Switchable Lipids: Conformational Change for Fast pH-Triggered Cytoplasmic Delivery†
Warren Viricel
Faculty of Pharmacy, University of Montreal, P.O. Box 6128, Downtown Station, Montreal, Quebec (Canada)
Search for more papers by this authorDr. Amira Mbarek
Faculty of Pharmacy, University of Montreal, P.O. Box 6128, Downtown Station, Montreal, Quebec (Canada)
Search for more papers by this authorCorresponding Author
Prof. Dr. Jeanne Leblond
Faculty of Pharmacy, University of Montreal, P.O. Box 6128, Downtown Station, Montreal, Quebec (Canada)
Faculty of Pharmacy, University of Montreal, P.O. Box 6128, Downtown Station, Montreal, Quebec (Canada)Search for more papers by this authorWarren Viricel
Faculty of Pharmacy, University of Montreal, P.O. Box 6128, Downtown Station, Montreal, Quebec (Canada)
Search for more papers by this authorDr. Amira Mbarek
Faculty of Pharmacy, University of Montreal, P.O. Box 6128, Downtown Station, Montreal, Quebec (Canada)
Search for more papers by this authorCorresponding Author
Prof. Dr. Jeanne Leblond
Faculty of Pharmacy, University of Montreal, P.O. Box 6128, Downtown Station, Montreal, Quebec (Canada)
Faculty of Pharmacy, University of Montreal, P.O. Box 6128, Downtown Station, Montreal, Quebec (Canada)Search for more papers by this authorThe National Sciences and Engineering Research Council of Canada (NSERC) is acknowledged for financial support. We thank Aline Mesnier and Hanaa Taleb for their contribution and Prof. Marc Servant (University of Montreal) for insightful discussions.
Abstract
We report the use of switchable lipids to improve the endosomal escape and cytosolic delivery of cell-impermeable compounds. The system is based on a conformational reorganization of the lipid structure upon acidification, as demonstrated by NMR spectroscopic studies. When incorporated in a liposome formulation, the switchable lipids triggered bilayer destabilization through fusion even in the presence of poly(ethylene glycol). We observed 88 % release of sulforhodamine B in 15 min at pH 5, and the liposome formulations demonstrated high stability at pH 7.4 for several months. By using sulforhodamine B as a model of a highly polar drug, we demonstrated fast cytosolic delivery mediated by endosomal escape in HeLa cells, and no toxicity.
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