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Efficient delivery of plasmid DNA using cholesterol-based cationic lipids containing polyamines and ether linkages.


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.

SUBMITTER: Kim BK 

PROVIDER: S-EPMC4057673 | biostudies-literature | 2014 Apr

REPOSITORIES: biostudies-literature

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Efficient delivery of plasmid DNA using cholesterol-based cationic lipids containing polyamines and ether linkages.

Kim Bieong-Kil BK   Seu Young-Bae YB   Bae Yun-Ui YU   Kwak Tae-Won TW   Kang Hyungu H   Moon Ik-Jae IJ   Hwang Guen-Bae GB   Park So-Young SY   Doh Kyung-Oh KO  

International journal of molecular sciences 20140428 5


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  ...[more]

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