Gözde AYGÜL, Fırat YERLİKAYA, Secil CABAN, İmran VURAL, Yılmaz ÇAPAN

Paklitaksel yüklü nanopartiküllerin formülasyonu ve in vitro incelenmesi

Bu çalışmada, paklitaksel yüklü PLGA nanopartikülleri emülsifikasyon-solvent difüzyon metodu kullanılarak hazırlanmış ve polimer ve yüzey aktif madde konsantrasyonunun paklitaksel yüklenmiş PLGA nanopartiküllerini partikül büyüklüğü, zeta potansiyel, enkapsülasyon etkinliği ve in vitro salım oranı üzerine etkisi incelenmiştir. Hazırlanan nanopartiküllerin ortalama partikül büyüklüğünün 190 ve 235 nm arasında olduğu gözlemlenmiştir. Paklitakselin nanopartiküllerin içine ankapsülasyon etkinliği %53-89 arasında bulunmuş olup nanopartiküllerin salım profillerinde başlangıçta patlama etkisini takiben 7 günlük kontrollü salım gözlemlenmiştir. In vitro sitotoksisite çalışmaları ilaç yüklü nanopartikül formülasyonlarının yüklenmemiş olanlara kıyasla daha sitotoksik olduğunu göstermiştir. Yapılan çalışmalar sonucunda, hazırlanan formülasyonun paklitaksel taşınmasında kullanılabileceği bulunmuştur.

Anahtar Kelimeler:

Paklitaksel, PLGA, Formülasyon, Nanopartiküller

Formulation and in Vitro Evaluation of Paclitaxel Loaded Nanoparticles

In this study, paclitaxel loaded PLGA nanoparticles were prepared using emulsification-solvent diffusion method and the influences of polymer and emulsifier concentrations on particle size, zeta potential, encapsulation efficiency and in vitro release rate of the paclitaxel loaded PLGA nanoparticles were evaluated. It was observed that average particle size of the prepared nanoparticles were between 190 and 235 nm. The encapsulation efficiency of paclitaxel into the nanoparticles was between 53-89% and the release profiles of the nanoparticles exhibited an initial burst effect followed by a controlled release for 7 days. In vitro cytotoxicity studies showed that drug loaded nanoparticle formulation was more cytotoxic than the blank nanoparticle formulation. According to the results of the studies performed, it can be concluded that prepared nanoparticle formulations may be a considerable approach for paclitaxel delivery.

Keywords:

Paclitaxel, PLGA, Formulation, Nanoparticles,

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