Spectroscopic and calorimetric studies on the interaction between PAMAM G4-OH and 5-fluorouracil in aqueous solutions

The results of spectroscopic measurements (an increase in solubility, equilibrium dialysis, 1H NMR titration) and calorimetric measurements (isothermal titration ITC) indicate spontaneous (ΔG<0) binding of 5-fluorouracil molecules by PAMAM G4-OH dendrimer with terminal hydroxyl groups in an aqueo...

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Published inSpectrochimica acta. Part A, Molecular and biomolecular spectroscopy Vol. 171; pp. 401 - 405
Main Authors Buczkowski, Adam, Urbaniak, Pawel, Piekarski, Henryk, Palecz, Bartlomiej
Format Journal Article
LanguageEnglish
Published England Elsevier B.V 15.01.2017
Subjects
1H NMR spectroscopy
5-Fluorouracil
Calorimetry - methods
Dendrimers - chemistry
Equilibrium dialysis
Fluorouracil - chemistry
Isothermal titration calorimetry
Nylons - chemistry
PAMAM G4-OH
Proton Magnetic Resonance Spectroscopy
Solubility measurements
Solutions
Temperature
PAMAM G4-OH
Isothermal titration calorimetry
1H NMR spectroscopy
5-Fluorouracil
Solubility measurements
Equilibrium dialysis
H NMR spectroscopy
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Summary:The results of spectroscopic measurements (an increase in solubility, equilibrium dialysis, 1H NMR titration) and calorimetric measurements (isothermal titration ITC) indicate spontaneous (ΔG<0) binding of 5-fluorouracil molecules by PAMAM G4-OH dendrimer with terminal hydroxyl groups in an aqueous solution. PAMAM G4-OH dendrimer bonds about n=8±1 molecules of the drug with an equilibrium constant of K=70±10. The process of saturating the dendrimer active sites by the drug molecules is exothermal (ΔH<0) and is accompanied by an advantageous change in entropy (ΔS>0). The parameters of binding 5-fluorouracil by PAMAM G4-OH dendrimer were compared with those of binding this drug by the macromolecules of PAMAM G3-OH and G5-OH. [Display omitted] •8 molecules of 5-fluorouracil are spontaneous combined by PAMAM G4-OH dendrimer.•Process of saturating the dendrimer active sites by the drug molecules is exothermal.•And is accompanied by an advantageous change in entropy (ΔS>0).•The constant of bonding 5-fluorouracil to the active site of G4-0H equals K =70±10.•With increasing the generation, both the number of 5-FU molecules and the K increase.
ISSN:1386-1425
1873-3557
DOI:10.1016/j.saa.2016.08.030