Switchable Lipids: Conformational Change for Fast pH-Triggered Cytoplasmic Delivery

作者: Warren Viricel , Amira Mbarek , Jeanne Leblond

DOI: 10.1002/ANIE.201504661

关键词:

摘要: We report the use of switchable lipids to improve endosomal escape and cytosolic delivery cell-impermeable compounds. The system is based on a conformational reorganization lipid structure upon acidification, as demonstrated by NMR spectroscopic studies. When incorporated in liposome formulation, triggered bilayer destabilization through fusion even presence poly(ethylene glycol). observed 88 % release sulforhodamine B 15 min at pH 5, formulations high stability pH 7.4 for several months. By using model highly polar drug, we fast mediated HeLa cells, no toxicity.

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