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

ArticleAçık Erişim

Özet

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. © 2022 Informa UK Limited, trading as Taylor & Francis Group.

Anahtar Kelimeler

antifungal activityinclusion complexeslyophilizationVoriconazole2-Hydroxypropyl-beta-cyclodextrinAnimalsbeta-CyclodextrinsMiceMycosesSolubility2 hydroxypropyl beta cyclodextrinalpha cyclodextrinbeta cyclodextrincyclodextrin derivativegamma cyclodextrinmethyl beta cyclodextrinbeta cyclodextrin derivativemycosis3T3 cell lineanimal cellanimal experimentanimal modelArticleAspergillusbroth dilutionCandida albicansCandida glabrataCandida parapsilosiscomplex formationcontrolled study
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Tam Kayıt
AlanDeğerDil
dc.contributor.authorBaşaran, Ebru
dc.contributor.authorAykaç, Kadir
dc.contributor.authorYenilmez, Evrim
dc.contributor.authorBüyükköroğlu, Gülay
dc.contributor.authorTunali, Yağmur
dc.contributor.authorDemirel, Müzeyyen
dc.date.accessioned2026-10-18T20:27:32.119855512Z
dc.date.available2026-10-18T20:27:32.119855512Z
dc.date.issued2022
dc.description.abstractIn 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. © 2022 Informa UK Limited, trading as Taylor & Francis Group.
dc.description.sponsorshipThe study was financed by The Scientific And Technological Research Council of Turkey (TÜBİTAK) with the Project Number of 216S731. The authors would like to thank Medicinal Plants, Drugs and Scientific Research Centre (AUBIBAM) management for SEM, Doping and Narcotic Substances Analysis Laboratory (DOPNA-LAB) for FT-IR and 1H-NMR analyses to Eskişehir Technical University Faculty of Engineering and Architecture Department of Materials Engineering for XRD analyses.
dc.identifier.doi10.1080/10837450.2022.2037635
dc.identifier.eissn1097-9867
dc.identifier.endpage241
dc.identifier.issn1083-7450
dc.identifier.issue2
dc.identifier.pmid35107405
dc.identifier.scopus2-s2.0-85124820298
dc.identifier.startpage228
dc.identifier.urihttps://rdlopen.rawdatalibrary.net/r/ebyu/12657
dc.identifier.volume27
dc.identifier.wosWOS:000752320900001
dc.language.isoen
dc.publisherTaylor and Francis Ltd.
dc.relation.ispartofPharmaceutical Development and Technology
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectantifungal activity
dc.subjectinclusion complexes
dc.subjectlyophilization
dc.subjectVoriconazole
dc.subject2-Hydroxypropyl-beta-cyclodextrin
dc.subjectAnimals
dc.subjectbeta-Cyclodextrins
dc.subjectMice
dc.subjectMycoses
dc.subjectSolubility
dc.subject2 hydroxypropyl beta cyclodextrin
dc.subjectalpha cyclodextrin
dc.subjectbeta cyclodextrin
dc.subjectcyclodextrin derivative
dc.subjectgamma cyclodextrin
dc.subjectmethyl beta cyclodextrin
dc.subjectbeta cyclodextrin derivative
dc.subjectmycosis
dc.subject3T3 cell line
dc.subjectanimal cell
dc.subjectanimal experiment
dc.subjectanimal model
dc.subjectArticle
dc.subjectAspergillus
dc.subjectbroth dilution
dc.subjectCandida albicans
dc.subjectCandida glabrata
dc.subjectCandida parapsilosis
dc.subjectcomplex formation
dc.subjectcontrolled study
dc.titleFormulation and characterization studies of inclusion complexes of voriconazole for possible ocular application
dc.typeArticle
dspace.entity.typePublication
rdl.citation.scopus7
rdl.citation.wos8
rdl.departmentDepartment of Pharmaceutical Technology, Faculty of Pharmacy, Erzincan Binali Yıldırım University, Erzincan, Turkey.
rdl.source.indexSCOPUS
rdl.source.indexWOS
rdl.source.indexPUBMED
rdl.wos.indexScience Citation Index Expanded (SCI-EXPANDED)