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Idarubicin-Gold Complex: From Crystal Growth to Gold Nanoparticles
Carole Barbey1, Nadia Bouchemal1, Pascal Retailleau2
1CNRS, UMR 7244, NBD-CSPBAT, Laboratoire de Chimie, Structures et Propriétés de Biomatériaux et d'Agents Thérapeutiques Université Sorbonne Paris Nord, 1 Rue de Chablis, Bobigny 93000, France.
None:
Idarubicin (IDA) is the analog of daunorubicin (DNR). The absence of the methoxy group at position 4 of IDA remarkably improved lipophilicity, which is responsible for extra cellular uptake, higher DNA-binding ability, and considerable cytotoxicity in correlation with doxorubicin (DOX) and DNR. In this paper, we conceived two principal objectives: we realized the crystal structure of IDA by X-ray diffraction measurements on single crystals at room temperature (monoclinic, space group P21, a = 5.1302(2) Å, b = 9.9122(5) Å, c = 24.8868(11) Å; β = 91.425(4)°; V = 1265.14(10) Å3) with refinements of the structure converged to the final R = 3.87%. The second objective has been to develop gold nanoparticles encapsulated with idarubicin through an original methodology in which gold salt (HAuCl4) is chelated with IDA and diacid polymer (PEG) to form hybrid nanoparticles called IDA IN PEG-AuNPs in which drug solubility was enhanced. The computational studies were in agreement with the experimental observations. These hybrid nanoparticles and their precursors were analyzed by Raman, UV-Vis, 1H NMR, and transmission electron microscopy (TEM). The main results are completed by a theoretical approach to understand the whole process.
