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Volume 13
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Article

Multivalent Calixarene-Based Liposomes as Platforms for Gene and Drug Delivery

by
José Antonio Lebrón
1,
Manuel López-López
2,
Clara B. García-Calderón
3,
Ivan V. Rosado
3,
Fernando R. Balestra
4,5,
Pablo Huertas
4,5,
Roman V. Rodik
6,
Vitaly I. Kalchenko
6,
Eva Bernal
1,
María Luisa Moyá
1,*,
Pilar López-Cornejo
1,* and
Francisco J. Ostos
1,*
1
Department of Physical Chemistry, Faculty of Chemistry, University of Seville, C/Profesor García González 1, 41012 Seville, Spain
2
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
3
Institute of Biomedicine of Seville (IBiS), University Hospital Virgen del Rocío/CSIC/University of Seville, Avda. Manuel Siurot s/n, 41013 Seville, Spain
4
Department of Genetics, Faculty of Biology, University of Seville, C/Profesor García González 1, 41012 Seville, Spain
5
Andalusian Center of Molecular Biology and Regenerative Medicine (CABIMER), University of Seville-CSIC-University Pablo de Olavide, Avda. Américo Vespucio 24, 41092 Seville, Spain
6
Institute of Organic Chemistry, National Academy of Science of Ukraine, Murmanska Str. 5, 02660 Kiev, Ukraine
*
Authors to whom correspondence should be addressed.
Pharmaceutics 2021, 13(8), 1250; https://doi.org/10.3390/pharmaceutics13081250
Submission received: 20 July 2021 / Revised: 6 August 2021 / Accepted: 8 August 2021 / Published: 12 August 2021
(This article belongs to the Special Issue Supramolecular Systems for Gene and Drug Delivery)
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Abstract

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.
Keywords: cationic calix[4]arenes; liposomes; nucleic acids; transfection efficiency; doxorubicin; encapsulation cationic calix[4]arenes; liposomes; nucleic acids; transfection efficiency; doxorubicin; encapsulation
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MDPI and ACS Style

Lebrón, J.A.; López-López, M.; García-Calderón, C.B.; V. Rosado, I.; Balestra, F.R.; Huertas, P.; Rodik, R.V.; Kalchenko, V.I.; Bernal, E.; Moyá, M.L.; et al. Multivalent Calixarene-Based Liposomes as Platforms for Gene and Drug Delivery. Pharmaceutics 2021, 13, 1250. https://doi.org/10.3390/pharmaceutics13081250

AMA Style

Lebrón JA, López-López M, García-Calderón CB, V. Rosado I, Balestra FR, Huertas P, Rodik RV, Kalchenko VI, Bernal E, Moyá ML, et al. Multivalent Calixarene-Based Liposomes as Platforms for Gene and Drug Delivery. Pharmaceutics. 2021; 13(8):1250. https://doi.org/10.3390/pharmaceutics13081250

Chicago/Turabian Style

Lebrón, José Antonio, 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, and et al. 2021. "Multivalent Calixarene-Based Liposomes as Platforms for Gene and Drug Delivery" Pharmaceutics 13, no. 8: 1250. https://doi.org/10.3390/pharmaceutics13081250

APA Style

Lebrón, J. A., López-López, M., García-Calderón, C. B., V. Rosado, I., Balestra, F. R., Huertas, P., Rodik, R. V., Kalchenko, V. I., Bernal, E., Moyá, M. L., López-Cornejo, P., & Ostos, F. J. (2021). Multivalent Calixarene-Based Liposomes as Platforms for Gene and Drug Delivery. Pharmaceutics, 13(8), 1250. https://doi.org/10.3390/pharmaceutics13081250

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