In situ targeted activation of an anticancer agent using ultrasound-triggered release of composite droplets
European Journal of Medicinal Chemistry
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The efficiency of a drug is usually highly dependent on the way it is administered or delivered. As such, targeted-therapy, which requires conceiving drug-delivery vehicles that will change their state from a relatively stable structure with a very slow leak-rate to an unstable structure with a fast release, clearly improves the pharmacokinetics, the absorption, the distribution, the metabolism and the therapeutic index of a given drug. In this context, we have developed a particularly effective double stimuli-responsive drug-delivery method allowing an ultrasound-induced release of a monomethylauristatin E-glucuronide prodrug and its subsequent activation by a β-glucuronidase. This led to an increase of cytotoxicity of about 80% on cancer cells.
AuthorsBezagu, M; Clarhaut, J; Renoux, B; Monti, F; Tanter, M; Tabeling, P; Cossy, J; Couture, O; Papot, S; Arseniyadis, S
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