Preparation of a DNA Complex with Lipoglutamide Having Tetraethylene Glycol Tails, and Its Application to DNA Delivery into Tumor Cells1

Article abstract of DOI:10.1246/bcsj.69.2335

We newly prepared a polyion complex of DNA with lipoglutamide, N,N′-bis(18-hydroxy-7,10,13,16-tetraoxaoctadecyl)-L-glutamide hydrochloride (abbreviated to 2EO₄C₆N⁺). Formation and characterization of the DNA/2EO₄C₆N⁺ complex were investigated by elemental analysis, melting temperature, and light-scattering measurements. Compaction of DNA by binding with the cationic 2EO₄C₆N⁺ was seen by multi-angle light scattering. Aggregation of the DNA/2EO₄C₆N⁺ complex was significantly depressed compared with the DNA complex without tetraethylene glycol. The DNA/2EO₄C₆N⁺ complex had low cytotoxicity and efficient internalization into tumor cells compared with native DNA.