Mixed Cationic Liposomes Based on L-Amino Acids As Efficient Delivery Systems of Therapeutic Molecules into Cells

• Published in: Biochemistry (Moscow). Supplement series A, Membrane and cell biology Vol. 17; no. 2; pp. 136 - 147
• Main Authors: Denieva, Z. G., Koloskova, O. O., Gileva, A. M., Budanova, U. A., Sebyakin, Yu. L.
• Format: Journal Article
• Language: English
• Published: Moscow Pleiades Publishing 01.06.2023; Springer Nature B.V
• Subjects: Alanine; Amino acids; Antineoplastic drugs; Antitumor agents; Biological activity; Biomedical and Life Sciences; Cations; Cell Biology; Cell lines; Drug delivery; Drugs; Endoplasmic reticulum; L-Alanine; L-Serine; Lecithin; Life Sciences; Lipids; Liposomes; Nucleic acids; Ornithine; Phosphatidylcholine; Phospholipids; Transfection; Zeta potential; cerasome-forming lipids; targeted delivery; cationic amphiphiles; amino acid derivatives; anticancer agents
• ISSN: 1990-7478; 1990-7494
• DOI: 10.1134/S1990747823030054

This work aimed to produce mixed liposomes based on natural amino acids as vehicles for delivery of anticancer drugs and nucleic acids. Liposomes were formed from cationic lipids based on L -alanine and L -serine, a cerasome-forming lipid based on L -ornithine, and phospholipids phosphatidylcholine (PC) or 1,2-dioleoyl- sn -glycero-3-phosphoethanolamine (DOPE). For the developed agents, particle size, zeta potential, and stability were determined, and the biological activity was studied on the MCF-7 and HEK 293 cell lines. Liposomes based on L -serine demonstrated the ability to accumulate in the endoplasmic reticulum of cells within 1 h, and their transfection activity significantly exceeded that of the commercial drug Lipofectamine-2000. At the same time, the proposed system had a slight toxic effect (IC 50 , 0.475 mg/mL and the safe working concentration, 0.24 mg/mL). Thus, the results suggest that mixed liposomes based on L -serine can serve as an efficient delivery system of drugs into cells.