Evaluation of the Active Targeting of Melanin Granules after Intravenous Injection of Dendronized Nanoparticles.

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.
Authors	C Bordeianu, A Parat, S Piant, A Walter, C Zbaraszczuk-Affolter, F Meyer, S Begin-Colin, S Boutry, R N Muller, E Jouberton, J-M Chezal, B Labeille, E Cinotti, J-L Perrot, E Miot-Noirault, S Laurent, D Felder-Flesch
Journal	Molecular pharmaceutics (Mol Pharm) Vol. 15 Issue 2 Pg. 536-547 (02 05 2018) ISSN: 1543-8392 [Electronic] United States
PMID	29298480 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References	Melanins Polymers Radioisotopes Radiopharmaceuticals Lutetium Lutetium-177
Topics	Animals Biopsy Cell Line, Tumor (transplantation) Humans Injections, Intravenous Lutetium (chemistry) Magnetic Resonance Imaging Male Melanins (metabolism) Melanoma (diagnostic imaging, pathology) Mice Microscopy, Confocal Nanoparticles (administration & dosage, chemistry) Polymers (administration & dosage, chemistry) Radioisotopes (chemistry) Radionuclide Imaging Radiopharmaceuticals (administration & dosage, chemistry) Skin (diagnostic imaging, pathology) Skin Neoplasms (diagnostic imaging, pathology) Tissue Distribution

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