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Mol Pharm ; 15(2): 536-547, 2018 02 05.
Article in English | MEDLINE | ID: mdl-29298480

ABSTRACT

The biodistribution of dendronized iron oxides, NPs10@D1_DOTAGA and melanin-targeting NPs10@D1_ICF_DOTAGA, was studied in vivo using magnetic resonance imaging (MRI) and planar scintigraphy through [177Lu]Lu-radiolabeling. MRI experiments showed high contrast power of both dendronized nanoparticles (DPs) and hepatobiliary and urinary excretions. Little tumor uptake could be highlighted after intravenous injection probably as a consequence of the negatively charged DOTAGA-derivatized shell, which reduces the diffusion across the cells' membrane. Planar scintigraphy images demonstrated a moderate specific tumor uptake of melanoma-targeted [177Lu]Lu-NPs10@D1_ICF_DOTAGA at 2 h post-intravenous injection (pi), and the highest tumor uptake of the control probe [177Lu]Lu-NPs10@D1_DOTAGA at 30 min pi, probably due to the enhanced permeability and retention effect. In addition, ex vivo confocal microscopy studies showed a high specific targeting of human melanoma samples impregnated with NPs10@D1_ICF_Alexa647_ DOTAGA.


Subject(s)
Melanins/metabolism , Melanoma/diagnostic imaging , Nanoparticles/chemistry , Radiopharmaceuticals/administration & dosage , Skin Neoplasms/diagnostic imaging , Animals , Biopsy , Cell Line, Tumor/transplantation , Humans , Injections, Intravenous , Lutetium/chemistry , Magnetic Resonance Imaging , Male , Melanoma/pathology , Mice , Microscopy, Confocal , Nanoparticles/administration & dosage , Polymers/administration & dosage , Polymers/chemistry , Radioisotopes/chemistry , Radionuclide Imaging , Radiopharmaceuticals/chemistry , Skin/diagnostic imaging , Skin/pathology , Skin Neoplasms/pathology , Tissue Distribution
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