| Novel cholesterol spermine conjugates provide efficient cellular delivery of plasmid DNA and small interfering RNA. | |
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MedLine Citation:
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PMID: 22138073 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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New polycationic lipids corresponding to the two different classes of amphiphiles ("head-tail" and "gemini") were designed and used as components of non-viral gene delivery systems. The hydrophobic domain of lipids is based on the cholesterol residue and the hydrophilic one - on the naturally occurring polyamine - spermine. Ester and carbamate linker groups as well as oligomethylene spacers of various lengths were used to connect cholesterol and spermine motifs in order to estimate the structure-activity relationships of novel polycationic lipids and to determine an effective and safe transfectant suitable for the delivery of different nucleic acids. The cationic liposomes composed of the synthesized polycationic lipids and DOPE provided delivery of FITC-labeled oligonucleotide, plasmid DNA and siRNA into HEK293 cells with an efficiency significantly higher than that of Lipofectamine 2000. We found that the transfection activity of polycationic lipids is influenced by a linker type, a spacer length and the amount of cholesterol residues. The lipid containing two cholesterol units, carbamate linker and spacer of six methylene groups demonstrated the best in vitro transfection results among other analogues tested and was defined as a promising candidate for further transfection studies to be hold in vivo. |
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Authors:
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Mikhail A Maslov; Tatyana O Kabilova; Ivan A Petukhov; Nina G Morozova; Galina A Serebrennikova; Valentine V Vlassov; Marina A Zenkova |
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Publication Detail:
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Type: JOURNAL ARTICLE Date: 2011-11-25 |
Journal Detail:
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Title: Journal of controlled release : official journal of the Controlled Release Society Volume: - ISSN: 1873-4995 ISO Abbreviation: - Publication Date: 2011 Nov |
Date Detail:
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Created Date: 2011-12-5 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 8607908 Medline TA: J Control Release Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Copyright Information:
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Copyright © 2011. Published by Elsevier B.V. |
Affiliation:
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Moscow State University of Fine Chemical Technologies, 86, Vernadskiy ave., Moscow, Russia. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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