Formulation Development of Lornoxicam Loaded Heat Triggered Ocular In-situ Gel Using Factorial Design        
Yazarlar (9)
Heybet Kerem Polat
T.C. Sağlık Bakanlığı,, Türkiye
Sedat Ünal
Erciyes Üniversitesi, Türkiye
Eren Aytekin
Hacettepe Üniversitesi, Türkiye
Nasıf Fatih Karakuyu
Süleyman Demirel Üniversitesi, Türkiye
Esra Pezik
Erzincan Binali Yıldırım Üniversitesi, Türkiye
Muhammet Kerim Haydar
Erzincan Binali Yıldırım Üniversitesi, Türkiye
Dr. Öğr. Üyesi Nihat KURT Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Osman Doğan
Hacettepe Üniversitesi, Türkiye
Behzad Mokhtare
Dicle Üniversitesi, Türkiye
Makale Türü Özgün Makale
Makale Alt Türü SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale
Dergi Adı Drug Development and Industrial Pharmacy
Dergi ISSN 0363-9045 Wos Dergi Scopus Dergi
Dergi Tarandığı Indeksler SCI-Expanded
Dergi Grubu Q3
Makale Dili İngilizce
Basım Tarihi 09-2023
Cilt No 49
Sayı 9
Sayfalar 601 / 615
DOI Numarası 10.1080/03639045.2023.2264932
Makale Linki http://dx.doi.org/10.1080/03639045.2023.2264932
Özet
Objective: In the current research, lornoxicam-loaded in situ gels were developed, and their potential usage in ocular inflammation was evaluated. Significance: Lornoxicam cyclodextrin complex prepared with hydroxypropyl methylcellulose and poloxamer P407 because of the low viscosity of in situ gels to provide easy application. However, washing and removing it from the ocular surface becomes difficult due to the gelation formation with heat. Methods: A three-level factorial experimental design was used to evaluate the effects of poloxamer 407 concentration, polymer type, and polymer concentration on viscosity, pH, gelation capacity, gelation time, and gelation temperature, which were considered the optimal indicators of lornoxicam-containing formulations. Results: As a result of the three-level factorial experimental design, the optimized formulation contained 15 (%w/v) poloxamer 407 and 1 (%w/v) hydroxypropyl methylcellulose. The optimize formulation viscosity 25 °C = 504 ± 49cP, viscosity 35 °C = 11247 ± 214cP, pH = 6.80 ± 0.01, gelation temprature = 35 ± 0.2 °C, and gelation time= 34 ± 0.2 s was obtained. In the in vitro release studies, 68% of lornoxicam was released with a burst effect in the first three hours; then, the release continued for eight hours with controlled release. Release kinetics of the formulations were modeled mathematically, and it was found to be compatible with the Korsemeyer-Peppas and Weibull models. In cell culture studies, cell viability at 100 µg/mL was 83% and 96% for NL6 and NL6-CD, respectively. In Draize’s in vivo test, no negative conditions occurred in rats. Conclusions: Therefore, the NL6-CD formulation has the potential to be a favorable option for treating ocular inflammation.
Anahtar Kelimeler
cell viability | cyclodextrin | draize test | Lornoxicam | release kinetic