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Authors: Wagener, Karolin
Bros, Matthias
Krumb, Matthias
Langhanki, Jens
Pektor, Stefanie
Worm, Matthias
Schinnerer, Meike
Montermann, Evelyn
Miederer, Matthias
Frey, Holger
Opatz, Till
Rösch, Frank
Title: Targeting of immune cells with trimannosylated liposomes
Online publication date: 13-Aug-2021
Language: english
Abstract: Dendritic cells (DCs) are a compelling target in cancer immunotherapy as they initialize strong antigen-specific immune responses. Drug delivery systems (DDSs) such as liposomes provide the opportunity to deliver antigens and immunostimulatory molecules to DCs, which in turn initiate an antigen-specific immune response. To address predominantly DCs, DDSs need to be equipped with targeting moieties. This study evaluates liposomes, bearing the oligosaccharide trimannose on their surface, for their ability to address DCs in vitro and in vivo. Trimannose as a saccharidic structure is known to be recognized by receptors on the surface of DCs. To obtain trimannosylated liposomes, azide-bearing trimannose is coupled to alkyne-functionalized hyperbranched polyglycerol (hbPG) with a bis(hexadecyl)glycerol (BisHD) anchor in a Cu(I)-catalyzed alkyne-azide cycloaddition (CuAAC). To enable tracking of the liposomes in vivo, the trimannosylated BisHD-hbPG lipids are radiolabeled with 18F in a CuAAC. Subsequently, liposomes are produced via the thin-film hydration method followed by extrusion. The behavior of the trimannosylated liposomes is evaluated in in vitro cell binding assays and in vivo µPET and ex vivo biodistribution studies in healthy C57BL/6 mice and the results are compared to similar liposomes not bearing trimannose on their surface.
DDC: 540 Chemie
540 Chemistry and allied sciences
570 Biowissenschaften
570 Life sciences
Institution: Johannes Gutenberg-Universität Mainz
Department: FB 09 Chemie, Pharmazie u. Geowissensch.
Place: Mainz
Version: Published version
Publication type: Zeitschriftenaufsatz
License: CC BY-NC-ND
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Journal: Advanced therapeutics
Pages or article number: 1900185
Publisher: Wiley-VCH
Publisher place: Weinheim
Issue date: 2020
ISSN: 2366-3987
Publisher URL:
Publisher DOI: 10.1002/adtp.201900185
Appears in collections:JGU-Publikationen

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