title: Nanoassemblies Based on Supramolecular Complexes of Nonionic Amphiphilic Cyclodextrin and Sorafenib as Effective Weapons to Kill Human HCC Cells.
abstract: Sorafenib (Sor), an effective chemiotherapeutic drug utilized against hepatocellular carcinoma (HCC), robustly interacts with nonionic amphiphilic cyclodextrin (aCD, SC6OH), forming, in aqueous solution, supramolecular complexes that behave as building blocks of highly water-dispersible colloidal nanoassemblies. SC6OH/Sor complex has been characterized by complementary spectroscopic techniques, such as UV-vis, steady-state fluorescence and anisotropy, resonance light scattering and (1)H NMR. The spectroscopic evidences and experiments carried out in the presence of an adamantane derivative, which competes with drug for CD cavity, agree with the entrapment of Sor in aCD, pointing out the role of the aCD cavity in the interaction between drug and amphiphile. Nanoassemblies based on SC6OH/Sor display size of ∼200 nm, negative zeta-potential (ζ = -11 mV), and both maximum loading capacity (LC ∼ 17%) and entrapment efficiency (EE ∼ 100%). Kinetic release profiles show a slower release of Sor from nanoassemblies with respect to the free drug. SC6OH/Sor nanoassemblies have very low hemolytic activity and high efficiency in vitro in decreasing cell growth and viability of HCC cell lines, such as HepG2, Hep3B, and PLC/PRF/5, opening promising chances to their in vivo applications.
authors.affiliation: CNR-ISMN Istituto per lo Studio dei Materiali Nanostrutturati - U.O.S. di Palermo, Via Ugo La Malfa 153, 90146 Palermo, Italy.
authors.forename: Maria Luisa
authors.initials: ML
authors.lastname: Bondì
authors.affiliation: Dipartimento di Scienze Chimiche, Biologiche, Farmaceutiche ed Ambientali, Università di Messina , V.le F. Stagno D'Alcontres 31, 98166 Messina, Italy.
authors.forename: Angela
authors.initials: A
authors.lastname: Scala
authors.affiliation: CNR-ISMN Istituto per lo Studio dei Materiali Nanostrutturati c/o Dipartimento di Scienze Chimiche, Biologiche, Farmaceutiche ed Ambientali dell'Universitá di Messina, V.le F.Stagno D'Alcontres 31, 98166 Messina, Italy.
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Sortino
authors.affiliation: Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche (STEBICEF), Università degli Studi di Palermo , Via Archirafi 32, 90123 Palermo, Italy.
authors.forename: Erika
authors.initials: E
authors.lastname: Amore
authors.affiliation: Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche (STEBICEF), Università degli Studi di Palermo , Via Archirafi 32, 90123 Palermo, Italy.
authors.forename: Chiara
authors.initials: C
authors.lastname: Botto
authors.affiliation: Istituto di Biomedicina e Immunologia Molecolare "A. Monroy" - Consiglio Nazionale delle Ricerche, Via Ugo La Malfa 153, 90146 Palermo, Italy.
authors.forename: Antonina
authors.initials: A
authors.lastname: Azzolina
authors.affiliation: Istituto di Biomedicina e Immunologia Molecolare "A. Monroy" - Consiglio Nazionale delle Ricerche, Via Ugo La Malfa 153, 90146 Palermo, Italy.
authors.forename: Daniele
authors.initials: D
authors.lastname: Balasus
authors.affiliation: Istituto di Biomedicina e Immunologia Molecolare "A. Monroy" - Consiglio Nazionale delle Ricerche, Via Ugo La Malfa 153, 90146 Palermo, Italy.
authors.forename: Melchiorre
authors.initials: M
authors.lastname: Cervello
authors.affiliation: CNR-ISMN Istituto per lo Studio dei Materiali Nanostrutturati c/o Dipartimento di Scienze Chimiche, Biologiche, Farmaceutiche ed Ambientali dell'Universitá di Messina, V.le F.Stagno D'Alcontres 31, 98166 Messina, Italy.
authors.forename: Antonino
authors.initials: A
authors.lastname: Mazzaglia
mesh_terms: D000218:Adamantane / Q000737:chemistry; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D001667:Binding, Competitive; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003505:Cyclodextrins / Q000737:chemistry*; D003692:Delayed-Action Preparations / Q000737:chemistry / Q000494:pharmacology*; D004339:Drug Compounding; D065546:Drug Liberation; D004912:Erythrocytes / Q000166:cytology / Q000187:drug effects; D006461:Hemolysis / Q000187:drug effects; D022781:Hepatocytes / Q000187:drug effects / Q000473:pathology; D006801:Humans; D007700:Kinetics; D049329:Nanostructures / Q000737:chemistry* / Q000648:ultrastructure; D009536:Niacinamide / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D010671:Phenylurea Compounds / Q000737:chemistry / Q000494:pharmacology*; D000077157:Sorafenib; D013501:Surface-Active Agents / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D003505:Cyclodextrins; D003692:Delayed-Action Preparations; D010671:Phenylurea Compounds; D013501:Surface-Active Agents; D009536:Niacinamide; D000077157:Sorafenib; D000218:Adamantane