Multivalent Calixarene-Based Liposomes as Platforms for Gene and Drug Delivery
José Antonio Lebrón,
Manuel López-López,
Clara B. García-Calderón,
Ivan V. Rosado,
Fernando R. Balestra,
Pablo Huertas,
Roman V. Rodik,
Vitaly I. Kalchenko,
Eva Bernal,
María Luisa Moyá,
Pilar López-Cornejo,
Francisco J. Ostos
Affiliations
José Antonio Lebrón
Department of Physical Chemistry, Faculty of Chemistry, University of Seville, C/Profesor García González 1, 41012 Seville, Spain
Manuel López-López
Department of Chemical Engineering, Physical Chemistry and Materials Science, Faculty of Experimental Sciences, University of Huelva, Campus de El Carmen, Avda. de las Fuerzas Armadas s/n, 21071 Huelva, Spain
Clara B. García-Calderón
Institute of Biomedicine of Seville (IBiS), University Hospital Virgen del Rocío/CSIC/University of Seville, Avda. Manuel Siurot s/n, 41013 Seville, Spain
Ivan V. Rosado
Institute of Biomedicine of Seville (IBiS), University Hospital Virgen del Rocío/CSIC/University of Seville, Avda. Manuel Siurot s/n, 41013 Seville, Spain
Fernando R. Balestra
Department of Genetics, Faculty of Biology, University of Seville, C/Profesor García González 1, 41012 Seville, Spain
Pablo Huertas
Department of Genetics, Faculty of Biology, University of Seville, C/Profesor García González 1, 41012 Seville, Spain
Roman V. Rodik
Institute of Organic Chemistry, National Academy of Science of Ukraine, Murmanska Str. 5, 02660 Kiev, Ukraine
Vitaly I. Kalchenko
Institute of Organic Chemistry, National Academy of Science of Ukraine, Murmanska Str. 5, 02660 Kiev, Ukraine
Eva Bernal
Department of Physical Chemistry, Faculty of Chemistry, University of Seville, C/Profesor García González 1, 41012 Seville, Spain
María Luisa Moyá
Department of Physical Chemistry, Faculty of Chemistry, University of Seville, C/Profesor García González 1, 41012 Seville, Spain
Pilar López-Cornejo
Department of Physical Chemistry, Faculty of Chemistry, University of Seville, C/Profesor García González 1, 41012 Seville, Spain
Francisco J. Ostos
Department of Physical Chemistry, Faculty of Chemistry, University of Seville, C/Profesor García González 1, 41012 Seville, Spain
The formation of calixarene-based liposomes was investigated, and the characterization of these nanostructures was carried out using several techniques. Four amphiphilic calixarenes were used. The length of the hydrophobic chains attached to the lower rim as well as the nature of the polar group present in the upper rim of the calixarenes were varied. The lipid bilayer was formed with one calixarene and with the phospholipid 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine, DOPE. The cytotoxicity of the liposomes for various cell lines was also studied. From the results obtained, the liposomes formed with the least cytotoxic calixarene, (TEAC12)4, were used as nanocarriers of both nucleic acids and the antineoplastic drug doxorubicin, DOX. Results showed that (TEAC12)4/DOPE/p-EGFP-C1 lipoplexes, of a given composition, can transfect the genetic material, although the transfection efficiency substantially increases in the presence of an additional amount of DOPE as coadjuvant. On the other hand, the (TEAC12)4/DOPE liposomes present a high doxorubicin encapsulation efficiency, and a slow controlled release, which could diminish the side effects of the drug.
