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Fine tuning of the pH-dependent drug release rate from polyHPMA-ellipticinium conjugates
- 1.0394937 - ÚMCH 2014 RIV GB eng J - Journal Article
Sedláček, Ondřej - Studenovský, Martin - Větvička, D. - Ulbrich, Karel - Hrubý, Martin
Fine tuning of the pH-dependent drug release rate from polyHPMA-ellipticinium conjugates.
Bioorganic & Medicinal Chemistry. Roč. 21, č. 18 (2013), s. 5669-5672. ISSN 0968-0896. E-ISSN 1464-3391
R&D Projects: GA ČR GAP304/12/0950; GA MPO FR-TI4/625
Grant - others:AV ČR(CZ) M200501201
Program: M
Institutional support: RVO:61389013
Keywords : ellipticine * controlled release * hydrazone
Subject RIV: FD - Oncology ; Hematology
Impact factor: 2.951, year: 2013
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.
Permanent Link: http://hdl.handle.net/11104/0224113
Number of the records: 1