In situ targeted activation of an anticancer agent using ultrasound-triggered release of composite droplets. Bezagu, M., Clarhaut, J., Renoux, B., Monti, F., Tanter, M., Tabeling, P., Cossy, J., Couture, O., Papot, S., & Arseniyadis, S. European Journal of Medicinal Chemistry, 142:2–7, December, 2017.
Paper doi abstract bibtex 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 ultrasoundinduced 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.
@article{bezagu_situ_2017,
title = {In situ targeted activation of an anticancer agent using ultrasound-triggered release of composite droplets},
volume = {142},
issn = {02235234},
url = {https://linkinghub.elsevier.com/retrieve/pii/S0223523417302234},
doi = {10.1016/j.ejmech.2017.03.057},
abstract = {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 ultrasoundinduced 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.},
language = {en},
urldate = {2023-04-12},
journal = {European Journal of Medicinal Chemistry},
author = {Bezagu, Marine and Clarhaut, Jonathan and Renoux, Brigitte and Monti, Fabrice and Tanter, Mickael and Tabeling, Patrick and Cossy, Janine and Couture, Olivier and Papot, Sebastien and Arseniyadis, Stellios},
month = dec,
year = {2017},
pages = {2--7},
}
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