1. Institute of Chemistry and Biochemistry, Freie Universit?t Berlin, Berlin, Germany;2. Institute of Radiopharmaceutical Cancer Research, Helmholtz‐Zentrum Dresden – Rossendorf (HZDR), Dresden, Germany
Abstract:
Here, the synthesis and characterization of three improved nanosystems is presented based on amino functionalized hyperbranched polyglycerol (hPG; Mw = 16.8 kDa) as potential copper(ii ) chelators. The ligands, N‐methyl‐N‐picolylglycine amide, 2,6‐pyridine dicarboxylic acid monoamide, and cyclam tetraacetic acid (TETA) monoamide, are covalently attached to the polymer with amide bonds. In this paper, the Cu(ii ) loading capacity, the stability of the Cu(ii )‐loaded carriers at different pHs, with competing ligands and in human serum, as well as the transport of Cu(ii ) in biological systems are investigated. For the first time, a different cytotoxicity of functionalized polymer nanoparticles with and without Cu(ii ) is observed. The cyclam‐based carrier combines the highest loading capacity (29 Cu ions/nanoparticle), best stability with respect to pH and EDTA (45% remaining Cu after 24 h), lowest cytotoxicity (IC50 > 100 × 10?6m (unloaded), 1500 × 10?6m Cu(ii ); Cu:carrier 29:1), and the highest stability in human serum.
