Bioorthogonal Drug Release from Nanometric Micelles in Living Cells
Abstract: We explored a bioorthogonal approach to release drugs from stimuli‐responsive micelles inside tumor cells. The concept relies on sydnonimine‐based micelles that undergo quantitative cleavage in presence of cyclooctynes, hence releasing their content within living cells. Four cleavable micelles were developed to allow massive burst release of Entinostat, a potent histone deacetylase inhibitor, following their internalization inside cancer cells. A comparative study on the influence of the bioorthogonal‐mediated versus passive drug release from micelles was carried out. The results indicated that a fast release of the drug triggered a stronger antiproliferative activity on tumor cells compared to the passive diffusion of the drug from the micelles core. These finding may be of great interest for the development of new nanomedicines.
- Location
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Deutsche Nationalbibliothek Frankfurt am Main
- Extent
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Online-Ressource
- Language
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Englisch
- Bibliographic citation
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Bioorthogonal Drug Release from Nanometric Micelles in Living Cells ; day:23 ; month:06 ; year:2023 ; extent:7
Chemistry - a European journal ; (23.06.2023) (gesamt 7)
- Creator
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Madegard, Léa
Girard, Melissa
Yaw, Benjamin Riss
Porte, Karine
Audisio, Davide
Papot, Sébastien
Taran, Frédéric
- DOI
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10.1002/chem.202301359
- URN
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urn:nbn:de:101:1-2023062315405680151372
- Rights
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Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
- Last update
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14.08.2025, 10:49 AM CEST
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Associated
- Madegard, Léa
- Girard, Melissa
- Yaw, Benjamin Riss
- Porte, Karine
- Audisio, Davide
- Papot, Sébastien
- Taran, Frédéric
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