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Adjusting the Structure of β-Cyclodextrin to Improve Complexation of Anthraquinone-Derived Drugs
Authors:Agata Krzak  Olga Swiech  Maciej Majdecki  Piotr Garbacz  Paulina Gwardys  Renata Bilewicz
Institution:1.Faculty of Chemistry, University of Warsaw, Pasteura 1, 02093 Warsaw, Poland; (A.K.); (P.G.); (P.G.);2.Faculty of Chemistry, Biological and Chemical Research Centre, University of Warsaw, Żwirki i Wigury 101, 02089 Warsaw, Poland;3.Institute of Organic Chemistry, Polish Academy of Sciences, Kasprzaka 44/52, 01224 Warsaw, Poland;
Abstract:β-Cyclodextrin (CD) derivatives containing an aromatic triazole ring were studied as potential carriers of the following drugs containing an anthraquinone moiety: anthraquinone-2-sulfonic acid (AQ2S); anthraquinone-2-carboxylic acid (AQ2CA); and a common anthracycline, daunorubicin (DNR). UV-Vis and voltammetry measurements were carried out to determine the solubilities and association constants of the complexes formed, and the results revealed the unique properties of the chosen CDs as effective pH-dependent drug complexing agents. The association constants of the drug complexes with the CDs containing a triazole and lipoic acid (βCDLip) or galactosamine (βCDGAL), were significantly larger than that of the native βCD. The AQ2CA and AQ2S drugs were poorly soluble, and their solubilities increased as a result of complex formation with βCDLip and βCDGAL ligands. AQ2CA and AQ2S are negatively charged at pH 7.4. Therefore, they were less prone to form an inclusion complex with the hydrophobic CD cavity than at pH 3 (characteristic of gastric juices) when protonated. The βCDTriazole and βCDGAL ligands were found to form weaker inclusion complexes with the positively charged drug DNR at an acidic pH (pH 5.5) than in a neutral medium (pH 7.4) in which the drug dissociates to its neutral, uncharged form. This pH dependence is favorable for antitumor applications.
Keywords:cyclodextrins  anthraquinone-2-sulfonic acid  anthraquinone-2-carboxylic acid  daunorubicin  association constant  solubility  inclusion complex
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