Journal
CHEMISTRY-A EUROPEAN JOURNAL
Volume 22, Issue 33, Pages 11578-11582Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.201602758
Keywords
click chemistry; drug delivery; folic acid; liposomes; polyglycerol
Categories
Funding
- Max Planck Graduate Center Mainz
- DFG research center [SFB1066]
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Synthetic access to multiple surface decorations are a bottleneck in the development of liposomes for receptor mediated targeting. This opens a complex multiparameter space, exploration of which is severely limited in terms of sample numbers and turnaround times. Here, we unlock this technological barrier by a combination of a milligram-scale liposome formulation using dual centrifugation and orthogonal click chemistry on the liposomal surface. Application of these techniques to conceptually new amphiphilic compounds, which feature norbornene and alkyne groups at the apex of sterically stabilizing, hyperbranched polyglycerol moieties, revealed a particular influence of the membrane anchor of functional amphiphiles. Folic acid residues clicked to cholesterol-based amphiphiles were inefficient in folate-mediated cell targeting, while dialkyl-anchored amphiphiles remained stable in the liposomal membrane and imparted efficient targeting properties. These findings are of specific importance considering the popularity of cholesterol as a lipophilic anchor.
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