Tag Archives: complexation

Characterization of Inclusion Complexes between Miconazole and Different Cyclodextrin Derivatives

Hajnal Kelemen1, Gabriel Hancu1, Serban Andrei Gâz-Florea2, Eniko Nemes-Nagy3, Lajos Attila Papp1, Eleonora Mircia4

1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Medicine and Pharmacy, Tîrgu Mureş, Romania
2. Department of Organic Chemistry, Faculty of Pharmacy, University of Medicine and Pharmacy, Tîrgu Mureş, Romania
3. Department of Biochemistry, Faculty of Pharmacy, University of Medicine and Pharmacy, Tîrgu Mureş, Romania
4. Department of Pharmaceutical Industry, Faculty of Pharmacy, University of Medicine and Pharmacy, Tîrgu Mureş, Romania

DOI: 10.2478/amma-2018-0012

Objective: Miconazole, an imidazole antifungal derivative, is a very hydrophobic compound, a major drawback in obtaining topical pharmaceutical formulations with optimal bioavailability. Cyclodextrins (CDs) may increase local drug delivery by enhancing the drug release and/or permeation. The aim of the study is the characterization of inclusion complexes between miconazole and different CD derivatives.
Methods: Several CD derivatives were tested in the experiments. The binary systems between miconazole and different CDs were prepared in 1:1 molar ratios by physical-mixture and kneading methods. Differential scanning calorimetry (DSC) and Fourier transformed-infrared spectroscopy (FT-IR) methods were used to characterize solid state interactions between miconazole and CDs in their binary systems.
Results: The FT-IR analysis suggests the formation of a new solid phase, indicating a molecular interaction between the components. The DSC analysis sustains the hypothesis of formation of partial inclusion complexes between miconazole nitrate and CD. Conclusion: The thermic behaviour of the complexes depends both on the preparation method and the composition of the products.

Keywords: , , , ,
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New Perspectives: Quinolones as Complexation Agents

Rusu Aura, Gyéresi Á., Hancu G.

University of Medicine and Pharmacy Târgu Mureş, Faculty of Pharmacy, Department of Pharmaceutical Chemistry

Background: Quinolones are synthetic antibacterial agents, with a 4-oxo-1,4-dihydroquinolinic structure, which is based on the nalidixic acid model. The 4-oxo and 3-carboxyl groups confer quinolones excellent chelatation properties with metallic ions.
Aim: To highlight a few theories regarding the complexation phenomenon of quinolones.
Methods: Complexes with metallic ions have been characterized (stoichiometry, in vitro physical-chemicals properties, stability studies, and behavioral studies in different biological mediums).
Results: New availabilities have been identified: bioavailability of the complexed quinolones and formulation of new pharmaceutical products with a superior bioavailability and therapeutic effect; the antimicrobial activity of quinolone complexes; quinolone complexes as antitumor drugs with the aim of obtaining less toxic compounds; understanding the mechanism of action of quinolones, which is a challenge especially regarding their selectivity at the bacterial DNA level; development of new determination methods, based on the complexation of quinolones with metallic ions.
Conclusions: The 21st century may provide new useful therapeutic aspects on the basis of complexation between quinolones and metals.

Keywords: , , ,
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