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Micelle-forming block copolymers tailored for inhibition of P-gp-mediated multidrug resistance: structure to activity relationship
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SYSNO ASEP 0510951 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název Micelle-forming block copolymers tailored for inhibition of P-gp-mediated multidrug resistance: structure to activity relationship Tvůrce(i) Braunová, Alena (UMCH-V) RID
Kaňa, Martin (MBU-M) ORCID
Kudláčová, Júlia (UMCH-V) RID, ORCID
Kostka, Libor (UMCH-V) RID, ORCID
Bouček, J. (CZ)
Betka, J. (CZ)
Šírová, Milada (MBU-M) RID, ORCID
Etrych, Tomáš (UMCH-V) RID, ORCIDČíslo článku 579 Zdroj.dok. Pharmaceutics. - : MDPI
Roč. 11, č. 11 (2019), s. 1-22Poč.str. 22 s. Jazyk dok. eng - angličtina Země vyd. CH - Švýcarsko Klíč. slova polymer therapeutics ; multidrug resistance ; micelles Vědní obor RIV CD - Makromolekulární chemie Obor OECD Polymer science Vědní obor RIV – spolupráce Mikrobiologický ústav - Mikrobiologie, virologie CEP NV16-28600A GA MZd - Ministerstvo zdravotnictví Způsob publikování Open access Institucionální podpora UMCH-V - RVO:61389013 ; MBU-M - RVO:61388971 UT WOS 000502280100031 EID SCOPUS 85076552758 DOI 10.3390/pharmaceutics11110579 Anotace Multidrug resistance (MDR) is often caused by the overexpression of efflux pumps, such as ABC transporters, in particular, P-glycoprotein (P-gp). Here, we investigate the di- and tri- block amphiphilic polymer systems based on polypropylene glycol (PPO) and copolymers of (N-(2-hydroxypropyl)methacrylamide) (PHPMA) as potential macromolecular inhibitors of P-gp, and concurrently, carriers of drugs, passively targeting solid tumors by the enhanced permeability and retention (EPR) effect. Interestingly, there were significant differences between the effects of di- and tri- block polymer-based micelles, with the former being significantly more thermodynamically stable and showing much higher P-gp inhibition ability. The presence of Boc-protected hydrazide groups or the Boc-deprotection method did not affect the physico-chemical or biological properties of the block copolymers. Moreover, diblock polymer micelles could be loaded with free PPO containing 5–40 wt % of free PPO, which showed increased P-gp inhibition in comparison to the unloaded micelles. Loaded polymer micelles containing more than 20 wt % free PPO showed a significant increase in toxicity. Thus, loaded diblock polymer micelles containing 5–15 wt % free PPO are potential candidates for in vitro and in vivo application as potent MDR inhibitors and drug carriers. Pracoviště Ústav makromolekulární chemie Kontakt Eva Čechová, cechova@imc.cas.cz ; Tel.: 296 809 358 Rok sběru 2020 Elektronická adresa https://www.mdpi.com/1999-4923/11/11/579/pdf
Počet záznamů: 1