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Adjusting the Structure of β-Cyclodextrin to Improve Complexation of Anthraquinone-Derived Drugs

Authors :
Piotr Garbacz
Paulina Gwardys
Olga Swiech
Renata Bilewicz
Maciej Majdecki
Agata Krzak
Source :
Molecules, Vol 26, Iss 7205, p 7205 (2021), Molecules, Molecules; Volume 26; Issue 23; Pages: 7205
Publication Year :
2021
Publisher :
MDPI AG, 2021.

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.

Details

Language :
English
ISSN :
14203049
Volume :
26
Issue :
7205
Database :
OpenAIRE
Journal :
Molecules
Accession number :
edsair.doi.dedup.....cf0135a044715131e01456cfaca79a8c