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Merck

Shear-stress sensitive lenticular vesicles for targeted drug delivery.

Nature nanotechnology (2012-06-12)
Margaret N Holme, Illya A Fedotenko, Daniel Abegg, Jasmin Althaus, Lucille Babel, France Favarger, Renate Reiter, Radu Tanasescu, Pierre-Léonard Zaffalon, André Ziegler, Bert Müller, Till Saxer, Andreas Zumbuehl
RESUMEN

Atherosclerosis results in the narrowing of arterial blood vessels and this causes significant changes in the endogenous shear stress between healthy and constricted arteries. Nanocontainers that can release drugs locally with such rheological changes can be very useful. Here, we show that vesicles made from an artificial 1,3-diaminophospholipid are stable under static conditions but release their contents at elevated shear stress. These vesicles have a lenticular morphology, which potentially leads to instabilities along their equator. Using a model cardiovascular system based on polymer tubes and an external pump to represent shear stress in healthy and constricted vessels of the heart, we show that drugs preferentially release from the vesicles in constricted vessels that have high shear stress.

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O-Phosphorylethanolamine