Preparation and characterisation of a new lipospermine for gene delivery into various cell-lines

A novel cationic amphiphile consisting of a hydrophobic 1,3 dioleoylglycerol moiety and a positively charged spermine head group, 1,3-dioleoyloxy-2-(N-5-carbamoyl-spermine)-propane (DOCSPER), has been prepared. Based on naturally occurring materials, DOCSPER is susceptible to metabolic degradation and a promising agent for delivery of therapeutical genes in vivo. In aqueous solutions this lipospermine spontaneously forms liposomes with a size of about 20-100 nm. Liposomes composed of DOCSPER and the helper lipid dioleoylphosphatidylethanolamine (DOPE) were several hundred nm in size. DOCSPER liposomes were tested for their ability to transfect the rat glioblastoma cell-line F98, the rat colon carcinoma cell-line CC531, the T-cell line Jurkat and the human mamma tumour cell-lines MCF-7 and MaTu. Transfectability and toxicity of liposomes prepared with DOCSPER were compared with the Lipofectin reagent. Toxicity was significantly lower and transfection efficiencies were similar compared to Lipofectin. Lipid/DNA complex formation was controlled by turbidity measurements allowing easy determination of optimal lipid/DNA ratio for transfection. (C) 1998 Elsevier Science B.V. All rights reserved.