Etodolak Yüklü Poli Laktid-Ko-Glikolid Nanopartikülleri: Formülasyon ve İn Vitro Karakter

Year 2009, Issue: 2, 105 - 114, 01.06.2009

Yasemin Çırpanlı Cecile Robineau Yılmaz Çapan Sema Çalış

Abstract

Etodolak prostaglandin sentezini inhibe eden nonsteroidal antienflamatuar ilaçtır NSAİİ . NSAİİ’lar ağrı ve inflamasyon semptomlarını tedavi ederler. Etodolak artrit ve osteoartritin neden olduğu ağrı veya inflamasyon tedavisinde kullanılır. Tedavi sırasındaki en önemli yan etkileri genellikle gastrontestinal rahatsızlıklardır ve nanopartiküler ilaç taşıyıcı sistemler bu yan etkileri azaltabilir. Bu çalışmada, nanopartiküller nanopresipitasyon tekniğine göre hazırlanmıştır. Partikül büyüklüklüğü ve zeta potansiyel ölçümleri Malvern Zetasizer Malvern Instruments, UK aleti ile yapılmıştır. Ortalama partikül büyüklükleri boş ve etodolak yüklü nanopartiküller için sırasıyla 175 ve 184 nm bulunmuştur ve bütün fomülasyonlar için polidispersite indeksleri PI 0.2’den küçüktür. Zeta potansiyel değerleri negatiftir. Taramalı elektron mikroskobu Jeol- SEM ASID-10, Japan ile incelenen nanopartikül fotoğraflarında yüzey düzgün ve küresel bulunmuştur. Formülasyonun ilaç yükleme değeri % 17 bulunmuştur. Nanopartikül formülasyonu 144 saate kadar uzayan kontrollü salım profili göstermiştir. Bu sonuçlar etodolak yüklü PLGA nanopartiküllerinin bu antiinflamatuvar ilaç için umut vaadedici taşıyıcı system olabileceğini göstermiştir.

Keywords

Etodolak, poli laktid-ko-glikolid, nanopartikül, in vitro karakterizasyon

Etodolac Loaded Poly Lactide-Co-Glycolide Nanoparticles: Formulation and In Vitro Characterization

Abstract

Etodolac is a nonsteroidal anti-inflammatory drug NSAID which blocks the enzyme that makes prostaglandins. NSAIDs treat the symptoms of pain and inflammation. Etodolac is used to treat pain or inflammation caused by arthritis or osteoarthritis. The commonest side effects during therapy are generally gastrointestinal disturbances and nanoparticulate drug delivery systems may reduce these side effects. In this study, nanoparticles were prepared with nanoprecipitation technique. Particle size and zeta potential measurements were performed by Malvern Zetasizer Malvern Instruments, UK . Mean particle sizes measured were 175 nm and 184 nm for blank and etodolac loaded nanoparticles, respectively and polydispersity indices PI were lower than 0.2 for all formulations. Zeta potential values were negative. Examination of photographs of the nanoparticles with Scanning Electron Microscope Jeol-SEM ASID-10, Japan revealed that the surface were smooth and spherical. The encapsulation efficiency value of the formulation was found to be 17 %. Nanoparticle formulation showed a significant controlled release profile extended up to 144 h. These results indicated that etodolac-loaded PLGA nanoparticles might provide a promising carrier system for the effective delivery of this anti-inflammatory drug.

Keywords

Etodolac, poly lactide-co-glycolide, nanoparticle, in vitro characterization

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