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    Wyświetlanie 1-2 z 2
    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
    Tytuł:
    Chemiczne aspekty celowanej terapii przeciwnowotworowej I. Kowalencyjne połączenia ligand-nośnik
    Chemical as pects of targeted anticancer therapy I. Covalent bond of ligand to carier
    Autorzy:
    Werengowska, K. M.
    Wiśniewski, M.
    Terzyk, A.P.
    Gurtowska, N.
    Drewa, T. A.
    Powiązania:
    https://bibliotekanauki.pl/articles/171972.pdf
    Data publikacji:
    2011
    Wydawca:
    Polskie Towarzystwo Chemiczne
    Tematy:
    nanonośniki leków
    terapia celowana
    ligandy
    wiązania kowalencyjne
    system dostarczania leków przeciwnowotworowych
    nanocarriers of drugs
    targeted therapy
    ligands
    covalent bond
    anticancer drug delivery system
    Opis:
    In this study we describe the most popular biomedical engineering nanoparticles including carbon nanotubes [17-20], liposomes [4-7], polymeric micells [11-13], quantum dots [3, 21-23], hydrogels [24-27], dendrimers [14-16] which are recently considered as modern drug carriers. These nanomaterials are applied for cancer diagnostic and targeted delivery of active compounds as chemotherapeutics in so called targeted therapy. Thus, we characterized the ideas of targeted therapy for which compositions of carriers with antibody are constructed (Figs. 3, 4). We also compared the traditional and targeted mechanisms [1, 3, 28-29] of drug delivery (Fig. 2). During targeted therapy only the essential dose of drug (less than during conventional chemotherapy) is delivering to the cancer cell. In additional, the application of targeted therapy reduces side effects, being very characteristic for the traditional treatment. The anticancer compound can selectively hits the target only, due to the presence of the ligands attached to the surface of nanocarirer. We characterized ligands which are often use in nanomedicine: antibodies [33-37], folic acid [30-33], peptides [33, 38, 39], aptamers [33, 40, 41] and transferrin [33, 42-44]. The purpose of this study is description of the bioconjugation of ligand-nanocarrier. This step is necessary and very important in synthesis of the novel drug delivery systems in targeted anticancer therapy. We report recent advances in the field showing the formation of amides (Figs. 6-8) [51-57], thioethers (Figs. 9-11) [52, 60-66], disulfides (Fig. 12) [69], and acethyl-hydrazone groups (Fig. 13) [73]. Special attention is paid to the process such as Diels-Alder (Figs. 14, 15) [74, 75] and "click chemistry" through the cycloaddition of Huisgen (Figs. 16, 17) [79-82]. We describe also the reaction of Staudinger [83] and the process of formation Schiff 's base [84]. The processes enable very mild and selective modification of the carriers through formation of amide bound. These methods ware less popular but allow the fictionalization of nanocarriers in biomedical application. Each reaction or process needs special and individual environment and conditions, which are summarized in Table 1.
    Źródło:
    Wiadomości Chemiczne; 2011, 65, 9-10; 887-915
    0043-5104
    2300-0295
    Pojawia się w:
    Wiadomości Chemiczne
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
      Wyświetlanie 1-2 z 2

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