Počet záznamů: 1
Enhanced Topical and Transdermal Delivery of Antineoplastic and Antiviral Acyclic Nucleoside Phosphonate cPr-PMEDAP
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SYSNO ASEP 0370825 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název Enhanced Topical and Transdermal Delivery of Antineoplastic and Antiviral Acyclic Nucleoside Phosphonate cPr-PMEDAP Tvůrce(i) Vávrová, K. (CZ)
Kovaříková, P. (CZ)
Školová, B. (CZ)
Líbalová, M. (CZ)
Roh, J. (CZ)
Čáp, R. (CZ)
Holý, Antonín (UOCHB-X)
Hrabálek, A. (CZ)Celkový počet autorů 8 Zdroj.dok. Pharmaceutical Research. - : Springer - ISSN 0724-8741
Roč. 28, č. 12 (2011), s. 3105-3115Poč.str. 11 s. Jazyk dok. eng - angličtina Země vyd. US - Spojené státy americké Klíč. slova acyclic nucleoside phosphonates ; antivirals ; antineoplastics ; permeation enhancer ; topical skin application ; transdermal delivery Vědní obor RIV CC - Organická chemie CEP 1M0508 GA MŠMT - Ministerstvo školství, mládeže a tělovýchovy CEZ AV0Z40550506 - UOCHB-X (2005-2011) UT WOS 000297710200014 DOI 10.1007/s11095-011-0508-4 Anotace Acyclic nucleoside phosphonates possess unique antiviral and antineoplastic activities; however, their polar phosphonate moiety is associated with low ability to cross biological membranes. We explored the potential of transdermal and topical delivery of 2,6-diaminopurine derivative cPr-PMEDAP. In vitro diffusion of cPr-PMEDAP was investigated using formulations at different pH and concentration and with permeation enhancer through porcine and human skin. Ability of 0.1-5% cPr-PMEDAP to cross human skin barrier was very low with flux values similar to 40 ng/cm(2)/h, the majority of compound found in the stratum corneum. The highest permeation rates were found at pH 6; increased donor concentration had no influence. The permeation enhancer dodecyl 6-dimethylaminohexanoate (DDAK, 1%) increased flux of cPr-PMEDAP (up to 61 times) and its concentration in nucleated epidermis (up to similar to 0.5 mg of cPr-PMEDAP/g of the tissue). No deamination of cPr-PMEDAP into PMEG occurred during permeation studies, but N-dealkylation into PMEDAP mediated by skin microflora was observed. Transdermal or topical application of cPr-PMEDAP enabled by the permeation enhancer DDAK may provide an attractive alternative route of administration of this potent antitumor and antiviral compound. Pracoviště Ústav organické chemie a biochemie Kontakt asep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Viktorie Chládková, Tel.: 232 002 434 Rok sběru 2012
Počet záznamů: 1