Tag Archives: complexation

Characterization of Inclusion Complexes between Miconazole and Different Cyclodextrin Derivatives

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.

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New Perspectives: Quinolones as Complexation Agents

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.

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