TY  - JOUR
AU  - Miletić, Tijana
AU  - Kyriakos, Kachrimanis
AU  - Graovac, Adrijana
AU  - Ibrić, Svetlana
PY  - 2013
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/1841
AB  - The present work investigates the effect of complexation with hydroxypropyl-beta-cyclodextrin (HPBCD) and 2-O-methyl-beta-cyclodextrin (2-O-MBCD), on voriconazole solubility, dissolution rate and chemical stability. Drug-cyclodextrin complexes were prepared as aqueous solutions, which were spray-dried, and their properties were compared to wet ground samples and physical mixtures. DSC analysis revealed absence of crystalline voriconazole from spray-dried complexes. FTIR spectroscopy indicated changes in the H-bonding network of the hydroxyl groups of cyclodextrin following drug inclusion. Dissolution rate of voriconazole was significantly higher from spray-dried complexes with either cyclodextrin in comparison with free drug, physical mixtures, or wet ground mixtures. However, two degradation impurities were found in aged samples, with slightly higher impurity level with HPBCD. Performed solubility studies suggested that 2-O-MBCD is more efficient solubilizer. Molecular docking simulations showed a difference in the 1:1 binding affinities and sites, with HPBCD surprisingly forming complexes of much lower energy, thus suggesting a multiple rather than a 1:1 complexation.
PB  - Elsevier Sci Ltd, Oxford
T2  - Carbohydrate Polymers
T1  - Spray-dried voriconazole-cyclodextrin complexes: Solubility, dissolution rate and chemical stability
VL  - 98
IS  - 1
SP  - 122
EP  - 131
DO  - 10.1016/j.carbpol.2013.05.084
ER  - 

@article{
author = "Miletić, Tijana and Kyriakos, Kachrimanis and Graovac, Adrijana and Ibrić, Svetlana",
year = "2013",
abstract = "The present work investigates the effect of complexation with hydroxypropyl-beta-cyclodextrin (HPBCD) and 2-O-methyl-beta-cyclodextrin (2-O-MBCD), on voriconazole solubility, dissolution rate and chemical stability. Drug-cyclodextrin complexes were prepared as aqueous solutions, which were spray-dried, and their properties were compared to wet ground samples and physical mixtures. DSC analysis revealed absence of crystalline voriconazole from spray-dried complexes. FTIR spectroscopy indicated changes in the H-bonding network of the hydroxyl groups of cyclodextrin following drug inclusion. Dissolution rate of voriconazole was significantly higher from spray-dried complexes with either cyclodextrin in comparison with free drug, physical mixtures, or wet ground mixtures. However, two degradation impurities were found in aged samples, with slightly higher impurity level with HPBCD. Performed solubility studies suggested that 2-O-MBCD is more efficient solubilizer. Molecular docking simulations showed a difference in the 1:1 binding affinities and sites, with HPBCD surprisingly forming complexes of much lower energy, thus suggesting a multiple rather than a 1:1 complexation.",
publisher = "Elsevier Sci Ltd, Oxford",
journal = "Carbohydrate Polymers",
title = "Spray-dried voriconazole-cyclodextrin complexes: Solubility, dissolution rate and chemical stability",
volume = "98",
number = "1",
pages = "122-131",
doi = "10.1016/j.carbpol.2013.05.084"
}

Miletić, T., Kyriakos, K., Graovac, A.,& Ibrić, S.. (2013). Spray-dried voriconazole-cyclodextrin complexes: Solubility, dissolution rate and chemical stability. in Carbohydrate Polymers
Elsevier Sci Ltd, Oxford., 98(1), 122-131.
https://doi.org/10.1016/j.carbpol.2013.05.084

Miletić T, Kyriakos K, Graovac A, Ibrić S. Spray-dried voriconazole-cyclodextrin complexes: Solubility, dissolution rate and chemical stability. in Carbohydrate Polymers. 2013;98(1):122-131.
doi:10.1016/j.carbpol.2013.05.084 .

Miletić, Tijana, Kyriakos, Kachrimanis, Graovac, Adrijana, Ibrić, Svetlana, "Spray-dried voriconazole-cyclodextrin complexes: Solubility, dissolution rate and chemical stability" in Carbohydrate Polymers, 98, no. 1 (2013):122-131,
https://doi.org/10.1016/j.carbpol.2013.05.084 . .