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Wyświetlanie 1-2 z 2
Tytuł:
Low generation polyamidoamine dendrimers (PAMAM) and biotinPAMAM conjugate – the detailed structural studies by 1 H and 13C nuclear magnetic resonance spectroscopy
Autorzy:
Wróbel, Konrad
Wołowiec, Stanisław
Powiązania:
https://bibliotekanauki.pl/articles/2040134.pdf
Data publikacji:
2020-12-30
Wydawca:
Uniwersytet Rzeszowski. Wydawnictwo Uniwersytetu Rzeszowskiego
Tematy:
biotin conjugate
nuclear magnetic resonance polyamidoamine dendrimer
Opis:
Introduction. The concept of targeted drug delivery is nowadays based on nanoparticle transporters. Such drug delivery systems for cancer cells should follow the requirements like: efficient drug release, selective binding and internalization to cancer cells. The anticancer drug selectivity can be achieved by attachment of cancer cell-recognizing molecules, like biotin. Among nanosized carriers the PAMAM dendrimers are tested intensely, especially they can be modified by covalent attachment of prodrug molecules and biotin as targeting molecule. Aim. We aimed at construction and characterization of a conjugate formed between PAMAM and biotin (Biot). The nuclear magnetic resonances is powerful tool to determine both the structure and stoichiometry of the conjugate. Material and methods. PAMAM G0 has been synthesized and functionalized with biotin by reaction with N-hydroxysuccinimide ester of biotin to obtain G0 double-substituted with biotin. All the compound were thoroughly characterized by the NMR spectroscopy. Results. The conjugate of PAMAM G0 dendrimer with two amide-bonded biotin molecules was obtained and fully characterized by NMR spectroscopy. Conclusion. N-hydroxysuccinimide ester of biotin spontaneously reacts with PAMAM G0 to obtain the conjugate of 2:1 biotin:G0 stoichiometry. The latter was designed as a targeting molecule in formation of megameric multidrug delivery system.
Źródło:
European Journal of Clinical and Experimental Medicine; 2020, 4; 281-285
2544-2406
2544-1361
Pojawia się w:
European Journal of Clinical and Experimental Medicine
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Synthesis and characterization of Fulvestrant and Paclitaxel conjugates with polyamidoamine dendrimer fourth generation
Autorzy:
Wróbel, Konrad
Wołowiec, Stanisław
Powiązania:
https://bibliotekanauki.pl/articles/29519437.pdf
Data publikacji:
2023-09-30
Wydawca:
Uniwersytet Rzeszowski. Wydawnictwo Uniwersytetu Rzeszowskiego
Tematy:
PAMAM dendrimer
double-conjugation
Fulvestrant
Paclitaxel
anticancer drug delivery system
Opis:
Introduction and aim. Poorly soluble anticancer drugs can be attached covalently into biologically inert macromolecule in order to administrate a drug as water soluble form. It was proven that covalent linkers, for instance amide or carbamate bonds are susceptible to hydrolysis. Thus the attached drug can be released from the conjugates in tissue, specifically within the targeted cell. We aimed at construction of water soluble conjugates of Fulvestrant and Paclitaxel with PAMAM G4 dendrimer. In order to obtain water soluble conjugates the amine groups were substituted with R-glycidol. Material and methods. Polyamidoamine dendrimer of fourth generation was synthesized and examined by detailed NMR analysis in water and in DMSO. The conjugates were covalently linked to amine groups of PAMAM after activation of Fulvestrant 17-OH group with 4-nitrophenylchloroformate and activation of end-carboxyl group of Paclitaxel succinate. Results. The method of binary conjugate PAMAMG4-Fulvestrant-Paclitaxel synthesis was elaborated and the product was characterized by physicochemical methods. Conclusion. The glycidylated PAMAMG4-Fulvestrant-Paclitaxel conjugate is better soluble in water than unconverted drugs.
Źródło:
European Journal of Clinical and Experimental Medicine; 2023, 3; 442-449
2544-2406
2544-1361
Pojawia się w:
European Journal of Clinical and Experimental Medicine
Dostawca treści:
Biblioteka Nauki
Artykuł
    Wyświetlanie 1-2 z 2

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