High-molecular weight star conjugates containing docetaxel with high anti-tumor activity and low systemic toxicity in vivo
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388971%3A_____%2F15%3A00439488" target="_blank" >RIV/61388971:_____/15:00439488 - isvavai.cz</a>
Alternative codes found
RIV/61389013:_____/15:00439488
Result on the web
<a href="http://dx.doi.org/10.1039/C4PY01120A" target="_blank" >http://dx.doi.org/10.1039/C4PY01120A</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1039/C4PY01120A" target="_blank" >10.1039/C4PY01120A</a>
Alternative languages
Result language
angličtina
Original language name
High-molecular weight star conjugates containing docetaxel with high anti-tumor activity and low systemic toxicity in vivo
Original language 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 wasderivatized 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 andretention (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
Czech name
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Czech description
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Classification
Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
EC - Immunology
OECD FORD branch
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Result continuities
Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2015
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Polymer Chemistry
ISSN
1759-9954
e-ISSN
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Volume of the periodical
6
Issue of the periodical within the volume
1
Country of publishing house
GB - UNITED KINGDOM
Number of pages
11
Pages from-to
160-170
UT code for WoS article
000345898100017
EID of the result in the Scopus database
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