Yeni Jenerasyon TREN ve Jeffamine® D230 Çekirdekli PEG Sonlu PAMAM Dendrimerler: Sentezi, Karakterizasyonu, Sulfametoksazol (SMZ) İçin Kompleks ve İn Vitro Salımı Çalışması

Year 2018, Volume: 8 Issue: 1, 189 - 197, 31.03.2018

Mustafa Ulvi Gürbüz Ali Serol Ertürk Metin Tülü

https://doi.org/10.21597/jist.407872

Abstract

Sulfametoksazol (SMZ) bir antibiyotiktir ve trimetoprim ile bakteriyostatik ve idrar yolu enfeksiyonlarının tedavisinde yaygın olarak kullanılır. SMZ ile ilgili sorun, zayıf su çözünürlüğü, dolayısıyla klinik uygulamalarda düşük biyoyararlanımıdır. Bu çalışmada, yeni jenerasyon TREN (T) ve Jeffamine® D230 (D) çekirdekli PEG bisamin sonlu (T5.PEG COOH ve D5.PEG COOH) PAMAM dendrimer sentezlendi. Sentezlenen dendrimerler, 1H NMR ve ATR-FTIR ile karakterize edilerek SMZ’nin ilaç taşıyıcı ve in vitro salımı çalışması araştırıldı. PAMAM dendrimerin SMZ’nin çözünürlüğünü arttırmada ki rol’ü 0.002 M dendrimer varlığında 54 kat ve T5.PEG COOH> D5.PEG COOH azalan sıralamada belirlendi. İn vitro salımı çalışması gösteriyor ki, 2 saat sonra SMZ’den en yavaş salımı SMZ-T5.PEG COOH (% 12.3) ilaç-dendrimer çözeltisinde gözlendi.

Keywords

İlaç taşıyıcı sistem, pegilasyon, poly(amidoamin) pamam, sulfametoksazol

New-Generation TREN and Jeffamine® D230 Core PEG Terminated PAMAM Dendrimers: Synthesis, Characterization, Complexation

Abstract

Sulfamethoxazole (SMZ) is an antibiotic and used widely in the treatment of bacteriostatic and urinary tract infections with trimethoprim. The problem with SMZ is its poor water solubility, therefore, low bioavailability in clinical applications. In this study, we synthesized new-generation TREN and Jeffamine® D230 core PEG bisamine terminated (T5.PEG COOH and D5.PEG COOH) PAMAM dendrimers. Synthesized dendrimers were characterized by 1H NMR, and ATR-FTIR investigated as drug carriers of SMZ and in vitro release studies. The role of PAMAM dendrimer in the solubility enhancement of SMZ was in the decreasing order of T5.PEG COOH> D5.PEG COOH, and 54-fold in the presence of 0.002 M dendrimer. In vitro release studies showed that after 2h, the slowest release of SMZ was observed from the drug-dendrimer solution of SMZ-T5.PEG COOH (% 12.3).

Keywords

Drug delivery system, pegylation, poly(amidoamine) pamam, sulfamethoxazole

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