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Polymer conjugates of the highly potent cytostatic drug 2-pyrrolinodoxorubicin
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SYSNO ASEP 0353988 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název Polymer conjugates of the highly potent cytostatic drug 2-pyrrolinodoxorubicin Tvůrce(i) Studenovský, Martin (UMCH-V) RID, ORCID
Ulbrich, Karel (UMCH-V) RID
Ibrahimová, Markéta (MBU-M)
Říhová, Blanka (MBU-M) RIDZdroj.dok. European Journal of Pharmaceutical Sciences. - : Elsevier - ISSN 0928-0987
Roč. 42, 1-2 (2011), s. 156-163Poč.str. 8 s. Jazyk dok. eng - angličtina Země vyd. NL - Nizozemsko Klíč. slova polymer conjugates ; tumor drug-delivery ; pH-controlled release Vědní obor RIV CD - Makromolekulární chemie CEP IAAX00500803 GA AV ČR - Akademie věd CEZ AV0Z40500505 - UMCH-V (2005-2011) AV0Z50200510 - MBU-M (2005-2011) UT WOS 000286708600019 DOI 10.1016/j.ejps.2010.11.006 Anotace This paper describes the synthesis and biological evaluation of a conjugate of the highly cytotoxic drug 2-pyrrolinodoxorubicin (p-DOX) with an N-(2-hydroxypropyl)methacrylamide copolymer (PHPMA), utilizing the advantageous concept of polymer–drug conjugates. The hydrazone bond between the polymer and drug is susceptible to pH-controlled hydrolysis, enabling prolonged stability in circulation and fast p-DOX release under conditions mimicking the intracellular environment. The in vitro cytostatic activity of free p-DOX was in accordance with literature, whereas its PHPMA conjugate exhibited a 1.3- to 5-fold lower cytotoxicity, depending on the cancer cell line, when compared to the free p-DOX. On mice bearing T-cell EL4 lymphoma, no tumor suppression was observed from the free p-DOX at a subtoxic dose of 0.1 mg/kg, whereas the PHPMA/p-DOX conjugate significantly inhibited the initial tumor growth at approximately equitoxic doses of 0.4 and 0.8 mg p-DOX eq/kg. Pracoviště Ústav makromolekulární chemie Kontakt Eva Čechová, cechova@imc.cas.cz ; Tel.: 296 809 358 Rok sběru 2011
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