Administration of water soluble drugs encapsulated within the interior of liposomes has been shown to increase drug efficacy and reduce toxic side effects relative to conventional drug administration.  Current FDA approved liposome based drug delivery systems rely on passive leakage which make it difficult to deliver the correct dosage of drug.  To improve delivery efficiency triggered release liposome systems have been developed to deliver contents upon exposure to external stimuli including temperature, pH, light, and ultrasound.  Reported herein is the development of a novel chemically triggered release system.  Triggered release experiments demonstrate rapid leakage of tracer molecules (carboxyfluorescein, glucose) from a liposome system upon treatment with a non-toxic chemical trigger under physiologically relevant conditions.  The chemical trigger is a Zn(II)-dipicolylamine coordination complex and mechanistic studies indicate that leakage is induced by association of the trigger with a phosphatidylserine target molecule that is in the liposome membrane.

Chemically triggered release from liposomes

244th National Meeting (2012)

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