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

BAŞARAN E., AYKAÇ K., Yenilmez E., BÜYÜKKÖROĞLU G., TUNALI Y., DEMİREL M.

PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY, cilt.27, sa.2, ss.228-241, 2022 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 27 Sayı: 2
  • Basım Tarihi: 2022
  • Doi Numarası: 10.1080/10837450.2022.2037635
  • Dergi Adı: PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Business Source Elite, Business Source Premier, Chemical Abstracts Core, EMBASE, International Pharmaceutical Abstracts, MEDLINE
  • Sayfa Sayıları: ss.228-241
  • Anahtar Kelimeler: Voriconazole, inclusion complexes, lyophilization, antifungal activity, IN-SITU GEL, X-RAY-DIFFRACTION, BETA-CYCLODEXTRIN, POLYMERIC NANOPARTICLES, DRUG, DELIVERY, SOLUBILITY, SYSTEMS, ENDOPHTHALMITIS
  • Anadolu Üniversitesi Adresli: Evet

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 alpha-cyclodextrin (alpha-CD), beta-cyclodextrin (beta-CD), gamma-cyclodextrin (gamma-CD), hydroxypropyl-cyclodextrin (HP-CD), hydroxypropyl-beta-cyclodextrin (HP-beta-CD) hydroxypropyl-gamma-cyclodextrin (HP-gamma-CD), methyl-beta-cyclodextrin (M-beta-CD) and sulfabutylether-beta-cyclodextrin (SBE-beta-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.