Thiol-ene Reaction: An Efficient Tool to Design Lipophilic Polyphosphoesters for Drug Delivery Systems
| Autor: | Vanslambrouck, Stéphanie, Riva, Raphaël, Ucakar, Bernard, Préat, Véronique, Gagliardi, Mick, Molin, Daniel G. M., Lecomte, Philippe, Jérôme, Christine |
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| Přispěvatelé: | Fysiologie, RS: Carim - V03 Regenerative and reconstructive medicine vascular disease |
| Jazyk: | angličtina |
| Rok vydání: | 2021 |
| Předmět: | |
| Zdroj: | Molecules, 26(6):1750. Multidisciplinary Digital Publishing Institute (MDPI) Molecules, Vol 26, Iss 1750, p 1750 (2021) Molecules Volume 26 Issue 6 |
| ISSN: | 1420-3049 |
| Popis: | Poly(ethylene glycol)-b-polyphosphoester (PEG-b-PPE) block copolymer nanoparticles are promising carriers for poorly water soluble drugs. To enhance the drug loading capacity and efficiency of such micelles, a strategy was investigated for increasing the lipophilicity of the PPE block of these PEG-b-PPE amphiphilic copolymers. A PEG-b-PPE copolymer bearing pendant vinyl groups along the PPE block was synthesized and then modified by thiol-ene click reaction with thiols bearing either a long linear alkyl chain (dodecyl) or a tocopherol moiety. Ketoconazole was used as model for hydrophobic drugs. Comparison of the drug loading with PEG-b-PPE bearing shorter pendant groups is reported evidencing the key role of the structure of the pendant group on the PPE backbone. Finally, a first evidence of the biocompatibility of these novel PEG-b-PPE copolymers was achieved by performing cytotoxicity tests. The PEG-b-PPE derived by tocopherol was evidenced as particularly promising as delivery system of poorly water-soluble drugs. |
| Databáze: | OpenAIRE |
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