Switchable Lipids: Conformational Change for Fast pH-Triggered Cytoplasmic Delivery.
Angew Chem Int Ed Engl
; 54(43): 12743-7, 2015 Oct 19.
Article
em En
| MEDLINE
| ID: mdl-26189870
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 sulforhodamineâ
B in 15â
min at pHâ
5, and the liposome formulations demonstrated high stability at pHâ
7.4 for several months. By using sulforhodamineâ
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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Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Polietilenoglicóis
/
Rodaminas
/
Preparações de Ação Retardada
/
Corantes Fluorescentes
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Lipídeos
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Lipossomos
Idioma:
En
Ano de publicação:
2015
Tipo de documento:
Article