<abstract xmlns="http://www.w3.org/1999/xhtml"><bold>Objective</bold>: 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.<bold>Methods</bold>: 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.<bold>Results</bold>: 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.<bold>Conclusion</bold>: The thermic behaviour of the complexes depends both on the preparation method and the composition of the products.</abstract>

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.

Characterization of Inclusion Complexes between Miconazole and Different Cyclodextrin Derivatives

Department of Pharmaceutical Chemistry, Faculty of Pharmacy

Department of Organic Chemistry, Faculty of Pharmacy

Department of Biochemistry, Faculty of Pharmacy

Department of Pharmaceutical Industry, Faculty of Pharmacy

Acta Marisiensis - Seria Medica

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Objective: Miconazole, an imidazole antifungal derivative, is a very hydrophobic compound, a major drawback in obtaining topical pharmaceutical formulations...

Characterization of Inclusion Complexes between Miconazole and Different Cyclodextrin Derivatives

Publié en ligne: 07 juil. 2018

Pages: 70 - 76

Reçu: 17 mai 2018

Accepté: 17 juin 2018

DOI: https://doi.org/10.2478/amma-2018-0012

Mots clés
miconazole, cyclodextrins, complexation, differential scanning calorimetry, Fourier transform-infrared spectroscopy

© 2018 Hajnal Kelemen et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Characterization of Inclusion Complexes between Miconazole and Different Cyclodextrin Derivatives

Publié en ligne: 07 juil. 2018

Pages: 70 - 76

Reçu: 17 mai 2018

Accepté: 17 juin 2018

DOI: https://doi.org/10.2478/amma-2018-0012

Mots clésmiconazole, cyclodextrins, complexation, differential scanning calorimetry, Fourier transform-infrared spectroscopy

© 2018 Hajnal Kelemen et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Mots clés
miconazole, cyclodextrins, complexation, differential scanning calorimetry, Fourier transform-infrared spectroscopy