Biodistribution of Modular Nanotransporter Carrying Auger Electron Emitter and Targeted at Melanoma Cells in Murine Tumor Modelстатья

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Дата последнего поиска статьи во внешних источниках: 27 марта 2018 г.

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[1] Biodistribution of modular nanotransporter carrying auger electron emitter and targeted at melanoma cells in murine tumor model / M. S. Vorontsova, N. B. Morozova, T. A. Karmakova et al. // Physics of Cancer: Interdisciplinary Problems and Clinical Application. American Institutes of Physics. AIP Conference Proceedings. — Vol. 1882. — United States: United States, 2017. — P. 020078–1–020078–4. Recombinant modular nanotransporter containing -melanocyte-stimulating hormone peptide sequence (MNT-MSH) as a ligand module was designed for nucleus-targeted delivery of cytotoxic agents into melanoma cells. MNT-MSH radiolabeled with Auger electron emitter (111In-NOTA–MNT-MSH) showed a high antitumor efficacy in mice bearing syngeneic melanoma after intratumoral (i.t.) injection. This study is aimed at evaluating the biodistribution of the radioconjugate in melanoma tumor model in vivo. 111In-NOTA–MNT-MSH was administered i.t. in C57Bl/6j mice bearing subcutaneously implanted B16-F1 murine melanoma cells, expressing high levels of MCR1. The tissue uptake of radioactivity was determined ex vivo by gamma-counter measurements. The intravenous route of administration did not provide a desirable level of radioactivity accumulation in the tumor, possibly, due to a high uptake of the transporter in liver tissue. After i.t. administration 111In-NOTA–MNT-MSH provided a high local retention of radionuclide, ranged from 400 to 350 %ID/g within at least 48 hours post-injection. MNT containing Auger electron emitter and alpha-MSH peptide as vector ligand could be a promising basis for radiopharmaceutical preparations intended for melanoma treatment. [ DOI ]

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