期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 26, 期 16, 页码 4025-4029出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.06.085
关键词
Cationic liposome; Folic acid; Folate receptor; Gene delivery; Transfection efficiency
资金
- National High Technology Research and Development Program (863 Program) of China [2014AA020707]
- National Natural Science Foundation of China [21176046, 21503035]
- Fundamental Research Funds for the Central Universities [DC201502020205]
In our previous Letter, we have carried out the synthesis of a novel DDCTMA cationic lipid which was formulated with DOPE for gene delivery. Herein, we used folic acid (FA) as targeting ligand and cholesterol (Chol) as helper lipid instead of DOPE for enhancing the stability of the liposomes. These liposomes were characterized by dynamic laser scattering (DLS), transmission electron microscopy (TEM) and agarose gel electrophoresis assays of pDNA binding affinity. The lipoplexes were prepared by using different weight ratios of DDCTMA/Chol (1:1, 2:1, 3:1, 4:1) liposomes and different concentrations of FA (50-200 mu g/mL) combining with pDNA. The transfection efficiencies of the lipoplexes were evaluated using pGFP-N2 and pGL3 plasmid DNA against NCI-H460 cells in vitro. Among them, the optimum gene transfection efficiency with DDCTMA/Chol (3:1)/FA (100 mu g/mL) was obtained. The results showed that FA could improve the gene transfection efficiencies of DDCTMA/Chol cationic liposome. Our results also convincingly demonstrated FA (100 mu g/mL)-coated DDCTMA/Chol (3:1) cationic liposome could serve as a promising candidate for the gene delivery. (C) 2016 Elsevier Ltd. All rights reserved.
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