Elektroeğirme Yöntemi ile Antitüberkülostatik İlaç Yüklü Nanofiber Üretimi ve Karakterizasyonu

Year 2022, , 654 - 661, 30.06.2022

Hilal İrem Onurlu Dilek Bilgiç Alkaya , Serap Ayaz Seyhan , Sümeyye Cesur , Oğuzhan Gündüz

https://doi.org/10.35414/akufemubid.1027082

Abstract

Bu çalışma, Tüberküloz hastalarında antitüberküloz ilaçların etkili kombine formulasyonlarının üretilmesindeki zorluklar nedeniyle yeni kombinasyon formulasyonlarının değerlendirilmesi amacıyla tasarlanmıştır. Bunun için tedavide etkin antitüberkülostatikler olan pirazinamid, izoniazid, rifampisin ve etambutol biyolojik olarak parçalanabilen polikaprolakton (PCL), nanofiberlere yüklenmiş, böylelikle mevcut yan etkilerinin azaltılması da hedeflenmiştir. Mycobacterium Tuberculosis basiline karşı etkin bir tedavi için çalışmada etken maddelerin elektroeğirme yöntemiyle polimerik nanofiber formasyonları içine yüklenmesi gerçekleştirilmiştir. Bunun için öncelikle farklı konsantrasyonlarda hazırlanan PCL polimeri DMF:THF (1:1 w/w) karışımı içinde çözülmüş ve homojen bir çözelti verecek şekilde Tween 80 (%1) eklenmiştir. Elde edilen çözeltiden elektroeğirme yöntemi ile lifler elde edilmiştir. Sistem, farklı konsantrasyon ve voltajlar (17 kV, 20 kV, 23 kV, 26 kV ve 29 kV) uygulanarak optimize edilmiştir. Optimizasyon çalışmasında, %12 konsantrasyonda hazırlanan çözeltiden en uygun PCL fiber yapısı elde edilmiştir. Sistem optimizasyonu sonunda 4 farklı etken maddenin 20 kV, 1.0 ml/h akış hızı, 18 cm plaka mesafesi koşullarında metanol içerisinde çözeltilerinde tek tek ve kombinasyonları halinde fiber ile kaplanması sağlanmıştır. Çözeltilerinin elektriksel iletkenliği, yüzey gerilimi, yoğunluk ve viskozite özellikleri belirlenmiştir. Daha sonra, elektroeğirme yöntemiyle elde edilen nanofiberlerin karakterizasyon amacıyla SEM görüntüleri alınmış ve ilaç salınımı in vitro olarak incelenmiştir. İlaç salımı pH: 7.4 fosfat tamponu ile gerçekleştirilmiş ve salım UV spektrofotometresi ile analiz edilmiştir. İlaç kaplı liflerden ilaç salımı, uzun süreli ve kontrollü bir şekilde sağlanmıştır.

Keywords

Antitüberküloz, Elektroeğirme, Polikaprolakton, İlaç Salım

Supporting Institution

Marmara Üniversitesi Bilimsel Araştırma Projeleri Komisyonu Başkanlığı

Project Number

SAG-C-YLP-120917-0517

Production and Characterization of Antituberculostatic Drug-Loaded Nanofibers by Electrospinning Method

Abstract

This study was designed to evaluate new combination formulations because of the difficulties in producing effectively combined formulations of antituberculosis drugs in tuberculosis patients. For this, pyrazinamide, isoniazid, rifampicin, and ethambutol, which are effective antituberculostatics in treatment, are loaded on biodegradable polycaprolactone nanofibers, thus reducing the existing side effects. Loading of active ingredients into polymeric nanofiber formulations by electrospinning method in the study for an effective treatment against Mycobacterium Tuberculosis bacillus. For this, polycaprolactone (PCL) polymer prepared at different concentrations was dissolved in DMF: THF (1:1 w/w) mixture, and Tween 80 (1%) was added to give a homogeneous solution. Nanofibers were obtained from the solution obtained by the electrospinning method. The system was optimized by applying different concentration voltages (17 kV, 20 kV, 23 kV, 26 kV, and 29 kV). In the system optimization study, the most suitable PCL nanofiber structure was obtained from the solution prepared at 12% concentration. At the end of the system optimization, 4 different active substances were coated with fiber individually or in combinations in their solutions in methanol at 20 kV, 1.0 ml/h flow rate, 18 cm plate distance conditions. The electrical conductivity, surface tension, density, and viscosity properties of the solutions were determined. Then, SEM images were taken for characterization of nanofibers obtained by electrospinning method, and drug release was investigated in vitro. Drug release was performed with pH: 7.4 phosphate buffer and release were analyzed by UV spectrophotometer. Drug release from drug-coated nanofibers was achieved in a long-term and controlled manner.

Keywords

Antituberculosis, Electrospinning, Polycaprolactone, Drug Release

Project Number

SAG-C-YLP-120917-0517

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