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Fine tuning of the pH-dependent drug release rate from polyHPMA-ellipticinium conjugates
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SYSNO ASEP 0394937 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Fine tuning of the pH-dependent drug release rate from polyHPMA-ellipticinium conjugates Author(s) Sedláček, Ondřej (UMCH-V) RID, ORCID
Studenovský, Martin (UMCH-V) RID, ORCID
Větvička, D. (CZ)
Ulbrich, Karel (UMCH-V) RID
Hrubý, Martin (UMCH-V) RID, ORCIDSource Title Bioorganic & Medicinal Chemistry. - : Elsevier - ISSN 0968-0896
Roč. 21, č. 18 (2013), s. 5669-5672Number of pages 4 s. Language eng - English Country GB - United Kingdom Keywords ellipticine ; controlled release ; hydrazone Subject RIV FD - Oncology ; Hematology R&D Projects GAP304/12/0950 GA ČR - Czech Science Foundation (CSF) FR-TI4/625 GA MPO - Ministry of Industry and Trade (MPO) Institutional support UMCH-V - RVO:61389013 UT WOS 000323803900002 DOI 10.1016/j.bmc.2013.07.038 Annotation 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 24 h in a pH 5.0 phosphate saline buffer. The ellipticinium drug retained the antiproliferative activity of the ellipticine. Workplace Institute of Macromolecular Chemistry Contact Eva Čechová, cechova@imc.cas.cz ; Tel.: 296 809 358 Year of Publishing 2014
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