Fine tuning of the pH-dependent drug release rate from polyHPMA-ellipticinium conjugates

0394937 - ÚMCH 2014 RIV GB eng J - Článek v odborném periodiku
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
Grant CEP: GA ČR GAP304/12/0950; GA MPO FR-TI4/625
Grant ostatní: AV ČR(CZ) M200501201
Program: M
Institucionální podpora: RVO:61389013
Klíčová slova: ellipticine * controlled release * hydrazone
Kód oboru RIV: FD - Onkologie a hematologie
Impakt faktor: 2.951, rok: 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.
Trvalý link: http://hdl.handle.net/11104/0224113