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

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Date

2021-08-12

Authors

Lebrón, José Antonio
López-López, Manuel
García-Calderón, Clara B.
V. Rosado, Ivan
Balestra, Fernando R.
Huertas, Pablo
Rodik, Roman V.
Kalchenko, Vitaly I.
Bernal, Eva
Moyá, María Luisa

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MDPI
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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.

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Medical Subject Headings::Chemicals and Drugs::Biomedical and Dental Materials::Membranes, Artificial::Liposomes
Medical Subject Headings::Chemicals and Drugs::Polycyclic Compounds::Macrocyclic Compounds::Calixarenes
Medical Subject Headings::Chemicals and Drugs::Pharmaceutical Preparations::Dosage Forms::Delayed-Action Preparations
Medical Subject Headings::Analytical, Diagnostic and Therapeutic Techniques and Equipment::Investigative Techniques::Genetic Techniques::Gene Transfer Techniques::Transfection
Medical Subject Headings::Anatomy::Cells::Cells, Cultured::Cell Line
Medical Subject Headings::Chemicals and Drugs::Organic Chemicals::Hydrocarbons::Hydrocarbons, Cyclic::Hydrocarbons, Aromatic::Polycyclic Hydrocarbons, Aromatic::Naphthacenes::Anthracyclines::Daunorubicin::Doxorubicin
Medical Subject Headings::Technology and Food and Beverages::Technology, Industry, and Agriculture::Manufactured Materials::Nanostructures
Medical Subject Headings::Chemicals and Drugs::Chemical Actions and Uses::Pharmacologic Actions::Therapeutic Uses::Antineoplastic Agents
Medical Subject Headings::Chemicals and Drugs::Nucleic Acids, Nucleotides, and Nucleosides::Nucleic Acids

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Keywords

Cationic calix[4]arenes, Liposomes, Nucleic acids, Transfection efficiency, Doxorubicin, Encapsulation, Liposomas, Ácidos nucleicos, Doxorrubicina, Encapsulación celular

Citation

Lebrón JA, López-López M, García-Calderón CB, V Rosado I, Balestra FR, Huertas P, et al. Multivalent Calixarene-Based Liposomes as Platforms for Gene and Drug Delivery. Pharmaceutics. 2021 Aug 12;13(8):1250