Journal article
Synthesis and Stability Studies of α,α‐Difluoro Ester Phospholipids
Department of Chemistry, Technical University of Denmark1
Center for Nanomedicine and Theranostics, Centers, Technical University of Denmark2
Department of Micro- and Nanotechnology, Technical University of Denmark3
Colloids and Biological Interfaces, Department of Micro- and Nanotechnology, Technical University of Denmark4
Organic Chemistry, Department of Chemistry, Technical University of Denmark5
The synthesis of two new α,α‐difluoro ester phospholipid conjugates is described and the stability of their liposomal formulations in three different aqueous buffers (pH 4.5, 7.5 and 8.5) has been investigated. The studies confirmed that α,α‐difluoro esters are much more prone to hydrolysis when positioned close to the hydrophilic head group of phospholipids than when the functionality is placed in the lipophilic part of the bilayer in liposomes.
This observation lends further support to the concept of protecting hydrolysable functionalities by formulation as part of the membrane of liposomes.
| Language: | English |
|---|---|
| Publisher: | WILEY‐VCH Verlag |
| Year: | 2012 |
| Pages: | 6656-6661 |
| ISSN: | 1434193x and 10990690 |
| Types: | Journal article |
| DOI: | 10.1002/ejoc.201200565 |
| ORCIDs: | Andresen, Thomas Lars and Clausen, Mads Hartvig |
