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

Pharmaceutics

卷:13

Manuel López-López¹  Fernando R. Balestra²  Pablo Huertas²  Pilar López-Cornejo³  José Antonio Lebrón³  María Luisa Moyá³  Francisco J. Ostos³  Eva Bernal³  Clara B. García-Calderón⁴  Ivan V. Rosado⁴  Vitaly I. Kalchenko⁵  Roman V. Rodik⁵ 

[1] 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;

[2] Department of Genetics, Faculty of Biology, University of Seville, C/Profesor García González 1, 41012 Seville, Spain;

[3] Department of Physical Chemistry, Faculty of Chemistry, University of Seville, C/Profesor García González 1, 41012 Seville, Spain;

[4] Institute of Biomedicine of Seville (IBiS), University Hospital Virgen del Rocío/CSIC/University of Seville, Avda. Manuel Siurot s/n, 41013 Seville, Spain;

[5] Institute of Organic Chemistry, National Academy of Science of Ukraine, Murmanska Str. 5, 02660 Kiev, Ukraine;

关键词: cationic calix[4]arenes;    liposomes;    nucleic acids;    transfection efficiency;    doxorubicin;    encapsulation;   

DOI  :  10.3390/pharmaceutics13081250

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown