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

Abstract

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 kerase-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 (IC50, 0.475 mg/mL and the safe working concentration, 0.24 mg/mL).