Pub Date : 2025-06-16DOI: 10.1016/j.nano.2025.102837
Mahdiyar Dehshiri MSc , Fateme Zarein MSc , Fatemeh Rajabi MSc , Mohammad Reza Javan PhD , Maryam Nikkhah PhD , Fatemeh Rahbarizadeh PhD , Jalil Mehrzad PhD, DVM , Seyed Mohammad Moazzeni PhD , Amir Ali Hamidieh MD , Saman Hosseinkhani PhD
Genetic modification of immune cells remains a major challenge in immunotherapy. While viral and non-viral carriers exist, low gene transfer efficiency persists with non-viral methods. We present a peptide-based carrier (MiRGD) for gene delivery to diverse immune cells. The MiRGD/plasmid complex formation was characterized via gel retardation, dynamic light scattering, and zeta potential analysis. After safety and efficiency optimization in HEK293T cells, MiRGD achieved 69 % chimeric antigen receptor (CAR) transfection in Jurkat T cells (>98 % viability) and 28 % in primary human T cells. Dendritic cells showed 61 % transfection with >85 % viability. In vivo, MiRGD functioned as a DNA vaccine against SARS-CoV-2, eliciting robust antibody titers, neutralization, and safe histopathology. These results demonstrate MiRGD's efficacy and biocompatibility for immune cell engineering (T cells, dendritic cells, macrophages) and vaccination, offering a cost-effective, non-toxic platform for immunotherapy applications.
{"title":"Efficient gene delivery to immune cells via a recombinant multifunctional chimeric peptide nanocarrier: Implications in immunotherapy","authors":"Mahdiyar Dehshiri MSc , Fateme Zarein MSc , Fatemeh Rajabi MSc , Mohammad Reza Javan PhD , Maryam Nikkhah PhD , Fatemeh Rahbarizadeh PhD , Jalil Mehrzad PhD, DVM , Seyed Mohammad Moazzeni PhD , Amir Ali Hamidieh MD , Saman Hosseinkhani PhD","doi":"10.1016/j.nano.2025.102837","DOIUrl":"10.1016/j.nano.2025.102837","url":null,"abstract":"<div><div>Genetic modification of immune cells remains a major challenge in immunotherapy. While viral and non-viral carriers exist, low gene transfer efficiency persists with non-viral methods. We present a peptide-based carrier (MiRGD) for gene delivery to diverse immune cells. The MiRGD/plasmid complex formation was characterized via gel retardation, dynamic light scattering, and zeta potential analysis. After safety and efficiency optimization in HEK293T cells, MiRGD achieved 69 % chimeric antigen receptor (CAR) transfection in Jurkat T cells (>98 % viability) and 28 % in primary human T cells. Dendritic cells showed 61 % transfection with >85 % viability. In vivo, MiRGD functioned as a DNA vaccine against SARS-CoV-2, eliciting robust antibody titers, neutralization, and safe histopathology. These results demonstrate MiRGD's efficacy and biocompatibility for immune cell engineering (T cells, dendritic cells, macrophages) and vaccination, offering a cost-effective, non-toxic platform for immunotherapy applications.</div></div>","PeriodicalId":19050,"journal":{"name":"Nanomedicine : nanotechnology, biology, and medicine","volume":"68 ","pages":"Article 102837"},"PeriodicalIF":4.2,"publicationDate":"2025-06-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144322453","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-06-13DOI: 10.1016/j.nano.2025.102834
Juntao Tan MD , Daqing Zhu MD , Guobiao Li MD , Hai Hu MD , Zongqiang Lai MD , Zhihua Li MD
Background
Triple-negative breast cancer (TNBC) lacks effective targeted therapies due to absent hormone receptors and HER2 expression, often resulting in poor prognosis. This study developed a theranostic system, AptPD-L1-FSNPs, combining PD-L1 aptamers with fluorescent silica nanoparticles (FSNPs) for targeted imaging and therapy in TNBC.
Methods
PD-L1 aptamers were conjugated to FSNPs, forming AptPD-L1-FSNPs. In vitro binding was evaluated using PD-L1-positive TNBC cells and negative controls. In vivo tumor targeting and biodistribution were assessed via fluorescence imaging in TNBC-bearing mice. Therapeutic efficacy was measured by tumor growth inhibition, survival, and apoptosis, with toxicity assessed in major organs.
Results
AptPD-L1-FSNPs showed high specificity to PD-L1-expressing TNBC cells and prolonged tumor retention in vivo. Treatment led to reduced tumor growth, increased apoptosis, and improved survival with minimal toxicity.
Conclusion
AptPD-L1-FSNPs offer targeted TNBC imaging and therapeutic potential, demonstrating promise for future clinical applications in personalized cancer treatment.
{"title":"A novel theranostic system of PD-L1-Aptamer-functionalized fluorescent silica nanoparticles for triple-negative breast cancer","authors":"Juntao Tan MD , Daqing Zhu MD , Guobiao Li MD , Hai Hu MD , Zongqiang Lai MD , Zhihua Li MD","doi":"10.1016/j.nano.2025.102834","DOIUrl":"10.1016/j.nano.2025.102834","url":null,"abstract":"<div><h3>Background</h3><div>Triple-negative breast cancer (TNBC) lacks effective targeted therapies due to absent hormone receptors and HER2 expression, often resulting in poor prognosis. This study developed a theranostic system, AptPD-L1-FSNPs, combining PD-L1 aptamers with fluorescent silica nanoparticles (FSNPs) for targeted imaging and therapy in TNBC.</div></div><div><h3>Methods</h3><div>PD-L1 aptamers were conjugated to FSNPs, forming AptPD-L1-FSNPs. <em>In vitro</em> binding was evaluated using PD-L1-positive TNBC cells and negative controls. <em>In vivo</em> tumor targeting and biodistribution were assessed <em>via</em> fluorescence imaging in TNBC-bearing mice. Therapeutic efficacy was measured by tumor growth inhibition, survival, and apoptosis, with toxicity assessed in major organs.</div></div><div><h3>Results</h3><div>AptPD-L1-FSNPs showed high specificity to PD-L1-expressing TNBC cells and prolonged tumor retention <em>in vivo</em>. Treatment led to reduced tumor growth, increased apoptosis, and improved survival with minimal toxicity.</div></div><div><h3>Conclusion</h3><div>AptPD-L1-FSNPs offer targeted TNBC imaging and therapeutic potential, demonstrating promise for future clinical applications in personalized cancer treatment.</div></div>","PeriodicalId":19050,"journal":{"name":"Nanomedicine : nanotechnology, biology, and medicine","volume":"68 ","pages":"Article 102834"},"PeriodicalIF":4.2,"publicationDate":"2025-06-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144291512","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-06-12DOI: 10.1016/j.nano.2025.102831
Ammar Alhasan PhD , S.F. Abdul Sani PhD , Hairul Anuar Tajuddin PhD , Tammar Hussein Ali PhD
Medical imaging plays a pivotal role in disease screening, early detection, and diagnosis. Among the various imaging modalities, computed tomography (CT) is one of the most widely utilized in clinical practice, offering high-resolution anatomical images critical for disease investigation. To enhance the visibility of tissues with similar densities, contrast agents are often required. Iodinated contrast agents, the most commonly used, are effective but have significant limitations, including short circulation times, the need for high-concentration injections, restricted tissue targeting, and potential side effects such as nephrotoxicity. These challenges have spurred the development of next-generation contrast agents. Nanostructured materials, particularly nanoparticles and quantum dots, have emerged as promising alternatives due to their superior X-ray attenuation, extended circulation times, and potential for multi-modal imaging applications such as CT/MRI and CT/fluorescence. Their unique properties, including small size, large surface area, and tunable functionalization enable targeted imaging and reduced side effects, making them ideal candidates for advanced diagnostics. This review highlights the recent advancements in synthesizing and optimizing nanostructured contrast agents based on their elemental composition, synthesis techniques, and imaging properties. It underscores the transformative potential of nano-based agents in enhancing diagnostic accuracy while minimizing adverse effects, marking a significant step forward in medical imaging technology.
{"title":"Development of nanoparticles and quantum dots as alternatives to iodinated contrast agents for mono-modal and bi-modal computed tomography imaging","authors":"Ammar Alhasan PhD , S.F. Abdul Sani PhD , Hairul Anuar Tajuddin PhD , Tammar Hussein Ali PhD","doi":"10.1016/j.nano.2025.102831","DOIUrl":"10.1016/j.nano.2025.102831","url":null,"abstract":"<div><div>Medical imaging plays a pivotal role in disease screening, early detection, and diagnosis. Among the various imaging modalities, computed tomography (CT) is one of the most widely utilized in clinical practice, offering high-resolution anatomical images critical for disease investigation. To enhance the visibility of tissues with similar densities, contrast agents are often required. Iodinated contrast agents, the most commonly used, are effective but have significant limitations, including short circulation times, the need for high-concentration injections, restricted tissue targeting, and potential side effects such as nephrotoxicity. These challenges have spurred the development of next-generation contrast agents. Nanostructured materials, particularly nanoparticles and quantum dots, have emerged as promising alternatives due to their superior X-ray attenuation, extended circulation times, and potential for multi-modal imaging applications such as CT/MRI and CT/fluorescence. Their unique properties, including small size, large surface area, and tunable functionalization enable targeted imaging and reduced side effects, making them ideal candidates for advanced diagnostics. This review highlights the recent advancements in synthesizing and optimizing nanostructured contrast agents based on their elemental composition, synthesis techniques, and imaging properties. It underscores the transformative potential of nano-based agents in enhancing diagnostic accuracy while minimizing adverse effects, marking a significant step forward in medical imaging technology.</div></div>","PeriodicalId":19050,"journal":{"name":"Nanomedicine : nanotechnology, biology, and medicine","volume":"68 ","pages":"Article 102831"},"PeriodicalIF":4.2,"publicationDate":"2025-06-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144294140","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-06-12DOI: 10.1016/j.nano.2025.102832
Ph.D Chunjing Guo , MD Min Cao , MD Ningning Diao , MD Wenxin Wang , MD Hongxu Geng , MD Yanguo Su , BD Tianying Sun , BD Xinyue Lu , Ph.D Ming Kong , Ph.D Daquan Chen
{"title":"Corrigendum to “novel pH-responsive E-selectin targeting natural polysaccharides hybrid micelles for diabetic nephropathy” [nanomedicine: nanotechnology, biology and medicine, volume 52, august 2023, 102,696]","authors":"Ph.D Chunjing Guo , MD Min Cao , MD Ningning Diao , MD Wenxin Wang , MD Hongxu Geng , MD Yanguo Su , BD Tianying Sun , BD Xinyue Lu , Ph.D Ming Kong , Ph.D Daquan Chen","doi":"10.1016/j.nano.2025.102832","DOIUrl":"10.1016/j.nano.2025.102832","url":null,"abstract":"","PeriodicalId":19050,"journal":{"name":"Nanomedicine : nanotechnology, biology, and medicine","volume":"67 ","pages":"Article 102832"},"PeriodicalIF":4.2,"publicationDate":"2025-06-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144263371","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-06-10DOI: 10.1016/j.nano.2025.102836
Dr. Mingfa Xie, Dr. Shijie Yuan, Dr. Guangsong Li, Prof. Hongjian Peng
Conjugates based on photosensitizer Ce6 and chemotherapeutic drug chrysin, when dispersed into water with DMSO, can rapidly self-assemble into nanoparticles. In Ce6-TEGDM-Chrysin, the two triethylene glycol monomethyl ether (TEGDM) chains enhance molecular polarity and hydrophilicity. Notably, one of the TEGDM chains extends toward the porphyrin ring plane, forming a wrapping configuration that increases steric hindrance to π-π stacking on the molecular plane. As a novel photosensitizer, Ce6-TEGDM-Chrysin exhibits outstanding photophysical properties, with a fluorescence lifetime of 3.10 ns, a fluorescence quantum yield of 18.3 %, and a singlet oxygen quantum yield of 46.2 % in DCM. Compared to Ce6-OMe-Chrysin as well as the co-assembled nanoparticle Ce6@Chrysin of Ce6 and chrysin, Ce6-TEGDM-Chrysin not only demonstrates superior photodynamic activity against melanoma but also exhibits a strong enrichment ability in mouse tumor tissues due to the EPR effect of nanodrugs and the inherent tumor affinity of porphyrins.
{"title":"Self-assembled nanomedicine of the conjugate based on Ce6 and chrysin improves photodynamic performance","authors":"Dr. Mingfa Xie, Dr. Shijie Yuan, Dr. Guangsong Li, Prof. Hongjian Peng","doi":"10.1016/j.nano.2025.102836","DOIUrl":"10.1016/j.nano.2025.102836","url":null,"abstract":"<div><div>Conjugates based on photosensitizer Ce6 and chemotherapeutic drug chrysin, when dispersed into water with DMSO, can rapidly self-assemble into nanoparticles. In Ce6-TEGDM-Chrysin, the two triethylene glycol monomethyl ether (TEGDM) chains enhance molecular polarity and hydrophilicity. Notably, one of the TEGDM chains extends toward the porphyrin ring plane, forming a wrapping configuration that increases steric hindrance to π-π stacking on the molecular plane. As a novel photosensitizer, Ce6-TEGDM-Chrysin exhibits outstanding photophysical properties, with a fluorescence lifetime of 3.10 ns, a fluorescence quantum yield of 18.3 %, and a singlet oxygen quantum yield of 46.2 % in DCM. Compared to Ce6-OMe-Chrysin as well as the co-assembled nanoparticle Ce6@Chrysin of Ce6 and chrysin, Ce6-TEGDM-Chrysin not only demonstrates superior photodynamic activity against melanoma but also exhibits a strong enrichment ability in mouse tumor tissues due to the EPR effect of nanodrugs and the inherent tumor affinity of porphyrins.</div></div>","PeriodicalId":19050,"journal":{"name":"Nanomedicine : nanotechnology, biology, and medicine","volume":"68 ","pages":"Article 102836"},"PeriodicalIF":4.2,"publicationDate":"2025-06-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144285769","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
We had previously examined the use of radioactive technetium-99m (Tc-99m)-labelled lactoferrin nanoparticles (LF-NPs) for sentinel lymph node (SLN) mapping. Compared with commercial tracer based on human serum albumin, LF-NPs exhibited better size uniformity and reduced batch variation. However, while in vitro tests with 99mTc-LF-NPs in RAW 264.7 macrophages were promising, the in vivo results revealed poor accumulation in the SLNs. To improve their in vivo performance, we performed surface modification of LF-NPs with different agents, including polyethylene glycol (PEG). Characterisation studies revealed that PEGylated LF-NPs (LF-NP@PEG) were the most effective. In vitro tests revealed significantly greater cellular uptake of LF-NP@PEG than unmodified LF-NPs. In vivo evaluation in animal model demonstrated increased SLN uptake and retention, which was supported by scintigraphic imaging studies. Although further refinements are needed, these findings suggest potential application for modified LF-NPs in SLN detection.
{"title":"Surface-modified 99mTc-Lactoferrin nanoparticles as tracers for sentinel lymph node mapping","authors":"Sanjay Kulkarni PhD , Anuj Kumar MSc , Soji Soman PhD , Abhijeet Pandey PhD , Suresh Subramanian PhD , Srinivas Mutalik PhD","doi":"10.1016/j.nano.2025.102835","DOIUrl":"10.1016/j.nano.2025.102835","url":null,"abstract":"<div><div>We had previously examined the use of radioactive technetium-99m (Tc-99m)-labelled lactoferrin nanoparticles (LF-NPs) for sentinel lymph node (SLN) mapping. Compared with commercial tracer based on human serum albumin, LF-NPs exhibited better size uniformity and reduced batch variation. However, while in vitro tests with <sup>99m</sup>Tc-LF-NPs in RAW 264.7 macrophages were promising, the in vivo results revealed poor accumulation in the SLNs. To improve their in vivo performance, we performed surface modification of LF-NPs with different agents, including polyethylene glycol (PEG). Characterisation studies revealed that PEGylated LF-NPs (LF-NP@PEG) were the most effective. In vitro tests revealed significantly greater cellular uptake of LF-NP@PEG than unmodified LF-NPs. In vivo evaluation in animal model demonstrated increased SLN uptake and retention, which was supported by scintigraphic imaging studies. Although further refinements are needed, these findings suggest potential application for modified LF-NPs in SLN detection.</div></div>","PeriodicalId":19050,"journal":{"name":"Nanomedicine : nanotechnology, biology, and medicine","volume":"68 ","pages":"Article 102835"},"PeriodicalIF":4.2,"publicationDate":"2025-06-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144285770","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-06-05DOI: 10.1016/j.nano.2025.102833
Man Li PhD, Yuting Yang PhD, Jiaojie Wei Master of Science, Xingli Cun PhD, Zhengze Lu PhD, Yue Qiu PhD, Zhirong Zhang PhD, Qin He PhD
{"title":"Corrigendum to “enhanced chemo-immunotherapy against melanoma by inhibition of cholesterol esterification in CD8+ T cells” [nanomedicine: nanotechnology, biology, and medicine 14 (2018) 2541–2550]","authors":"Man Li PhD, Yuting Yang PhD, Jiaojie Wei Master of Science, Xingli Cun PhD, Zhengze Lu PhD, Yue Qiu PhD, Zhirong Zhang PhD, Qin He PhD","doi":"10.1016/j.nano.2025.102833","DOIUrl":"10.1016/j.nano.2025.102833","url":null,"abstract":"","PeriodicalId":19050,"journal":{"name":"Nanomedicine : nanotechnology, biology, and medicine","volume":"67 ","pages":"Article 102833"},"PeriodicalIF":4.2,"publicationDate":"2025-06-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144221376","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-06-02DOI: 10.1016/j.nano.2025.102830
MD Yanguo Su , MD Chunjing Guo , MD Qiang Chena , MD Huimin Guo , BD Jinqiu Wang , BD Kaihang Mu , Ph.D Daquan Chen
{"title":"Corrigendum to “Construction of bionanoparticles based on Angelica polysaccharides for the treatment of stroke” [Nanomed: Nanotechnol Biol Med, volume 44, August 2022, 102570]","authors":"MD Yanguo Su , MD Chunjing Guo , MD Qiang Chena , MD Huimin Guo , BD Jinqiu Wang , BD Kaihang Mu , Ph.D Daquan Chen","doi":"10.1016/j.nano.2025.102830","DOIUrl":"10.1016/j.nano.2025.102830","url":null,"abstract":"","PeriodicalId":19050,"journal":{"name":"Nanomedicine : nanotechnology, biology, and medicine","volume":"67 ","pages":"Article 102830"},"PeriodicalIF":4.2,"publicationDate":"2025-06-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144189810","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-05-22DOI: 10.1016/j.nano.2025.102829
Xiangning Luo BS , Renli Luo MS , Yuanyuan Zhou BS , Yuanpeng Jiang BS , Cong Han BS , Aiguo Song PhD , Kun Qian PhD , Chunrong Qu PhD , Rui Cao PhD , Bin Xu PhD , Zhen Cheng PhD
Gastrin-releasing peptide receptor (GRPR) is overexpressed in most prostate cancers (PCa) and is a potential target in diagnosis and treatment. In this study, based on the previously reported GRPR antagonist RM26 and novel chelating agent Dar derivatives, we designed and evaluated two radiopharmaceuticals, [68Ga]Ga-Dar-C5-P2-RM26 and [68Ga]Ga-Dar-P2-RM26. Both radiotracers were easily prepared at room temperature and showed high radiochemical stability in phosphate-buffered saline (PBS) and fetal bovine serum (FBS). Cellular and animal experiments indicated that the two radiotracers exhibited specific tumor uptakes in PC-3 xenograft mice models. Specifically, [68Ga]Ga-Dar-C5-P2-RM26 and [68Ga]Ga-Dar-P2-RM26 displayed 6.617 ± 0.245 % ID/g and 5.973 ± 1.261 % ID/g tumor uptake, respectively. Positron emission tomography/ computer tomography (PET/CT) imaging results indicated that these two radiotracers showed excellent tumor-to-background contrast at 0.5 h, 1 h, and 2 h post intravenous injection (p.i.). In summary, [68Ga]Ga-Dar-C5-RM26 and [68Ga]Ga-Dar-RM26 are GRPR-targeted radiotracers with high potential for clinical translation in tumor-targeted imaging.
{"title":"Design and synthesis of GRPR-targeted PET probes based on Dar derivatives for imaging of prostate cancer","authors":"Xiangning Luo BS , Renli Luo MS , Yuanyuan Zhou BS , Yuanpeng Jiang BS , Cong Han BS , Aiguo Song PhD , Kun Qian PhD , Chunrong Qu PhD , Rui Cao PhD , Bin Xu PhD , Zhen Cheng PhD","doi":"10.1016/j.nano.2025.102829","DOIUrl":"10.1016/j.nano.2025.102829","url":null,"abstract":"<div><div>Gastrin-releasing peptide receptor (GRPR) is overexpressed in most prostate cancers (PCa) and is a potential target in diagnosis and treatment. In this study, based on the previously reported GRPR antagonist RM26 and novel chelating agent Dar derivatives, we designed and evaluated two radiopharmaceuticals, [<sup>68</sup>Ga]Ga-Dar-C5-P2-RM26 and [<sup>68</sup>Ga]Ga-Dar-P2-RM26. Both radiotracers were easily prepared at room temperature and showed high radiochemical stability in phosphate-buffered saline (PBS) and fetal bovine serum (FBS). Cellular and animal experiments indicated that the two radiotracers exhibited specific tumor uptakes in PC-3 xenograft mice models. Specifically, [<sup>68</sup>Ga]Ga-Dar-C5-P2-RM26 and [<sup>68</sup>Ga]Ga-Dar-P2-RM26 displayed 6.617 ± 0.245 % ID/g and 5.973 ± 1.261 % ID/g tumor uptake, respectively. Positron emission tomography/ computer tomography (PET/CT) imaging results indicated that these two radiotracers showed excellent tumor-to-background contrast at 0.5 h, 1 h, and 2 h post intravenous injection (p.i.). In summary, [<sup>68</sup>Ga]Ga-Dar-C5-RM26 and [<sup>68</sup>Ga]Ga-Dar-RM26 are GRPR-targeted radiotracers with high potential for clinical translation in tumor-targeted imaging.</div></div>","PeriodicalId":19050,"journal":{"name":"Nanomedicine : nanotechnology, biology, and medicine","volume":"67 ","pages":"Article 102829"},"PeriodicalIF":4.2,"publicationDate":"2025-05-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144134453","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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