title: P-Sulfocalix[6]arene as Nanocarrier for Controlled Delivery of Doxorubicin.
abstract: Given the high toxicity of the anthracycline antibiotic doxorubicin (DOX), it is relevant to search for nanocarriers that decrease the side effects of the drug and are able to transport it towards a therapeutic target Here, the encapsulation of DOX by p-sulfocalix[6]arene (calix) has been studied. The interaction of DOX with the macrocycle, as well as with DNA, has been investigated and the equilibrium constant for each binding process estimated. The results showed that the binding constant of DOX to DNA, KDNA, is three orders of magnitude higher than that to calix, Kcalix. The ability of calixarenes to encapsulate DOX molecules, as well as the capability of the DOX molecules included into the inner cavity of the macrocycle to bind with DNA have been examined. Cytotoxicity measurements were done in different cancer and normal cell lines to probe the decrease in the toxicity of the encapsulated DOX. The low toxicity of calixarenes has also been demonstrated for different cell lines.
authors.affiliation: Departamento de Química Física, Facultad de Química, Universidad de Sevilla, c/ Prof. García González n° 1, Seville, 41012, Spain.
authors.forename: Francisco J
authors.identifier: http://orcid.org/0000-0001-6583-6974
authors.initials: FJ
authors.lastname: Ostos
authors.affiliation: Departamento de Química Física, Facultad de Química, Universidad de Sevilla, c/ Prof. García González n° 1, Seville, 41012, Spain.
authors.forename: José A
authors.identifier: http://orcid.org/0000-0002-6938-3690
authors.initials: JA
authors.lastname: Lebrón
authors.affiliation: Departamento de Química Física, Facultad de Química, Universidad de Sevilla, c/ Prof. García González n° 1, Seville, 41012, Spain.
authors.forename: Maria L
authors.identifier: http://orcid.org/0000-0002-2736-9348
authors.initials: ML
authors.lastname: Moyá
authors.affiliation: Departamento de Ingeniería Química, Química FísicayCiencias de los Materiales, Facultad de Ciencias Experimentales, Universidad de Huelva, Campus 'El Carmen", E-21071, Huelva, Spain.
authors.forename: Manuel
authors.identifier: http://orcid.org/0000-0001-9060-9554
authors.initials: M
authors.lastname: López-López
authors.affiliation: Departamento de Química Física, Facultad de Química, Universidad de Sevilla, c/ Prof. García González n° 1, Seville, 41012, Spain.
authors.forename: Antonio
authors.initials: A
authors.lastname: Sánchez
authors.affiliation: Departamento de Química Física, Facultad de Química, Universidad de Sevilla, c/ Prof. García González n° 1, Seville, 41012, Spain.
authors.forename: Amparo
authors.initials: A
authors.lastname: Clavero
authors.affiliation: Instituto de Biomedicina de Sevilla (IBiS), Hospital Universitario Virgen del Rocío/CSIC/Universidad de Sevilla, Av. Manuel Siurot, s/n, 41013, Seville, Spain.
authors.forename: Clara B
authors.initials: CB
authors.lastname: García-Calderón
authors.affiliation: Instituto de Biomedicina de Sevilla (IBiS), Hospital Universitario Virgen del Rocío/CSIC/Universidad de Sevilla, Av. Manuel Siurot, s/n, 41013, Seville, Spain.
authors.forename: Iván V
authors.initials: IV
authors.lastname: Rosado
authors.affiliation: Departamento de Química Física, Facultad de Química, Universidad de Sevilla, c/ Prof. García González n° 1, Seville, 41012, Spain.
authors.forename: Pilar
authors.identifier: http://orcid.org/0000-0002-5825-9483
authors.initials: P
authors.lastname: López-Cornejo
mesh_terms: D000903:Antibiotics, Antineoplastic / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D047250:Calixarenes / Q000737:chemistry*; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004273:DNA, Neoplasm / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004317:Doxorubicin / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D015394:Molecular Structure; D053758:Nanoparticles / Q000737:chemistry*; D010636:Phenols / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D000903:Antibiotics, Antineoplastic; D004273:DNA, Neoplasm; D004337:Drug Carriers; D010636:Phenols; C476540:calix(6)arene; D047250:Calixarenes; D004317:Doxorubicin
keywords: DNA; calixarenes; chemotherapeutics; doxorubicin; drug delivery; nanocarriers