In Vivo Imaging of [60]Fullerene-Based Molecular Spherical Nucleic Acids by Positron Emission Tomography
18F-Labeled [60]fullerene-based molecular spherical nucleic acids (MSNAs), consisting of a human epidermal growth factor receptor 2 (HER2) mRNA antisense oligonucleotide sequence with a native phosphodiester and phosphorothioate backbone, were synthesized, site-specifically labeled with a positron...
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| Published in | Molecular pharmaceutics Vol. 20; no. 10; pp. 5043 - 5051 |
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| Main Authors | , , , , , , , , , , , |
| Format | Journal Article |
| Language | English |
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American Chemical Society
02.10.2023
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| Abstract | 18F-Labeled [60]fullerene-based molecular spherical nucleic acids (MSNAs), consisting of a human epidermal growth factor receptor 2 (HER2) mRNA antisense oligonucleotide sequence with a native phosphodiester and phosphorothioate backbone, were synthesized, site-specifically labeled with a positron emitting fluorine-18 and intravenously administrated via tail vein to HER2 expressing HCC1954 tumor-bearing mice. The biodistribution of the MSNAs was monitored in vivo by positron emission tomography/computed tomography (PET/CT) imaging. MSNA with a native phosphodiester backbone (MSNA-PO) was prone to rapid nuclease-mediated degradation, whereas the corresponding phosphorothioate analogue (MSNA-PS) with improved enzymatic stability showed an interesting biodistribution profile in vivo. One hour after the injection, majority of the radioactivity was observed in spleen and liver but also in blood with an average tumor-to-muscle ratio of 2. The prolonged radioactivity in blood circulation may open possibilities to the targeted delivery of the MSNAs. |
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| AbstractList | 18
F-Labeled [60]fullerene-based molecular
spherical
nucleic acids (MSNAs), consisting of a human epidermal growth factor
receptor 2 (HER2) mRNA antisense oligonucleotide sequence with a native
phosphodiester and phosphorothioate backbone, were synthesized, site-specifically
labeled with a positron emitting fluorine-18 and intravenously administrated
via tail vein to HER2 expressing HCC1954 tumor-bearing mice. The biodistribution
of the MSNAs was monitored
in vivo
by positron emission
tomography/computed tomography (PET/CT) imaging. MSNA with a native
phosphodiester backbone (MSNA-PO) was prone to rapid nuclease-mediated
degradation, whereas the corresponding phosphorothioate analogue (MSNA-PS)
with improved enzymatic stability showed an interesting biodistribution
profile
in vivo
. One hour after the injection, majority
of the radioactivity was observed in spleen and liver but also in
blood with an average tumor-to-muscle ratio of 2. The prolonged radioactivity
in blood circulation may open possibilities to the targeted delivery
of the MSNAs. 18F-Labeled [60]fullerene-based molecular spherical nucleic acids (MSNAs), consisting of a human epidermal growth factor receptor 2 (HER2) mRNA antisense oligonucleotide sequence with a native phosphodiester and phosphorothioate backbone, were synthesized, site-specifically labeled with a positron emitting fluorine-18 and intravenously administrated via tail vein to HER2 expressing HCC1954 tumor-bearing mice. The biodistribution of the MSNAs was monitored in vivo by positron emission tomography/computed tomography (PET/CT) imaging. MSNA with a native phosphodiester backbone (MSNA-PO) was prone to rapid nuclease-mediated degradation, whereas the corresponding phosphorothioate analogue (MSNA-PS) with improved enzymatic stability showed an interesting biodistribution profile in vivo. One hour after the injection, majority of the radioactivity was observed in spleen and liver but also in blood with an average tumor-to-muscle ratio of 2. The prolonged radioactivity in blood circulation may open possibilities to the targeted delivery of the MSNAs. F-Labeled [60]fullerene-based molecular spherical nucleic acids (MSNAs), consisting of a human epidermal growth factor receptor 2 (HER2) mRNA antisense oligonucleotide sequence with a native phosphodiester and phosphorothioate backbone, were synthesized, site-specifically labeled with a positron emitting fluorine-18 and intravenously administrated via tail vein to HER2 expressing HCC1954 tumor-bearing mice. The biodistribution of the MSNAs was monitored by positron emission tomography/computed tomography (PET/CT) imaging. MSNA with a native phosphodiester backbone (MSNA-PO) was prone to rapid nuclease-mediated degradation, whereas the corresponding phosphorothioate analogue (MSNA-PS) with improved enzymatic stability showed an interesting biodistribution profile . One hour after the injection, majority of the radioactivity was observed in spleen and liver but also in blood with an average tumor-to-muscle ratio of 2. The prolonged radioactivity in blood circulation may open possibilities to the targeted delivery of the MSNAs. |
| Author | Roivainen, Anne Moisio, Olli Rajander, Johan Salo, Harri Airaksinen, Anu J. Iqbal, Imran Virta, Pasi Äärelä, Antti Auchynnikava, Tatsiana Liljenbäck, Heidi Lehtimäki, Jyrki Andriana, Putri |
| AuthorAffiliation | Department of Chemistry Accelerator Laboratory Åbo Akademi University Turku Center for Disease Modeling Research and Development, Orion Pharma Turku PET Centre Turku University Hospital |
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| Snippet | 18F-Labeled [60]fullerene-based molecular spherical nucleic acids (MSNAs), consisting of a human epidermal growth factor receptor 2 (HER2) mRNA antisense... F-Labeled [60]fullerene-based molecular spherical nucleic acids (MSNAs), consisting of a human epidermal growth factor receptor 2 (HER2) mRNA antisense... 18 F-Labeled [60]fullerene-based molecular spherical nucleic acids (MSNAs), consisting of a human epidermal growth factor receptor 2 (HER2) mRNA antisense... |
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| Title | In Vivo Imaging of [60]Fullerene-Based Molecular Spherical Nucleic Acids by Positron Emission Tomography |
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