Formulation and characterization studies of inclusion complexes of voriconazole for possible ocular application

In our study, Voriconazole (VOR) was selected as an active agent to be used for the treatment of ocular fungal infections. To overcome low aqueous solubility of VOR, inclusion complexes with α-cyclodextrin (α-CD), β-cyclodextrin (β-CD), γ-cyclodextrin (γ-CD), hydroxypropyl-cyclodextrin (HP-CD), hydr...

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Bibliographic Details
Published in:Pharmaceutical development and technology 2022-02, Vol.27 (2), p.228-241
Main Authors: Başaran, Ebru, Aykaç, Kadir, Yenilmez, Evrim, Büyükköroğlu, Gülay, Tunali, Yağmur, Demirel, Müzeyyen
Format: Article
Language:English
Subjects:
2-Hydroxypropyl-beta-cyclodextrin
Animals
antifungal activity
beta-Cyclodextrins
inclusion complexes
lyophilization
Mice
Mycoses
Solubility
Voriconazole
Voriconazole - pharmacology
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Summary:In our study, Voriconazole (VOR) was selected as an active agent to be used for the treatment of ocular fungal infections. To overcome low aqueous solubility of VOR, inclusion complexes with α-cyclodextrin (α-CD), β-cyclodextrin (β-CD), γ-cyclodextrin (γ-CD), hydroxypropyl-cyclodextrin (HP-CD), hydroxypropyl-β-cyclodextrin (HP-β-CD) hydroxypropyl-γ-cyclodextrin (HP-γ-CD), methyl-β-cyclodextrin (M-β-CD) and sulfabutylether-β-cyclodextrin (SBE-β-CD) were formulated. Characterization studies revealed that inclusion complexes were formulated successfully with the lyophilization method. Aqueous solubility of VOR was enhanced up to 86 fold with the formation of the inclusion complexes. MTT analyses results revealed the safety of the complexes on 3T3 mouse fibroblast cell lines while Microbroth Dilution Method revealed the remarkable antifungal activities of the complexes. Analyses results revealed that inclusion complexes will overcome the poor ocular bioavailability of VOR resulting inefficient treatment of severe ocular fungal infections.
ISSN:1083-7450
1097-9867
DOI:10.1080/10837450.2022.2037635