DEVELOPMENT OF BESIFLOXACIN HCL LOADED OCULAR IN SITU GELS; IN VITRO CHARACTERIZATION STUDY

Year 2023, , 39 - 50, 20.01.2023

Heybet Kerem Polat , Sedat Ünal

https://doi.org/10.33483/jfpau.1154051

Cited By: 1

Abstract

Objective: The aim of this study is to develop in situ gel formulations containing besifloxacin hydrochloride are heat triggered, which are prepared by using different poloxamer and derivatives different polymers that will change the gelling temperature to increase corneal contact time, regulate drug release, improve ocular bioavailability and increase patient compliance increase mucoadhesion.

Material and Method: Various concentrations of poloxamer 188 (P188) and poloxamer 407 (P407) were used to create the in situ forming gels. To increase the gel's capacity for bioadhesion, mucoadhesives such hydroxypropylmethyl cellulose (HPMC) or hydroxyethyl cellulose (HEC) were included in the formulations. Drug release in vitro, sol-gel transition temperature, rheological behavior, pH, clarity, and mucoadhesion force were all assessed for the produced formulations.

Result and Discussion: The developed formulations' gelation temperatures ranged from 29 to 35°C. The preparations' viscosity and mucoadhesion force increased with increasing P407, HPMC, and HEC concentrations. Besifloxacin HCl forms in situ gel formulas with K1, K2, K3, and K6 suited for mucoadhesion characteristics, gelation temperature, and viscosity. These formulations exhibit pseudoplastic flow. Increasing polymer concentrations resulted in a reduction in the burst release of the formulations. However, at the end of 6 hours, drug release was finished in all formulations. The results show that in situ gels containing P407 and P188 show promise for besifloxacin HCl application.

Keywords

Besifloxacin HCl, gel, in situ, ocular, poloxamer

BESİFLOKSASİN HCL YÜKLÜ OKÜLER İN SİTU JELLERİN GELİŞTİRİLMESİ; İN VİTRO KARAKTERİZASYON ÇALIŞMASI

Abstract

Amaç: Bu çalışmanın amacı, kornea temas süresi artırılmış, ilaç salımı düzenlenmiş, oküler biyoyararlanımı iyileştirilmiş ve hasta uyuncunu artırmak amacıyla jelleşme sıcaklığını değiştirecek farklı poloksomer türevlerinin ve mukoadhezyonu değiştirecek farklı polimerlerin kullanılması ile hazırlanan ısı ile tetiklenip jelleşen ve besifloksasin hidroklorür içeren in situ jel formülasyonları geliştirmektir.

Gereç ve Yöntem: İn situ jeller oluşturmak için poloksamer 188 (P188) ve poloksamer 407 (P407)'nin farklı farklı konsantrasyonları denenmiş bununla beraber in situ jelin biyo-yapışkanlık özelliklerini artırmak amacıyla formülasyonlara hidroksipropilmetil selüloz (HPMC) veya hidroksietil selüloz (HEC) gibi muko yapışkanlar ilave edilmiştir. Üretilen formülasyonların in vitro ilaç salımı, sol-jel geçiş sıcaklığı, reolojik davranışları, pH, berraklık ve mukoadezif kuvveti değerlendirilmiştir.

Sonuç ve Tartışma: Geliştirilen formülasyonların jelleşme sıcaklıkları 29 ila 35°C arasında olduğu belirlenmiştir. Preparatların viskozitesi ve mukoadezyon kuvveti, artan P407, HPMC ve HEC konsantrasyonları ile artmış. Patlama salımında bir azalma ile sonuçlanmıştır. Bununla beraber 6 saat sonunda bütün formülasyonlarda ilaç salımı bitmiştir. Jelleşme sıcaklığı, viskoziteleri ve mukoadhezyonları uygun olduğu için K1, K2, K3 ve K6 formülasyonları seçilmiş ve bu formülasyonlara besifloksasin HCl yüklenmiştir. Bu dört formülasyonun psödoplastik akış sergilediği tespit edilmiştir. Artan polimer konsantrasyonlarında formülasyonların patlama salımında bir azalma ile sonuçlanmıştır. Bununla beraber 6 saat sonunda bütün formülasyonlarda ilaç salımı bitmiştir. Sonuçlar, besifloksasin HCl uygulaması için P407 ve P188 içeren in situ jellerin umut vadettiğini göstermektedir.

Keywords

Besifloksasin HCl, in situ, jel, oküler, poloksamer

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