Ali Serol Ertürk, Mustafa Ulvi Gürbüz, Metin TÜLÜ

Yüzey modifiye edilmiş farklı jenerasyon Jeffamine® D230 ve TREN-çekirdekli PAMAM dendrimerlerin kandesartan sileksetilin sulu çözünürlüğü üzerine etkisinin değerlendirilmesi

Dendrimerler üç boyutlu, çok dallı, monodispers, yıldız şeklinde makromoleküllerdir. Dendrimerlerin fiziksel ve kimyasal özellikleri çekirdek, tekrar eden dallar ve yüzey fonksiyonel grupları gibi moleküler yapı elemanları tarafından belirlenmektedir. Bu yapı elemanlarının türü, dendrimerlerin moleküler kapsülleme ve çözünürlük gibi özelliklerinde belirleyici olmaktadır. Bu çalışmada, yeni nesil Jeffamin® D230 (D) ve TREN (T) çekirdekli poli(amido amin) PAMAM dendrimerlerin, jenerasyon büyüklüğü (D2-D4 ve T2-T4), konsantrasyonu (0-1.0 mM) ve yüzey fonksiyonel gruplarının (NH2, COOH, TRIS), kandesartan sileksetil (CC)’in sudaki çözünürlüğüne olan etkisi araştırıldı. CC’nin (sudaki çözünürlük = 0.0048 mg/mL) gözlemlenen sudaki çözünürlük artışı, D4.COOH (5.25 mg/mL)> T4.COOH (4.77 mg/mL)> D4.TRIS (0.44 mg/mL)> T4.TRIS (0.32 mg/mL)> D4.NH2 (0.11 mg/mL)> T4.NH2 (0.08 mg/mL) sırasındadır.

Anahtar Kelimeler:

Dendrimer, poli(amido amin)) PAMAM, ilaç taşıyıcı

Evaluation of the effect of surface modified different generation Jeffamine® D230 and TREN-cored PAMAM dendrimers on the aqueous solubility of candesartan cilexetil

Dendrimers are three-dimensional, hyperbranched, monodisperse, and starburst macromolecules. The physical and chemical properties of dendrimers are attributed by their molecular construction units; namely, core, repetitive branching units, and terminal functional groups. The type of these units has also a determinant effect on their molecular encapsulation and solubility properties. In this study, the effect of generation size (D2-D4 and T2-T4), concentration (0-1.0 mM), and surface functional group (NH2, COOH, TRIS) of new-generation jeffamine® D230 (D) and TREN (T) core PAMAMs on the aqueous solubility of candesartan cilexetil (CC) was investigated. The observed solubility enhancement of CC (solubility in water = 0.0048 mg/mL) was in the order of D4.COOH (5.25 mg/mL)> T4.COOH (4.77 mg/mL)> D4.TRIS (0.44 mg/mL)> T4.TRIS (0.32 mg/mL)> D4.NH2 (0.11 mg/mL)> T4.NH2 (0.08 mg/mL).

Keywords:

dendrimer poly(amidoamin) PAMAM, drug carrier, candesertan cilexetil,

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