Radiolabeled Nanogels for Nuclear Molecular Imaging

• Published in: Macromolecular rapid communications. Vol. 34; no. 7; pp. 562 - 567
• Main Authors: Singh, Smriti, Bingöl, Bahar, Morgenroth, Agnieszka, Mottaghy, Felix M., Möller, Martin, Schmaljohann, Jörn
• Format: Journal Article
• Language: English
• Published: Weinheim WILEY-VCH Verlag 12.04.2013; WILEY‐VCH Verlag; Wiley; Wiley Subscription Services, Inc
• Subjects: Applied sciences; Biocompatibility; Biological and medical sciences; Chelating; Exact sciences and technology; Gallium Radioisotopes - chemistry; Gallium-68; Humans; Imaging; Investigative techniques, diagnostic techniques (general aspects); Isotope Labeling; Macrophages - chemistry; Medical sciences; Miscellaneous. Technology; Molecular Imaging - instrumentation; Nanocomposites; nanogels; Nanomaterials; Nanostructure; Organic polymers; Phagocytosis; Physicochemistry of polymers; poly(ethylene glycol); Polyethylene Glycols - chemical synthesis; Polyethylene Glycols - chemistry; Polyethyleneimine - chemical synthesis; Polyethyleneimine - chemistry; positron emission tomography; Properties and characterization; Radionuclide investigations; Self assembly; Solution and gel properties; Gallium 68; Hydrogen peroxide; End group; Positron emitter; Mercaptoacid; Labelled copolymer; Nanogel; poly(ethylene glycol); Propylene oxide copolymer; Amphiphilic polymer; Michael addition; Radiolabelling; Nitrogen crown compound; Gelation; nanogels; Crosslinking; Ethylene oxide copolymer; Experimental study; Sulfur copolymer; Esterification; Star copolymer; self-assembly; Particle size distribution; Chemical modification; Waterproofness; Gallium-68; Internalization; Preparation; positron emission tomography; Macrophage
• ISSN: 1022-1336; 1521-3927
• DOI: 10.1002/marc.201200744

An efficient and simple synthesis approach to form stable 68Ga‐labeled nanogels is reported and their fundamental properties investigated. Nanogels are obtained by self‐assembly of amphiphilic statistical prepolymers derivatised with chelating groups for radiometals. The resulting nanogels exhibit a well‐defined spherical shape with a diameter of 290 ± 50 nm. The radionuclide 68Ga is chelated in high radiochemical yields in an aqueous medium at room temperature. The phagocytosis assay demonstrates a highly increased internalization of nanogels by activated macrophages. Access to these 68Ga‐nanogels will allow the investigation of general behavior and clearance pathways of nanogels in vivo by nuclear molecular imaging. Biodegradable nanogels are prepared by crosslinking of amphiphilic, thiol‐functionalized star shaped P(EO‐stat‐PO). Incorporation of NODAGA, a chelating agent, in the prepolymer enabled the radiolabeling of nanogels with 68Ga for the purpose of investigation the in vivo behavior of nanogels. Nanogels are biocompatible and only ingested by macrophage on upregulation of phagocytosis capacity.