Mono(pyridine-N-oxide) DOTA analog and its G1/G4-PAMAM dendrimer conjugates labeled with 177Lu: Radiolabeling and biodistribution studies

Lázníčková, Alice; Biricova, V.; Lázníček, Milan; Hermann, Petr

doi:10.1016/j.apradiso.2013.10.021

Cited by 24 publications

(20 citation statements)

References 41 publications

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“…Recently, Laznickova et al (2014) have reported a successful radiolabeling of DOTA analog–G1/G4 PAMAM dendrimers conjugate with 177 Lu (beta emitting therapeutic radionuclide). These authors reported that G4 dendrimer conjugates modified on an average with 57 chelating units can be labeled with 177 Lu with high radionuclide purity and specific activity at 37 °C.…”

Section: Discussionmentioning

confidence: 99%

Radiolabeling optimization and characterization of 68 Ga labeled DOTA–polyamido-amine dendrimer conjugate – Animal biodistribution and PET imaging results

Ghai

Singh

Hazari

et al. 2015

Applied Radiation and Isotopes

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The present study describes the optimization of 68Ga radiolabeling with PAMAM dendrimer–DOTA conjugate. A conjugate (PAMAM–DOTA) concentration of 11.69 µM, provided best radiolabeling efficiency of more than 93.0% at pH 4.0, incubation time of 30.0 min and reaction temperature ranging between 90 and 100 °C. The decay corrected radiochemical yield was found to be 79.47 ± 0.01%. The radiolabeled preparation ([68Ga]-DOTA–PAMAM-D) remained stable (radiolabeling efficiency of 96.0%) at room temperature and in serum for up to 4-h. The plasma protein binding was observed to be 21.0%. After intravenous administration, 50.0% of the tracer cleared from the blood circulation by 30-min and less than 1.0% of the injected activity remained in blood by 1.0 h. The animal biodistribution studies demonstrated that the tracer excretes through the kidneys and about 0.33% of the %ID/g accumulated in the tumor at 1 h post injection. The animal organ's biodistribution data was supported by animal PET imaging showing good ‘non-specific’ tracer uptake in tumor and excretion is primarily through kidneys. Additionally, DOTA–PAMAM-D conjugation with αVβ3 receptors targeting peptides and drug loading on the dendrimers may improve the specificity of the 68Ga labeled product for imaging and treating angiogenesis respectively.

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Section: Discussionmentioning

confidence: 99%

Radiolabeling optimization and characterization of 68 Ga labeled DOTA–polyamido-amine dendrimer conjugate – Animal biodistribution and PET imaging results

Ghai

Singh

Hazari

et al. 2015

Applied Radiation and Isotopes

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“…177 Lu can mildly suppress the bone marrow growth and display the highest safety profile among all the therapeutic radionuclides, due to the fact that its β‐emission energy is relatively low and the average radiation range is only 670 µm in tissues . Laznickova et al conjugated G1 and G4 PAMAM dendrimers with 7.5 or 57 methylenepyridine‐ N ‐oxide pendant arm (DO3A‐py NO‐C ) as a chelating unit, respectively for labeling 177 Lu . The 177 Lu‐labeled G1/G4 dendrimer conjugates displayed a high specific activity and radiochemical purity at 37 °C.…”

Section: Radiolabeled Dendrimer‐based Nanodevices For Rt and Theranosmentioning

confidence: 99%

PAMAM Dendrimer‐Based Nanodevices for Nuclear Medicine Applications

Xiao

Shi

et al. 2019

Macromolecular Bioscience

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Nuclear medicine, involving nuclear medicine imaging and radiotherapy (RT), has become a mainstay of theranostics in the field of nanomedicine and several examples have been successfully translated into clinical practice. The combination of radionuclides with dendrimers has long been investigated in nuclear imaging, such as positron emission tomography (PET) and single‐photon emission computed tomography (SPECT), providing functional information for whole body quantitative analysis with high sensitivity due to the unique structural advantages of the dendrimer platform. Besides, radioisotopes with both therapeutic and imaging functionalities can also be combined with dendrimer platforms for theranostic applications. In this review, the recent advances in the development of radionuclide‐labeled poly(amidoamine) dendrimer‐based nanodevices for targeted PET, SPECT, SPECT/computed tomography, SPECT/magnetic resonance imaging of tumors, RT, as well as for SPECT‐imaging‐guided RT of cancer are summarized. Current restrictions hindering the clinical translation of dendrimer‐based nuclear nanodevices and future prospects are also discussed.

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“…DOTA and its derivatives are regularly used as chelators for 177 Lu radiolabeling. Recently, Laznickova et al reported that a DOTA analog with one methylene pyridine- N -oxide pendant arm (DO3A-py NO-C ) could serve as bifunctional chelators with stronger chelate ability than DTPA and EDTA [ 132 ]. In this study, 177 Lu labeled G1 and G4 dendrimer conjugates could be prepared with a high specific activity and radiochemical purity.…”

Section: Radiolabeled Dendrimers For Radionuclide Therapymentioning

confidence: 99%

Radiolabeled Dendrimers for Nuclear Medicine Applications

Zhao

Zhu

et al. 2017

Molecules

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Recent advances in nuclear medicine have explored nanoscale carriers for targeted delivery of various radionuclides in specific manners to improve the effect of diagnosis and therapy of diseases. Due to the unique molecular architecture allowing facile attachment of targeting ligands and radionuclides, dendrimers provide versatile platforms in this filed to build abundant multifunctional radiolabeled nanoparticles for nuclear medicine applications. This review gives special focus to recent advances in dendrimer-based nuclear medicine agents for the imaging and treatment of cancer, cardiovascular and other diseases. Radiolabeling strategies for different radionuclides and several challenges involved in clinical translation of radiolabeled dendrimers are extensively discussed.

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Mono(pyridine-N-oxide) DOTA analog and its G1/G4-PAMAM dendrimer conjugates labeled with 177Lu: Radiolabeling and biodistribution studies

Cited by 24 publications

References 41 publications

Radiolabeling optimization and characterization of 68 Ga labeled DOTA–polyamido-amine dendrimer conjugate – Animal biodistribution and PET imaging results

Radiolabeling optimization and characterization of 68 Ga labeled DOTA–polyamido-amine dendrimer conjugate – Animal biodistribution and PET imaging results

PAMAM Dendrimer‐Based Nanodevices for Nuclear Medicine Applications

Radiolabeled Dendrimers for Nuclear Medicine Applications

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