Nagihan UGURLU, Ebru ERDAL, Yesim ALTAY ASLAN

Oküler Enfeksiyonların Topikal Tedavisinde Nanopartiküler Sistemlerin Hazırlanması ve Karakterizasyonu

Çalışmada, PLGA nanopartiküllere besifloksasin etken maddesi yüklenmiş ve elde edilen yapının bakteriyel konjuktivit tedavisi için kontrollü ilaç salım sistemi olarak kullanılabilirliği araştırılmıştır. Besifloksasin, sistemik bir formülasyon içermediği ve hem gram-pozitif hem de gram-negative patojenlere karşı etkili olduğu için seçilmiştir. Topikal uygulama sonrasında, besifoksasinin uygulama bölgesindeki kalım süresini uzatmak amacıyla besifloksasinin nanopartiküllere yüklenmiş ve etkinliği test edilmiştir. Bu amaçla, besifloksasin yüklü PLGA nanopartiküller karakterize edilmiş, toksisite ve in vitro salım çalışmaları yapılmıştır. Nanopartiküller, morfolojik yapısı taramalı elektron mikroskobu, boyut ve yük analizi Zeta Sizer, fizikokimyasal yapısı Fourier Dönüşümü Kızılötesi Spektrometresi (FTIR) ile karakterize edilmiştir. Zeta Sizer sonuçlarına göre nanopartiküllerin ortalama 200nm boyutuna sahip olduğu belirlenmiştir ve SEM görüntüleri de sonuçları destekler niteliktedir. Nanopartikül yıkama solüsyonunda bulunan ilaç miktarının belirlenmesi sonucu, başlangıçtaki besifloksasin aktif madde konsantrasyonunun %40’ının PLGA nanopartiküllere yüklendiği tespit edilmiştir. Nanopartiküllerden besifloksasinin salım profili, ani bir salım şeklinde olmayıp daha yavaş ve kontrollü bir şekilde salındığı görülmüştür.

Preparation and Characterization of Nanoparticular Systems for Topical Treatment of Ocular Infections

In this study, the active ingredient of besifloxacin was loaded into PLGA nanoparticles and the usability of the obtainednanoparticles as a controlled drug release system for the treatment of bacterial conjunctivitis was investigated. Besifloxacin was selected because it does not contain a systemic formulation and is effective against both gram-positive andgram-negative pathogens. After topical application, besifloxacin was loaded into PLGA nanoparticles and tested for effectiveness in order to prolong the residence time of besifoxacin. For this purpose, besifloxacin loaded PLGA nanoparticles werecharacterized and toxicity and in vitro release studies were performed. Nanoparticles were characterized as morphologicalstructure by scanning electron microscopy (SEM), size and charge analysis by Zeta Sizer and physicochemical structure byFourier Transform Infrared Spectrometry (FTIR). According to the Zeta Sizer results, the nanoparticles have a mean sizeof 200nm and the SEM images support the results. It was determined that 40% of the initial concentration of besifloxacinactive substance was loaded on PLGA nanoparticles as a result of the determination of the amount of drug found in thesupernatant. The release pattern of besifloxacin from the nanoparticles was not found to be burst effect but was releasedin a slower and more controlled manner.

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