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The comparison of in vivo properties of water-soluble HPMA-based polymer conjugates with doxorubicin prepared by controlled RAFT or free radical polymerization

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    0448548 - ÚMCH 2016 RIV CZ eng J - Článek v odborném periodiku
    Chytil, Petr - Šírová, Milada - Koziolová, Eva - Ulbrich, Karel - Říhová, Blanka - Etrych, Tomáš
    The comparison of in vivo properties of water-soluble HPMA-based polymer conjugates with doxorubicin prepared by controlled RAFT or free radical polymerization.
    Physiological Research. Roč. 64, Suppl. 1 (2015), S41-S49. ISSN 0862-8408. E-ISSN 1802-9973
    Grant CEP: GA MŠk(CZ) EE2.3.30.0029; GA MŠk(CZ) ED1.1.00/02.0109
    Institucionální podpora: RVO:61389013 ; RVO:61388971
    Klíčová slova: HPMA copolymers * RAFT polymerization * drug delivery system
    Kód oboru RIV: EB - Genetika a molekulární biologie; CE - Biochemie (MBU-M)
    Impakt faktor: 1.643, rok: 2015
    http://www.biomed.cas.cz/physiolres/pdf/64%20Suppl%201/64_S41.pdf

    Two conjugates of anticancer drug doxorubicin (Dox) covalently bound by the hydrolytically degradable hydrazone bond to the polymer carrier based on water-soluble N-(2-hydroxypropyl) methacrylamide (HPMA) copolymers were synthesized and their properties were compared, namely their behavior in vivo. The polymer carriers differed in dispersity due to different methods of synthesis; the carrier with relatively high dispersity (HD) was prepared by free radical polymerization (Mw = 29 900 g/mol, Ð = 1.75) and the carrier with low dispersity (LD) by controlled radical polymerization (Mw = 30 000 g/mol, Ð = 1.13). Both polymer-Dox conjugates showed prolonged blood circulation and tumor accumulation of the drug in comparison with the free drug; e.g. the tumor-to-blood ratio for the polymer-bound Dox was 3-5 times higher. The LD polymer-Dox conjugate exhibited moderately higher tumor accumulation than the HD one at a dose of 1 x 15 mg Dox (eq.)/kg. Also, their anti-tumor activity did not differ when injected at this dose. However, the increase of the dose to 1 x 25 mg Dox (eq.)/kg resulted in the enhanced therapeutic activity of the conjugates, especially of the LD one with 100 % of long-term survivals. The dispersity of polymer drug carriers influenced the tumor accumulation rate, which affected the overall anti-cancer activity of polymer-drug conjugates.
    Trvalý link: http://hdl.handle.net/11104/0252997

     
     
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