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Core-crosslinked polymeric micelles with controlled release of covalently entrapped doxorubicin
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SYSNO ASEP 0346588 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název Core-crosslinked polymeric micelles with controlled release of covalently entrapped doxorubicin Tvůrce(i) Talelli, M. (NL)
Iman, M. (NL)
Varkouhi, A. K. (NL)
Rijcken, C. J. F. (NL)
Schiffelers, R. M. (NL)
Etrych, Tomáš (UMCH-V) RID, ORCID
Ulbrich, Karel (UMCH-V) RID
van Nostrum, C. F. (NL)
Lammers, T. (DE)
Storm, G. (NL)
Hennink, W. E. (NL)Zdroj.dok. Biomaterials. - : Elsevier - ISSN 0142-9612
Roč. 31, č. 30 (2010), s. 7797-7804Poč.str. 8 s. Jazyk dok. eng - angličtina Země vyd. GB - Velká Británie Klíč. slova doxorubicin ; cancer therapy ; polymeric micelle Vědní obor RIV CD - Makromolekulární chemie CEP KAN200200651 GA AV ČR - Akademie věd IAA400500806 GA AV ČR - Akademie věd CEZ AV0Z40500505 - UMCH-V (2005-2011) UT WOS 000281498600021 DOI 10.1016/j.biomaterials.2010.07.005 Anotace A physically entrapped anticancer drug (paclitaxel) was previously shown to be rapidly eliminated from the circulation, likely because the drug was insufficiently retained in the micelles. To fully exploit the EPR effect for drug targeting, a DOX methacrylamide derivative (DOX-MA) was covalently incorporated into the micellar core by free radical polymerization. The structure of the doxorubicin derivative is susceptible to pH-sensitive hydrolysis, enabling controlled release of the drug in acidic conditions (in either the intratumoral environment and/or the endosomal vesicles). The entire drug payload was released within 24 h incubation at pH 5 and 37 °C, whereas only around 5% release was observed at pH 7.4. DOX micelles showed higher cytotoxicity in B16F10 and OVCAR-3 cells compared to DOX-MA, likely due to cellular uptake of the micelles via endocytosis and intracellular drug release in the acidic organelles. Pracoviště Ústav makromolekulární chemie Kontakt Eva Čechová, cechova@imc.cas.cz ; Tel.: 296 809 358 Rok sběru 2011
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