Affinity Induced Surface Functionalization of Liposomes Using Cu-Free Click Chemistry

Martin Bak, Rasmus Irming Jølck, Rasmus Eliasen, Thomas Lars Andresen

Research output: Contribution to journalJournal articleResearchpeer-review

637 Downloads (Pure)


Functionalization of nanoparticles is a key element for improving specificity of drug delivery systems toward diseased tissue or cells. In the current study we report a highly efficient and chemoselective method for post-functionalization of liposomes with biomacromolecules, which equally well can be used for functionalization of other nanoparticles or solid surfaces. The method exploits a synergistic effect of having both affinity and covalent anchoring tags on the surface of the liposome. This was achieved by synthesizing a peptide linker system that uses Cu-free strain-promoted click chemistry in combination with histidine affinity tags. The investigation of post-functionalization of PEGylated liposomes was performed with a cyclic RGDfE peptide. By exploring both affinity and covalent tags a 98 ± 2.0% coupling efficiency was achieved, even a diluted system showed a coupling efficiency of 87 ± 0.2%. The reaction kinetics and overall yield were quantified by HPLC. The results presented here open new possibilities for constructing complex nanostructures and functionalized surfaces.
Original languageEnglish
JournalBioconjugate Chemistry
Issue number7
Pages (from-to)1673-80
Publication statusPublished - 2016


Dive into the research topics of 'Affinity Induced Surface Functionalization of Liposomes Using Cu-Free Click Chemistry'. Together they form a unique fingerprint.

Cite this