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Core-crosslinked polymeric micelles with controlled release of covalently entrapped doxorubicin

SYSNO ASEP	0346588
Document Type	J - Journal Article
R&D Document Type	Journal Article
Subsidiary J	Článek ve WOS
Title	Core-crosslinked polymeric micelles with controlled release of covalently entrapped doxorubicin
Author(s)	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)
Source Title	Biomaterials. - : Elsevier - ISSN 0142-9612 Roč. 31, č. 30 (2010), s. 7797-7804
Number of pages	8 s.
Language	eng - English
Country	GB - United Kingdom
Keywords	doxorubicin ; cancer therapy ; polymeric micelle
Subject RIV	CD - Macromolecular Chemistry
R&D Projects	KAN200200651 GA AV ČR - Academy of Sciences of the Czech Republic (AV ČR)
	IAA400500806 GA AV ČR - Academy of Sciences of the Czech Republic (AV ČR)
CEZ	AV0Z40500505 - UMCH-V (2005-2011)
UT WOS	000281498600021
DOI	10.1016/j.biomaterials.2010.07.005
Annotation	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.
Workplace	Institute of Macromolecular Chemistry
Contact	Eva Čechová, cechova@imc.cas.cz ; Tel.: 296 809 358
Year of Publishing	2011

Number of the records: 1