Fine tuning of the pH-dependent drug release rate from polyHPMA-ellipticinium conjugates
Language English Country England, Great Britain Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
23941688
DOI
10.1016/j.bmc.2013.07.038
PII: S0968-0896(13)00659-7
Knihovny.cz E-resources
- Keywords
- Controlled release, Drug delivery, Ellipticine, Hydrazone, PolyHPMA,
- MeSH
- Acrylamides chemistry MeSH
- Cell Line MeSH
- DNA chemistry metabolism MeSH
- Ellipticines chemistry MeSH
- Hydrazones chemistry MeSH
- Hydrogen-Ion Concentration MeSH
- Humans MeSH
- Drug Carriers chemical synthesis chemistry MeSH
- Cell Proliferation drug effects MeSH
- Antineoplastic Agents chemistry metabolism toxicity MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Acrylamides MeSH
- DNA MeSH
- Ellipticines MeSH
- Hydrazones MeSH
- N-(2-hydroxypropyl)methacrylamide MeSH Browser
- Drug Carriers MeSH
- Antineoplastic Agents MeSH
Polymer conjugates of anticancer drugs have shown high potential for assisting in cancer treatments. The pH-labile spacers allow site-specific triggered release of the drugs. We synthesized and characterized model drug conjugates with hydrazide bond-containing poly[N-(2-hydroxypropyl)methacrylamide] differing in the chemical surrounding of the hydrazone bond-containing spacer to find structure-drug release rate relationships. The conjugate selected for further studies shows negligible drug release in a pH 7.4 buffer but released 50% of the ellipticinium drug within 24h in a pH 5.0 phosphate saline buffer. The ellipticinium drug retained the antiproliferative activity of the ellipticine.
References provided by Crossref.org
Formation of DNA adducts by ellipticine and its micellar form in rats - a comparative study
