Micellar Iron Oxide Nanoparticles Coated with Anti-Tumor Glycosides.
Author: Groult, Hugo; García Álvarez, Isabel; Romero Ramírez, Lorenzo; Nieto Sampedro, Manuel; Herranz, Fernando; Fernández Mayoralas, Alfonso; Ruiz Cabello, Jesús
Abstract: The synthesis procedure of nanoparticles based on thermal degradation produces
organic solvent dispersible iron oxide nanoparticles (OA-IONP) with oleic acid coating and
unique physicochemical properties of the core. Some glycosides with hydrophilic sugar moieties
bound to oleyl hydrophobic chains have antimitotic activity on cancer cells but reduced in vivo
applications because of the intrinsic low solubility in physiological media, and are prone to enzymatic
hydrolysis. In this manuscript, we have synthetized and characterized OA-IONP-based micelles
encapsulated within amphiphilic bioactive glycosides. The glycoside-coated IONP micelles were
tested as Magnetic Resonance Imaging (MRI) contrast agents as well as antimitotics on rat glioma
(C6) and human lung carcinoma (A549) cell lines. Micelle antimitotic activity was compared with the
activity of the corresponding free glycosides. In general, all OA-IONP-based micellar formulations
of these glycosides maintained their anti-tumor effects, and, in one case, showed an unusual
therapeutic improvement. Finally, the micelles presented optimal relaxometric properties for their
use as T2-weighed MRI contrast agents. Our results suggest that these bioactive hydrophilic
nano-formulations are theranostic agents with synergistic properties obtained from two entities,
which separately are not ready for in vivo applications, and strengthen the possibility of using
biomolecules as both a coating for OA-IONP micellar stabilization and as drugs for therapy.
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