title: Inulin-based polymer coated SPIONs as potential drug delivery systems for targeted cancer therapy.
abstract: This paper deal with the synthesis and characterization of PEGylated squalene-grafted-inulin amphiphile capable of self-assembling and self-organizing into nanocarriers once placed in aqueous media. It was exploited as coating agent for obtaining doxorubicin loaded superparamagnetic iron oxide nanoparticles (SPIONs) endowed with stealth like behavior and excellent physicochemical stability. Inulin was firstly modified in the side chain with primary amine groups, followed in turn by conjugation with squalenoyl derivatives through common amidic coupling agents and PEGylation by imine linkage. Polymer coated SPIONs were so obtained by spontaneous self-assembling of inulin copolymer onto magnetite surface involving hydrophobic-hydrophobic interactions between the metallic core and the squalene moieties. The system was characterized in terms of hydrodynamic radius, zeta potential, shape and drug loading capacity. On the whole, the stealth-like shell stabilized the suspension in aqueous media, though allowing the release of the doxorubicin loaded in therapeutic range. The cytotoxicity profile on cancer (HCT116) cell line and in vitro drug uptake were evaluated both with and without an external magnetic field used as targeting agent and uptake promoter, displaying that magnetic targeting implies advantageous therapeutic effects, that is amplified drug uptake and increased anticancer activity throughout the tumor mass.
authors.affiliation: Laboratory of Biocompatible Polymers, Department of "Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche" (STEBICEF), University of Palermo, Palermo, Italy.
authors.forename: C
authors.initials: C
authors.lastname: Scialabba
authors.affiliation: Laboratory of Biocompatible Polymers, Department of "Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche" (STEBICEF), University of Palermo, Palermo, Italy. Electronic address: mariano.licciardi@unipa.it.
authors.forename: M
authors.initials: M
authors.lastname: Licciardi
authors.affiliation: Laboratory of Biocompatible Polymers, Department of "Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche" (STEBICEF), University of Palermo, Palermo, Italy.
authors.forename: N
authors.initials: N
authors.lastname: Mauro
authors.affiliation: Department of Scienza e Tecnologia del Farmaco, University of Torino, Torino, Italy.
authors.forename: F
authors.initials: F
authors.lastname: Rocco
authors.affiliation: Department of Scienza e Tecnologia del Farmaco, University of Torino, Torino, Italy.
authors.forename: M
authors.initials: M
authors.lastname: Ceruti
authors.affiliation: Laboratory of Biocompatible Polymers, Department of "Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche" (STEBICEF), University of Palermo, Palermo, Italy.
authors.forename: G
authors.initials: G
authors.lastname: Giammona
mesh_terms: D000903:Antibiotics, Antineoplastic / Q000008:administration & dosage*; D002470:Cell Survival / Q000187:drug effects; D004317:Doxorubicin / Q000008:administration & dosage*; D004337:Drug Carriers / Q000737:chemistry*; D065546:Drug Liberation; D045325:HCT116 Cells; D006801:Humans; D007444:Inulin / Q000737:chemistry*; D058185:Magnetite Nanoparticles / Q000737:chemistry*; D008855:Microscopy, Electron, Scanning; D015394:Molecular Structure; D010316:Particle Size; D011108:Polymers / Q000737:chemistry*; D017550:Spectroscopy, Fourier Transform Infrared; D013499:Surface Properties
chemical_list: D000903:Antibiotics, Antineoplastic; D004337:Drug Carriers; D058185:Magnetite Nanoparticles; D011108:Polymers; D004317:Doxorubicin; D007444:Inulin
keywords: Doxorubicin; Inulin copolymer; Magnetic targeting; Pegylated; SPIONs; Squalene