BERBERİN HCL İÇEREN SICAKLIĞA DUYARLI İN SİTU JELLEŞEN OFTALMİK İLAÇ TAŞIYICI SİSTEMİN TASARIMI VE DEĞERLENDİRİLMESİ

Abstract

Amaç: Bu çalışmada, oftalmik ilaç taşıyıcı sistemler için farklı fizyolojik uyaranlara duyarlı polimerlerin birleştirilmesiyle geliştirilen in situ jelleşen bir formülasyonun etkinliği araştırılmıştır. Etkin madde olarak berberin hidroklorür seçilmiştir. Çalışmanın temel amacı, uygulama kolaylığı sunan, oküler yüzeyde kalıcılığı artırarak terapötik etkinliği iyileştiren ve doz tekrarını azaltarak hasta uyumunu artıran yenilikçi bir oftalmik ilaç taşıyıcı sistem tasarlamaktı. Gereç ve Yöntem: Formülasyon, Pluronic F127, kitozan ve κ-karragenan polimerleri kullanılarak hazırlanmıştır. Pluronic F127 ve kitozan çözeltileri soğuk yöntemle, κ-karragenan çözeltisi ise 50°C’de hazırlanmıştır. Geliştirilen sistem berraklık, pH ve jelleşme sıcaklığı açısından değerlendirilmiştir. Elde edilen sonuçlara dayanarak, literatür verilerine uygun şekilde, optimal özellikler gösteren formülasyona 0.26 mg/ml konsantrasyonunda Berberin HCl eklenmiştir. Etken madde salım profili, 35°C’de pH 7.4 izotonik fosfat tamponu içinde diyaliz membran yöntemiyle değerlendirilmiştir. Stabilite çalışmaları kapsamında formülasyonlar 25 ± 2°C / %60 ± 5 bağıl nemde ve 5 ± 3°C’de bir ay boyunca saklanmıştır. Saklama süresi sonunda tüm analizler tekrarlanmış ve etken madde salım profilleri fark (f₁) ve benzerlik (f₂) faktörleri kullanılarak karşılaştırılmıştır. Sonuç ve Tartışma: Bu çalışmada, Berberin HCl içeren, üçlü polimer sistemiyle formüle edilmiş in situ jelleşen bir oftalmik ilaç taşıyıcı sistem geliştirilmiştir. Elde edilen bulgular, hasta uyumunu artırabilecek bu sistemin konvansiyonel göz damlalarına potansiyel bir alternatif olabileceğini göstermektedir; ancak bu durumun in vivo çalışmalarla desteklenmesi gerekmektedir.

Keywords

• Berberin HCl
• in situ jelleşme
• oftalmik formülasyon
• oftalmik ilaç taşıyıcı sistem
• polimer bazlı

Project Number

1919B012306007

DESIGN AND EVALUATION OF A TEMPERATURE RESPONSIVE IN SITU GELLING OPHTHALMIC DRUG DELIVERY SYSTEM CONTAINING BERBERINE HCL

Abstract

Objective: In this study, the efficacy of an in situ gelling formulation developed by combining polymers sensitive to different physiological stimuli for ophthalmic drug delivery systems was investigated. As the active pharmaceutical ingredient, berberine hydrochloride was selected. The primary aim of the study was to design an innovative ophthalmic drug delivery system that offers ease of administration, improves therapeutic efficacy by increasing retention on the ocular surface, and enhances patient compliance by reducing the frequency of dosing. Material and Method: The formulation was prepared using Pluronic F127, chitosan, and κ-carrageenan polymers. Pluronic F127 and chitosan solutions were prepared by the cold method, while the κ-carrageenan solution was prepared at 50°C. The developed system was evaluated in terms of clarity, pH, and gelation temperature. Based on the results obtained, Berberine HCl was added at a concentration of 0.26 mg/ml, in accordance with literature data, to the formulation that exhibited optimal characteristics. The drug release profile was evaluated at 35°C in pH 7.4 isotonic phosphate buffer using the dialysis membrane method. For the stability studies, the formulations were stored for one month at 25 ± 2°C / 60 ± 5% relative humidity and 5 ± 3°C. At the end of the storage period, all analyses were repeated and the drug release profiles were compared using difference (f₁) and similarity (f₂) factors. Result and Discussion: In this study, an in situ gelling ophthalmic drug delivery system containing berberine HCl was developed using a triple polymer system. The results suggest that this system, which may enhance patient compliance, could be a potential alternative to conventional eye drops; however, this needs to be supported by in vivo studies.

Keywords

• Berberine HCl
• in situ gelation
• ophthalmic drug delivery system
• ophthalmic formulation
• polymer based

Supporting Institution

TÜBİTAK

Project Number

1919B012306007

Thanks

Bu araştırma TÜBİTAK 2209A kapsamında desteklenmiştir. Teşekkür ederiz.

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