Polymeric anticancer drugs with pH-controlled activation
Language English Country Netherlands Media print
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
15158969
DOI
10.1016/j.ijpharm.2003.02.001
PII: S037851730400136X
Knihovny.cz E-resources
- MeSH
- Doxorubicin administration & dosage analogs & derivatives pharmacokinetics MeSH
- Hydrogen-Ion Concentration MeSH
- Polymethacrylic Acids administration & dosage pharmacokinetics MeSH
- Humans MeSH
- Lymphoma, T-Cell drug therapy metabolism MeSH
- Mice, Inbred BALB C MeSH
- Mice, Inbred C57BL MeSH
- Mice MeSH
- Cell Line, Tumor MeSH
- Neoplasms drug therapy metabolism MeSH
- Polymers administration & dosage pharmacokinetics MeSH
- Antineoplastic Agents administration & dosage pharmacokinetics MeSH
- Xenograft Model Antitumor Assays methods MeSH
- Animals MeSH
- Check Tag
- Humans MeSH
- Mice MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- doxorubicin-N-(2-hydroxypropyl)methacrylamide copolymer conjugate MeSH Browser
- Doxorubicin MeSH
- Polymethacrylic Acids MeSH
- Polymers MeSH
- Antineoplastic Agents MeSH
The paper is dealing with the synthesis and properties of new, nontargeted or antibody-targeted pH-sensitive polymer-doxorubicin (DOX) conjugates designed as anticancer drugs facilitating site-specific therapy. These conjugates are stable and inactive during transport in the body but activate inside target cells as a result of pH changes outside and inside the cells. Cytotoxicity of the conjugates depends on the detailed structure of the polymer and of the spacer between the drug and polymer carrier. In both protective and therapeutic regimes of drug administration, the in vivo antitumor activity of the pH-sensitive conjugates containing DOX was significantly enhanced (T-cell lymphoma EL 4, C57BL/16 mice) in comparison with the free DOX or classic PK1, the PHPMA-DOX conjugate clinically tested at present.
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