Çiğdem YÜCEL, Gökçe ŞEKER KARATOPRAK, Tuğba EREN BÖNCÜ, Rukiye Nur AKPOLAT

Antioksidan Etkili Rutin İçeren Mikroemülsiyon ve Mikroemülsiyon Jel Formülasyonlarının Geliştirilmesi, Karakterizasyonu ve Etkinliğinin İncelenmesi

Amaç: Çalışmada antioksidan etkili doğal bileşik olan rutinin, mikroemülsiyon (ME) ve mikroemülsiyon jel (MEj)formülasyonlarının geliştirilmesi ve uzatılmış antioksidan etkinliğinin değerlendirilmesi amaçlanmıştır.Gereç ve Yöntemler: Farklı oranlarda yağ/su/yüzey etkin madde:yardımcı yüzey etkin madde kullanılarak hazırlananME formülasyonlarının damlacık büyüklüklükleri, zeta potansiyel değerleri, viskoziteleri ve bekletme, santrifüj vedondurup çözme işlemleri sonrasındaki stabiliteleri tayin edilmiştir. Altı farklı ME formülasyonu arasından belirlenenstabil formülasyonlar ile MEj formülasyonları, %1’lik (a/h) Karbopol 938 kullanılarak hazırlanmıştır. Karakterizasyonçalışmaları yanı sıra L929 fare fibroblast hücre hattı kullanılarak hücre kültüründe toksisite testi, in vitro salım ve hücregeçiş çalışmaları yapılmıştır. Veriler ışığında en iyi belirlenen formülasyonun (F2 ME) antioksidan aktivitesi, 1,1-difenil-2-pikrilhidrazil (DPPH●) ve (2,2-Azino-bis3-etilbenzotiyazolin-6-sülfonik asit) (ABTS●+) radikal süpürücü etkiile belirlenmiştir.Bulgular: Altı farklı mikroemülsiyon formülasyonu geliştirilmiş ve karakterize edilmiştir. Toksisite çalışmasına göre,rutin çözeltisi ve rutin ile geliştirilen formülasyonlar toksik bulunmamıştır. Karakterizasyon, in vitro salım ve hücregeçiş çalışması verileri ile en iyi formülasyon olarak belirlenen F2 kodlu ME formülasyonundan salınan rutin miktarınınantioksidan etkisi incelenmiş ve DPPH●ve ABTS+● radikallerini süpürücü etkisi ispatlanmıştır.Sonuç: Sonuç olarak, bu çalışma ile toksik etkisi bulunmayan, yeni, rutin yüklü ME ve MEj formülasyonları başarıylageliştirilmiş, uzatılmış antioksidan etkinlik kanıtlanmıştır. Bu çalışmada geliştirilen rutin yüklü ME formülasyonununtopikal uygulama için potansiyel oluşturduğu düşünülmektedir.

Development, Characterization and Evaluation of Effectiveness of Microemulsion and Microemulsion Gel Formulations Containing Antioxidant Effective Rutin

Aim: In this study, it was aimed to develop microemulsion and microemulsion gel formulations of a natural product (rutin) that possesses antioxidant effect and to evaluate its prolonged antioxidant activity. Material and Methods: The droplet size, zeta potential, viscosity values and stability profiles following the holding, centrifugation and freeze-thawing processes applied to the ME formulations, prepared by using different ratios of oil/water/surfactant and co-surfactant, were determined. The most stable formulations out of the six different ME formulations were selected and then, the ME gel formulations were prepared using 1% (w/v) Carbopol 938. Besides characterization studies, toxicity test on cell culture with using L929 mouse fibroblast cell line, in vitro release and cell permeation studies were performed. Antioxidant activity of optimum formulation (F2 coded ME) were measured using 1,1-diphenyl-2-picrylhydrazyl (DPPH) ve 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid (ABTS●+) radical scavenging effect. Results: Six different ME formulations were developed and characterized. According to the toxicity study, rutin solution and rutin loaded formulations were not toxic. The antioxidant effect of the rutin released from the F2 coded ME formulation which was determined to be optimum formulation by characterization, in vitro release and cell permeation studies data was investigated and the scavenging effects of DPPH and ABTS + radicals were proven. Conclusion: In conclusion, new, nontoxic, rutin loaded ME and ME gel formulations were successfully developed and prolonged antioxidant activity was proved. It is assumed that the rutin loaded ME formulation developed in this study has a great potential for topical application.

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