Document Detail


Synthesis and DNA transfection properties of new head group modified malonic acid diamides.
MedLine Citation:
PMID:  21354464     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
Malonic acid diamides with two long hydrophobic alkyl chains and a basic polar head group as a new class of non-viral gene transferring compounds have shown high transfection efficiency and moderate toxicity. Based on the results obtained with saturated and unsaturated alkyl residues new derivatives with a more complex head group structure have been synthesized. For this purpose, cationic respectively basic groups were introduced by one or two lysine residues bound via tris(aminoethyl)amine spacer to the malonic acid diamide backbone. By studying in vitro gene delivery an increase of transfection efficacy was observed when using lipids with at least one unsaturated alkyl chain. This leads to cationic lipids exhibiting comparable or even higher transfection efficacies compared to the commercially available transfection agents LipofectAmine™ and SuperFect™. Phase transitions and phase structures of selected compounds have been analyzed and discussed in terms of transfection abilities. Particle size and zeta potential of liposomes and lipoplexes were also determined.
Authors:
Christian Wölk; Martin Heinze; Patrick Kreideweiß; Matthias Dittrich; Gerald Brezesinski; Andreas Langner; Bodo Dobner
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-2-24
Journal Detail:
Title:  International journal of pharmaceutics     Volume:  -     ISSN:  1873-3476     ISO Abbreviation:  -     Publication Date:  2011 Feb 
Date Detail:
Created Date:  2011-2-28     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7804127     Medline TA:  Int J Pharm     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2011. Published by Elsevier B.V.
Affiliation:
Institute of Pharmacy, Department of Biochemical Pharmacy, Martin-Luther-University, Wolfgang-Langenbeck-Strasse 4, 06120 Halle (Saale), Germany.
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