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Polymer nanomedicines with enzymatically triggered activation: A comparative study of in vitro and in vivo anti-cancer efficacy related to the spacer structure
M. Pechar, R. Pola, M. Studenovský, M. Bláhová, E. Grosmanová, A. Dydowiczová, M. Filipová, R. Islam, S. Gao, J. Fang, T. Etrych
Language English Country United States
Document type Journal Article, Research Support, Non-U.S. Gov't
- MeSH
- Doxorubicin pharmacology chemistry MeSH
- Humans MeSH
- Mice MeSH
- Cell Line, Tumor MeSH
- Neoplasms * drug therapy MeSH
- Nanomedicine MeSH
- Drug Carriers chemistry MeSH
- Polymers chemistry MeSH
- Antineoplastic Agents * pharmacology therapeutic use chemistry MeSH
- Animals MeSH
- Check Tag
- Humans MeSH
- Mice MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
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.
Faculty of Pharmaceutical Sciences Sojo University Ikeda 4 22 1 Nishi ku Kumamoto 860 0082 Japan
School of Pharmacy Queen's University Belfast 97 Lisburn Road Belfast BT9 7BL UK
References provided by Crossref.org
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