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

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• 作者：Martin Bak ; Rasmus I. Jølck ; Rasmus Eliasen ; Thomas L. Andresen
• 刊名：Bioconjugate Chemistry
• 出版年：2016
• 出版时间：July 20, 2016
• 年：2016
• 卷：27
• 期：7
• 页码：1673-1680
• 全文大小：406K
• 年卷期：0
• ISSN：1520-4812

文摘

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.