J Control Release 2014 Apr 22;180:42-50. Epub 2014 Feb 22.
Pharmaceutical Biotechnology, Center for NanoScience (CeNS), Ludwig-Maximilians-University (LMU) Munich, Butenandtstrasse 5-13, D-81377 Munich, Germany; Nanosystems Initiative Munich, Schellingstraße 4, D-80799 Munich, Germany. Electronic address:
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J Control Release 2012 Dec 23;164(3):380-6. Epub 2012 Jun 23.
Pharmaceutical Biotechnology, Center for System-Based Drug Research, Ludwig-Maximilians-University Munich, Butenandtstrasse 5-13, D-81377 Munich, Germany.
Cationic oligomers were assembled by solid-phase supported synthesis in few coupling steps based on C-terminal alanine and two lysine branchings, followed by elongation of the four arms with two to five repeats of artificial oligoamino acids containing the 1,2-diaminoethane motif, and ended by N-terminal cysteines or alanines. These sequence-defined oligomers, containing between 28 and 68 protonatable nitrogens, were evaluated for complex formation with plasmid DNA (pDNA) and short interfering RNA (siRNA), followed by reporter gene transfer and gene silencing experiments in Neuro2A cells. By two simple variations, the pDNA gene transfer activity could be thousand-fold improved, exceeding the gold standard linear PEI up to >50-fold. Read More
Bioconjug Chem 2016 Mar 24;27(3):647-59. Epub 2016 Jan 24.
Pharmaceutical Biotechnology, Center for System-based Drug Research and Center for NanoScience (CeNS), Ludwig-Maximilians-University , 81377 Munich, Germany.
Cationic polymers present a versatile platform for the nonviral delivery of therapeutic nucleic acids. In order to achieve effective nucleic acid transfer, polymeric carriers ought to comprise multiple functionalities. Precise chemistries for site-specific placements of the different delivery modules within the carriers present the basis for uncovering structure-activity relationships required for further optimization. Read More
Mol Pharm 2016 07 31;13(7):2332-45. Epub 2016 May 31.
Pharmaceutical Biotechnology, Center for System-Based Drug Research, Ludwig-Maximilians-Universität München , Butenandtstrasse 5-13, 81377 Munich, Germany.
For efficient and receptor-specific siRNA delivery, a new post-PEGylation strategy was established to provide siRNA polyplexes with targeting and shielding agents. For this purpose, core nanoparticles were formed by complexing siRNA with sequence-defined cationic lipo-oligomers. The T-shaped bis-oleoyl-oligoethanamino amides 454 and 595, containing stabilizing tyrosine and cysteine residues, were applied. Read More
Biomaterials 2013 Feb 28;34(5):1624-33. Epub 2012 Nov 28.
Department of Pharmacy, Pharmaceutical Biotechnology, Center for System-based Drug Research and Center for NanoScience-CeNS, Ludwig-Maximilians-University, Butenandtstrasse 5-13, 81377 Munich, Germany.
Nine sequence-defined, polycationic oligomers were synthesized containing motifs of three consecutive tyrosines (Y3) as stabilizing components for pDNA and siRNA polyplex assembly. For pDNA, a combination of terminal oligotyrosines and cysteines was necessary and sufficient for stable polyplex formation. Stable siRNA binding required a combination of terminal cysteines and oligotyrosines, as well as a central hydrophobic modification (oligotyrosines or fatty acids). Read More