title: Study of the interactions of PAMAM G3-NH2 and G3-OH dendrimers with 5-fluorouracil in aqueous solutions.
abstract: The results of spectroscopic measurements (increase in solubility, equilibrium dialysis, (1)H NMR titration) and calorimetric measurements (isothermal titration ITC) indicate spontaneous (ΔG<0) bonding of 5-fluorouracil by both cationic PAMAM G3-NH2 dendrimer and hydroxyl PAMAM G3-OH dendrimer in aqueous solutions. PAMAM G3-NH2 dendrimer bonds about n= 25±8 drug molecules. Some of them n1= 5±1 are bonded by terminal amine groups with equilibrium constant K1= 3890±930, while the remaining ones n2= 24 ±3 are bonded by amide groups with equilibrium constant K2= 110±30. Hydroxyl PAMAM G3-OH dendrimer bonds n=6.0±1.6 molecules of 5-fluorouracil through tertiary amine groups with equilibrium constant K= 65±10. The parameters of bonding 5-fluorouracil by PAMAM G3-NH2 and G3-OH dendrimer were compared with those of bonding this drug by the macromolecules of PAMAM of generations G4-NH2, G5-NH2 and G5-OH.
authors.affiliation: Department of Biophysical Chemistry, Faculty of Chemistry, University of Lodz, Pomorska 165, Lodz 90-236, Poland. Electronic address: adam.buczkowski@chemia.uni.lodz.pl.
authors.forename: Adam
authors.initials: A
authors.lastname: Buczkowski
authors.affiliation: Department of Biophysical Chemistry, Faculty of Chemistry, University of Lodz, Pomorska 165, Lodz 90-236, Poland.
authors.forename: Dariusz
authors.initials: D
authors.lastname: Waliszewski
authors.affiliation: Department of Inorganic and Analytical Chemistry, Faculty of Chemistry, University of Lodz, Tamka 12, Lodz 91-403, Poland.
authors.forename: Pawel
authors.initials: P
authors.lastname: Urbaniak
authors.affiliation: Department of Biophysical Chemistry, Faculty of Chemistry, University of Lodz, Pomorska 165, Lodz 90-236, Poland.
authors.forename: Bartlomiej
authors.initials: B
authors.lastname: Palecz
mesh_terms: D000964:Antimetabolites, Antineoplastic / Q000737:chemistry*; D002151:Calorimetry; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D050091:Dendrimers / Q000737:chemistry*; D005472:Fluorouracil / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy / Q000379:methods; D012995:Solubility; D014867:Water / Q000737:chemistry
chemical_list: D000964:Antimetabolites, Antineoplastic; D050091:Dendrimers; C104700:PAMAM Starburst; D014867:Water; D005472:Fluorouracil
keywords: (1)H NMR spectroscopy; 5-Fluorouracil; Equilibrium dialysis; Hydroxyl-terminated PAMAM G3-OH dendrimer; Isothermal titration calorimetry; PAMAM G3-NH(2) dendrimer; Solubility measurements