HPMA-based polymer conjugates for repurposed drug mebendazole and other imidazole-based therapeutics
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61389013%3A_____%2F21%3A00545100" target="_blank" >RIV/61389013:_____/21:00545100 - isvavai.cz</a>
Result on the web
<a href="https://www.mdpi.com/2073-4360/13/15/2530" target="_blank" >https://www.mdpi.com/2073-4360/13/15/2530</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.3390/polym13152530" target="_blank" >10.3390/polym13152530</a>
Alternative languages
Result language
angličtina
Original language name
HPMA-based polymer conjugates for repurposed drug mebendazole and other imidazole-based therapeutics
Original language description
Recently, the antitumor potential of benzimidazole anthelmintics, such as mebendazole and its analogues, have been reported to have minimal side effects, in addition to their well-known anti-parasitic abilities. However, their administration is strongly limited owing to their extremely poor solubility, which highly depletes their overall bioavailability. This study describes the design, synthesis, and physico-chemical properties of polymer-mebendazole nanomedicines for drug repurposing in cancer therapy. The conjugation of mebendazole to water-soluble and biocompatible polymer carrier was carried out via biodegradable bond, relying on the hydrolytic action of lysosomal hydrolases for mebendazole release inside the tumor cells. Five low-molecular-weight mebendazole derivatives, differing in their inner structure, and two polymer conjugates differing in their linker structure, were synthesized. The overall synthetic strategy was designed to enable the modification and polymer conjugation of most benzimidazole-based anthelmintics, such as albendazole, fenbendazole or albendazole, besides the mebendazole. Furthermore, the described methodology may be suitable for conjugation of other biologically active compounds with a heterocyclic N-H group in their molecules.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10404 - Polymer science
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
2021
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Polymers
ISSN
2073-4360
e-ISSN
2073-4360
Volume of the periodical
13
Issue of the periodical within the volume
15
Country of publishing house
CH - SWITZERLAND
Number of pages
14
Pages from-to
2530
UT code for WoS article
000682200100001
EID of the result in the Scopus database
2-s2.0-85111635782