Polymer nanomedicines with enzymatically triggered activation: a comparative study of in vitro and in vivo anti-cancer efficacy related to the spacer structure

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61389013%3A_____%2F22%3A00561407" target="_blank" >RIV/61389013:_____/22:00561407 - isvavai.cz</a>
Result on the web
<a href="https://www.sciencedirect.com/science/article/pii/S1549963422000831" target="_blank" >https://www.sciencedirect.com/science/article/pii/S1549963422000831</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.nano.2022.102597" target="_blank" >10.1016/j.nano.2022.102597</a>

Result language
angličtina
Original language name
Polymer nanomedicines with enzymatically triggered activation: a comparative study of in vitro and in vivo anti-cancer efficacy related to the spacer structure
Original language description
Polymer nanomedicines with anti-tumor activity should exhibit sufficient stability during systemic circulation to the target tissue. However, they should release the active drug selectively in the tumor. Thus, choice of a tumor-specific stimuli-sensitive spacer between the drug and the carrier is critical. Here, a series of polymer conjugates of anti-cancer drugs doxorubicin and pirarubicin covalently bound to copolymers based on N-(2-hydroxypropyl)methacrylamide via various enzymatically cleavable oligopeptide spacers were prepared and characterized. The highest rate of the drug release from the polymer carriers in presence of the lysosomal protease cathepsin B was determined for the copolymers with Val-Cit-Aba spacer. Copolymers containing pirarubicin were more cytotoxic and showed higher internalization rate than the corresponding doxorubicin counterparts. The conjugates containing GFLG and Val-Cit-Aba spacers exhibited the highest anti-tumor efficacy in vivo against murine sarcoma S-180, the highest rate of the enzymatically catalyzed drug release, and the highest cytotoxicity in vitro.
Czech name
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Czech description
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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

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

Publication year
2022
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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