Zhengchu Zhang,Zhibo Liu
The classical photodynamic therapy (PDT) requires external light to activate photosensitizers for cancer treatment. However, limited tissue penetration of light has been a long-standing challenge for PDT to cure malignant tumors in deep tissues. Recently, Cerenkov radiation (CR) emitted by radiotracers such as 18F-fluorodeoxyglucose (18F-FDG) has become an alternative and promising internal light source. Nevertheless, fluorine-18 (F-18) only releases 1.3 photons per decay in average; consequently, injection dose of F-18 goes beyond 10–30 times more than usual to acquire therapeutic efficacy because of its low Cerenkov productivity. Gallium-68 (Ga-68) is a favorable CR source owing to its ready availability from generator and 30-time higher Cerenkov productivity. Herein, we report, for the first time, the use of Ga-68 as a CR source to activate dextran-modified TiO2 nanoparticles (D-TiO2 NPs) for CR-induced PDT. Compared with 18F-FDG, 68Ga-labeled bovine serum albumin (68Ga-BSA) inhibited the growth of 4T1 cells and exhibited significantly stronger DNA damage to tumor cells. In vivo studies showed that the tumor growth was almost completely inhibited when tumor-bearing mice were treated with a combination of D-TiO2 NPs and 68Ga-BSA. This study proved that Ga-68 is a more potent radionuclide for PDT than F-18 both in vitro and in vivo offered a promising strategy of using a diagnostic dose of radioactivity to achieve depth-independent cancer therapy without using any external light source.
研究领域:
放射医学
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纳米医学
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肿瘤学
✓ 已验证
DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
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2025
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IF 4.7
Zhen-Peng Yu,Ke-Xin Sun,Dan Zhang,Zhi-Qiang Yu,Deng-Yun Chen,Hong Zhu,Hongwei Si,Peng-Fei Dai
Anaplastic lymphoma kinase (ALK) is prominently expressed in numerous malignant tumors, which lead to aberrant tumor proliferation, invasion and metastasis. Ceritinib (LDK378), as second-generation targeted drugs, has been used to treat advanced ALK-positive non-small cell lung cancer (NSCLC). Herein, we sought to develop a novel ALK-positron emission tomography/magnetic resonance (PET/MR) tracer 68 Ga-DOTA-CTB ( 68 Ga labeled ceritinib) based on ceritinib scaffold to monitor the ALK expression levels during targeted therapy with ceritinib. The 68 Ga-DOTA-CTB radiotracer, obtained via a simple labeling procedure, exhibits favorable radiochemical purity, stability, and pharmacokinetic properties. Subsequently, cellular uptake experiments have demonstrated that 68 Ga-DOTA-CTB could be accumulated in H2228 cells. Imaging and biodistribution experiments have revealed significant uptake of the radiotracer in the tumors of the experimental group, while tumors in the blocking group, which were saturated with an excess of precursor, exhibited a markedly reduced level of radioactivity. These empirical findings suggest that 68 Ga-DOTA-CTB holds substantial potential as a novel PET/MR imaging tracer for ALK-positive tumors.
研究领域:
肿瘤学
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核医学
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分子影像学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ACS Chemical Neuroscience
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2025
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IF 3.9
Wenjing Li,Xiaochuan Zha,Xiaoyu Zhang,Haixin Dai,Suyun Pu,Xinya Yao,Wenxue Hui,Rui Xu,Junyu Bao,Jiahao Yu,Yan Wei,Jiawen Huang,Na Guo,Ming Xu,Jian Zhao,Bingbing Cheng,Zonghua Luo
Focused ultrasound (FUS)-mediated blood-brain barrier (BBB) opening is an innovative approach for enhancing the delivery of central nervous system drugs. 68Ga radiotracers are advantageous for imaging due to their ideal half-life and imaging properties; however, their limited ability to traverse the BBB constrains their application in brain imaging. This study investigates the application of FUS to selectively deliver the 68Ga radiotracer, [68Ga]STZL4110, into the hippocampus for β-amyloid positron emission tomography (PET) imaging in an Alzheimer’s disease (AD) mouse model. The synthesis and radiolabeling of [68Ga]STZL4110 were accomplished, demonstrating robust binding to β-amyloid, as validated by Thioflavin T assays and in vitro autoradiography with both wild-type (WT) and APP/PS1 AD mouse brain sections. Cavitation activity measurements confirmed effective and consistent BBB opening post-FUS treatment, ensuring targeted delivery without vascular damage, as supported by histological analysis. Quantitative PET imaging revealed the successful detection of β-amyloid deposition following FUS treatment. Initially, [68Ga]STZL4110 showed a low volume of distribution in the right hippocampus of AD mice. FUS application significantly enhanced BBB permeability, leading to a 74% increase in [68Ga]STZL4110 uptake in the targeted right hippocampus of APP/PS1 mice compared with the left hippocampus, whereas no significant change was observed in WT mice. These findings suggest that combining FUS with [68Ga]STZL4110 could significantly enhance the sensitivity and specificity of 68Ga PET imaging for β-amyloid. FUS-mediated PET imaging may potentially address the challenge of effective brain imaging with radiotracers that traditionally exhibit a low penetration of the BBB.
研究领域:
神经影像学
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分子影像学
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神经病学
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放射学
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阿尔茨海默病研究
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）