Formulation of Hesperidin‐loaded In situ Gel for Ocular Drug Delivery: A Comprehensive Study        
Yazarlar (12)
Sefa Gözcü
Erzincan Binali Yıldırım Üniversitesi, Türkiye
Heybet Kerem Polat
T.C. Sağlık Bakanlığı,, Türkiye
Yakup Gültekin
Selçuk Üniversitesi, Türkiye
Sedat Ünal
Erciyes Üniversitesi, Türkiye
Nasıf Fatih Karakuyu
Süleyman Demirel Üniversitesi, Türkiye
Esra Köngül Şafak
Erciyes Üniversitesi, Türkiye
Osman Doğan
Hacettepe Üniversitesi, Türkiye
Esra Pezik
Erzincan Binali Yıldırım Üniversitesi, Türkiye
Muhammet Kerim Haydar
Erzincan Binali Yıldırım Üniversitesi, Türkiye
Eren Aytekin
Hacettepe Üniversitesi, Türkiye
Dr. Öğr. Üyesi Nihat KURT Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Burak Batuhan Laçin
Atatürk Üniversitesi, Türkiye
Makale Türü Açık Erişim Özgün Makale
Makale Alt Türü SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale
Dergi Adı Journal of the Science of Food and Agriculture
Dergi ISSN 0022-5142 Wos Dergi Scopus Dergi
Dergi Tarandığı Indeksler SCI-Expanded
Dergi Grubu Q1
Makale Dili Türkçe
Basım Tarihi 03-2024
Cilt No 104
Sayı 10
Sayfalar 5846 / 5859
DOI Numarası 10.1002/jsfa.13407
Makale Linki http://dx.doi.org/10.1002/jsfa.13407
Özet
BACKGROUND: Allergic conjunctivitis is one of the most common eye disorders. Different drugs are used for its treatment. Hesperidin is an active substance isolated from Citrus sinensis L. (Rutaceae) fruit peels, with known anti-inflammatory activity but low solubility. It was complexed with cyclodextrin and encapsulated in situ gel to extend its duration in the eye. RESULTS: The optimized formulation comprised 1% hesperidin, 1.5% hydroxyethyl cellulose, and 16% poloxamer 407. The viscosity at 25 °C was 492 ± 82 cP, and at 35 °C it was 8875 ± 248 cP, the pH was 7.01 ± 0.03, gelation temperature was 34 ± 1.3 °C, and gelation time was 33 ± 1.2 s. There was a 66% in vitro release in the initial 2 h, with a burst effect. A lipoxygenase (LOX) inhibition test determined that hesperidin was active at high doses on leukotyrens seen in the body in allergic diseases. In cell-culture studies, the hesperidin cyclodextrin complex loaded in situ gel, BRN9-CD (poloxamer 16%, hydroxy ethyl cellulose (HEC) 1.5%), enhanced cell viability in comparison with the hesperidin solution. It was determined that BRN9-CD did not cause any irritation in the ocular tissues in the Draize test. CONCLUSION: The findings of this study demonstrate the potential of the in situ gel formulation of hesperidin in terms of ease of application and residence time on the ocular surface. Due to its notable LOX inhibition activity and positive outcomes in the in vivo Draize test, it appears promising for incorporation into pharmaceutical formulations. © 2024 The Authors. Journal of The Science of Food and Agriculture published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.
Anahtar Kelimeler
cell viability | cyclodextrin | Draize test | hesperidin | lox inhibition