Abstract: Cationic liposomes are broadly used as non-viral vectors to deliver genetic materials that can be used to treat various diseases including cancer. To circumvent problems associated with cationic liposome-mediated delivery systems such as low transfection efficiency and serum-induced inhibition, cholesterol-based cationic lipids have been synthesized that resist the effects of serum. The introduction of an ether-type linkage and extension of the aminopropyl head group on the cholesterol backbone increased the transfection efficiency and DNA binding affinity compared to a carbamoyl-type linkage and a mono aminopropyl head group, respectively. Under optimal conditions, each liposome formulation showed higher transfection efficiency in AGS and Huh-7 cells than commercially available cationic liposomes, particularly in the presence of serum. The following molecular structures were found to have a positive effect on transfection properties: (i) extended aminopropyl head groups for a strong binding affinity to plasmid DNA; (ii) an ether linkage that favors electrostatic binding to plasmid DNA; and (iii) a cholesterol backbone for serum resistance.
Keywords: cholesterol; cationic lipids; cyanoethylation; transfection; gene delivery; macropinocytosis
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Kim, B.-K.; Seu, Y.-B.; Bae, Y.-U.; Kwak, T.-W.; Kang, H.; Moon, I.-J.; Hwang, G.-B.; Park, S.-Y.; Doh, K.-O. Efficient Delivery of Plasmid DNA Using Cholesterol-Based Cationic Lipids Containing Polyamines and Ether Linkages. Int. J. Mol. Sci. 2014, 15, 7293-7312.
Kim B-K, Seu Y-B, Bae Y-U, Kwak T-W, Kang H, Moon I-J, Hwang G-B, Park S-Y, Doh K-O. Efficient Delivery of Plasmid DNA Using Cholesterol-Based Cationic Lipids Containing Polyamines and Ether Linkages. International Journal of Molecular Sciences. 2014; 15(5):7293-7312.
Kim, Bieong-Kil; Seu, Young-Bae; Bae, Yun-Ui; Kwak, Tae-Won; Kang, Hyungu; Moon, Ik-Jae; Hwang, Guen-Bae; Park, So-Young; Doh, Kyung-Oh. 2014. "Efficient Delivery of Plasmid DNA Using Cholesterol-Based Cationic Lipids Containing Polyamines and Ether Linkages." Int. J. Mol. Sci. 15, no. 5: 7293-7312.