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Statements

Subject Item
n2:RIV%2F61388971%3A_____%2F15%3A00439488%21RIV15-GA0-61388971
rdf:type
skos:Concept n12:Vysledek
dcterms:description
Here we present the polymer conjugates where the core formed by poly(amido amine) dendrimers was grafted with semitelechelic N-(2-hydroxypropyl)methacrylamide (HPMA) copolymers containing docetaxel (DTX) attached by a pH-sensitive hydrazone bond. DTX was derivatized with three different keto acids prior to attachment to the polymer carrier to introduce reactive keto groups into the drug. The therapeutic efficacy of such high-molecular-weight star conjugates is based on: (a) the enhanced permeability and retention (EPR) effect facilitating selective accumulation within solid tumors; (b) pH-controlled release of the drug, thus ensuring faster DTX release in the mildly acidic tumor microenvironment. The star DTX conjugate had a remarkably higher maximum tolerated dose in comparison with free DTX when administered as a single i.v. injection ([similar]160 mg kg1vs. 40 mg kg1 of DTX) in C57BL/6 mice. The star DTX conjugate showed significantly higher antitumor activity than free drug in the EL4 T cell lymphoma growing in syngeneic C57BL/6 mice even when given at the same dose (20 mg kg1 of DTX eq.). Thus, the star DTX conjugates exert a much higher therapeutic activity and yet a lower systemic toxicity than free DTX. Here we present the polymer conjugates where the core formed by poly(amido amine) dendrimers was grafted with semitelechelic N-(2-hydroxypropyl)methacrylamide (HPMA) copolymers containing docetaxel (DTX) attached by a pH-sensitive hydrazone bond. DTX was derivatized with three different keto acids prior to attachment to the polymer carrier to introduce reactive keto groups into the drug. The therapeutic efficacy of such high-molecular-weight star conjugates is based on: (a) the enhanced permeability and retention (EPR) effect facilitating selective accumulation within solid tumors; (b) pH-controlled release of the drug, thus ensuring faster DTX release in the mildly acidic tumor microenvironment. The star DTX conjugate had a remarkably higher maximum tolerated dose in comparison with free DTX when administered as a single i.v. injection ([similar]160 mg kg1vs. 40 mg kg1 of DTX) in C57BL/6 mice. The star DTX conjugate showed significantly higher antitumor activity than free drug in the EL4 T cell lymphoma growing in syngeneic C57BL/6 mice even when given at the same dose (20 mg kg1 of DTX eq.). Thus, the star DTX conjugates exert a much higher therapeutic activity and yet a lower systemic toxicity than free DTX.
dcterms:title
High-molecular weight star conjugates containing docetaxel with high anti-tumor activity and low systemic toxicity in vivo High-molecular weight star conjugates containing docetaxel with high anti-tumor activity and low systemic toxicity in vivo
skos:prefLabel
High-molecular weight star conjugates containing docetaxel with high anti-tumor activity and low systemic toxicity in vivo High-molecular weight star conjugates containing docetaxel with high anti-tumor activity and low systemic toxicity in vivo
skos:notation
RIV/61388971:_____/15:00439488!RIV15-GA0-61388971
n3:aktivita
n5:P n5:I
n3:aktivity
I, P(EE2.3.20.0055), P(GAP301/11/0325), P(GCP207/12/J030)
n3:cisloPeriodika
1
n3:dodaniDat
n16:2015
n3:domaciTvurceVysledku
n10:8721386 n10:3814556 n10:1208241 n10:9165614 n10:1130706
n3:druhVysledku
n7:J
n3:duvernostUdaju
n17:S
n3:entitaPredkladatele
n18:predkladatel
n3:idSjednocenehoVysledku
182
n3:idVysledku
RIV/61388971:_____/15:00439488
n3:jazykVysledku
n11:eng
n3:klicovaSlova
star polymer; HPMA copolymers; docetaxel
n3:klicoveSlovo
n13:docetaxel n13:HPMA%20copolymers n13:star%20polymer
n3:kodStatuVydavatele
GB - Spojené království Velké Británie a Severního Irska
n3:kontrolniKodProRIV
[CEF17062E347]
n3:nazevZdroje
Polymer Chemistry
n3:obor
n14:EC
n3:pocetDomacichTvurcuVysledku
5
n3:pocetTvurcuVysledku
8
n3:projekt
n4:EE2.3.20.0055 n4:GCP207%2F12%2FJ030 n4:GAP301%2F11%2F0325
n3:rokUplatneniVysledku
n16:2015
n3:svazekPeriodika
6
n3:tvurceVysledku
Říhová, Blanka Šírová, Milada Rossmann, Pavel Tomalová, Barbora Etrych, Tomáš Kovář, Marek Ulbrich, Karel Strohalm, Jiří
n3:wos
000345898100017
s:issn
1759-9954
s:numberOfPages
11
n8:doi
10.1039/C4PY01120A