Kim, TW Chung, H Kwon, IC Sung, HC Jeong, SY 2024-01-21T13:03:30Z 2024-01-21T13:03:30Z 2021-09-05 2001-01 0724-8741 https://pubs.kist.re.kr/handle/201004/140810 Purpose. To enhance in vitro and in vivo transfection activity by optimizing lipid composition of cationic lipid emulsions. Methods. Various emulsion formulations having different cationic lipids as emulsifiers, and additional helper lipids as co-emulsifiers, were prepared. The stability of the emulsion and its complex with DNA was investigated by measuring the particle size change in phosphate buffer saline (PBS) over a period of 20 days. The activity of the emulsions in transfecting pCMV-beta into COS-1 cells in the presence or absence of 80% serum was evaluated. We also evaluated in vivo transfection activity using intravenously administered pCMV-Luc(+) as a reporter gene. Results. Among the cationic emulsifiers, 1,2-dioleoyl-sn-glycero-3-trimethylammonium-propane (DOTAP) formed the most stable and efficient emulsion gene carrier. Addition of 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE) increased in vitro transfection activity, but slightly compromised the stability of the emulsion. The loss was compensated for by including small amounts of Tween 80 in the emulsion. The in vitro and in vivo transfection activities were also increased by adding Tween 80. Even though in vitro transfection activity of liposomes was high in the absence of serum, the transfection activity of emulsions was far greater than that of liposomes in the presence of serum and for in vivo applications. Conclusions. By including DOPE as an endosomolytic agent and Tween 80 as a stabilization agent, the cationic emulsion becomes a more potent gene carrier for in vitro and in vivo applications, especially in the presence of serum. English KLUWER ACADEMIC/PLENUM PUBL GENE DELIVERY NONIONIC SURFACTANTS IN-VIVO COMPLEXES MECHANISM CELLS Optimization of lipid composition in cationic emulsion as in vitro and in vivo transfection agents Article 10.1023/A:1011074610100 1 PHARMACEUTICAL RESEARCH, v.18, no.1, pp.54 - 60 PHARMACEUTICAL RESEARCH 18 1 54 60 scie scopus 000168218800008 2-s2.0-0035048881 Chemistry, Multidisciplinary Pharmacology & Pharmacy Chemistry Pharmacology & Pharmacy Article GENE DELIVERY NONIONIC SURFACTANTS IN-VIVO COMPLEXES MECHANISM CELLS gene transfer DOTAP DOPE nonionic surfactant poly(ethylene glycol)