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

Year 2018, Volume: 22 Issue: 3, 928 - 937, 01.06.2018

Ali Serol Ertürk , Mustafa Ulvi Gürbüz , Metin Tülü

https://doi.org/10.16984/saufenbilder.312237

Abstract

 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.

Keywords

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

Abstract

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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