Uncharged Gemini-Amphiphiles as Components of Cationic Liposomes for Delivery of Nucleic Acids

• Published in: Russian journal of bioorganic chemistry Vol. 46; no. 6; pp. 1250 - 1260
• Main Authors: Shmendel, E. V., Bakhareva, S. A., Makarova, D. M., Chernikov, I. V., Morozova, N. G., Chernolovskaya, E. L., Zenkova, M. A., Maslov, M. A.
• Format: Journal Article
• Language: English
• Published: Moscow Pleiades Publishing 01-11-2020
• Subjects: Biochemistry; Biomedical and Life Sciences; Biomedicine; Bioorganic Chemistry; Life Sciences; Organic Chemistry; gene therapy; uncharged gemini-amphiphiles; nucleic acids; cytotoxicity; cationic liposomes; transfection
• ISSN: 1068-1620; 1608-330X
• DOI: 10.1134/S106816202006031X

New uncharged gemini-amphiphiles have been synthesized. A series of cationic liposomes based on the polycationic amphiphile 1,26-bis(cholest-5-en-3β-yloxycarbonylamino)-7,11,16,20-tetraazahexacosan tetrahydrochloride (2X3), 1,2-dioleoyl-
sn
-glycero-3-phosphoethanolamine (DOPE) and uncharged gemini-amphiphiles that contain short hydrophobic and long hydrophilic spacers have been prepared. The physicochemical characteristics, cytotoxicity, and transfection activity of cationic liposomes have been studied. Cationic liposomes that include 10% (mol) of a uncharged gemini-amphiphile with the oligooxymethylene spacer have formed small complexes with plasmid DNA and efficiently delivered it into eukaryotic cells.