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Start Over Creator Tomáš Etrych

11. Teprve kombinace metod a vzájemná diskuse umožní... uvidět celého slona

Creator:
Miroslav Raab and Tomáš Etrych
Format:
print, bez média, and svazek
Type:
article, články, model:article, and TEXT
Subject:
Věda. Všeobecnosti. Základy vědy a kultury. Vědecká práce, Ústav makromolekulární chemie (Akademie věd ČR), výzkum a vývoj, makromolekulární chemie, intelektuální spolupráce, research and development, macromolecular chemistry, intellectual cooperation, 12, and 00
Language:
Czech
Description:
Miroslav Raab, Tomáš Etrych.
Rights:
http://creativecommons.org/publicdomain/mark/1.0/ and policy:public

12. The pH-dependent and enzymatic release of cytarabine from hydrophilic polymer conjugates

Creator:
Pola, R., Olga Janoušková, and Tomáš Etrych
Format:
print, bez média, and svazek
Type:
article, články, model:article, and TEXT
Subject:
Fyziologie člověka a srovnávací fyziologie, fyziologie, physiology, HPMA copolymers, drug delivery system, nucleoside analogues, cytarabine, 14, and 612
Language:
English
Description:
Cytarabine is one of the most efficient drugs in the treatment of hematological malignancies. In this work, we describe the synthesis and characterization of two different polymer conjugates of cytarabine that were designed for the controlled release of cytarabine within the leukemia cells. Reactive copolymers of N-(2-hydroxypropyl)methacrylamide (HPMA) and 3-(3-methacrylamidopropanoyl)thiazolidine-2-thione) or 3-(Nmethacryloylglycyl- phenylalanylleucylglycyl)thiazolidine-2-thione were used in the study as reactive polymer precursors for reaction with cytarabine. The enzymatic release of cytarabine from the conjugate containing a GFLG spacer utilizing cathepsin B was verified. In addition to enzymolysis, the pH-dependent hydrolysis of cytarabine from both copolymers was also confirmed. Approximately 40 % and 20 % of the drug was released by spontaneous hydrolysis at pH 7.4 within 72 h from the polymer conjugates with the GFLG and β-Ala spacers, respectively. At pH 6.0, the spontaneous hydrolysis slowed down, and less than 10 % of the drug was liberated within 72 h. The results of the cytotoxicity evaluation of the polymer conjugates in vitro against various cell lines showed that the cytotoxicity of the polymer conjugates is approximately three times lower in comparison to free cytarabine., R. Pola, O. Janoušková, T. Etrych., and Obsahuje bibliografii
Rights:
http://creativecommons.org/publicdomain/mark/1.0/ and policy:public