Thermochemical and spectroscopic studies on the supramolecular complex of PAMAM-NH2 G4 dendrimer and 5-fluorouracil in aqueous solution

被引:33
作者
Buczkowski, Adam [1 ]
Urbaniak, Pawel [2 ]
Palecz, Bartlomiej [1 ]
机构
[1] Univ Lodz, Dept Phys Chem, PL-90236 Lodz, Poland
[2] Univ Lodz, Dept Inorgan & Analyt Chem, PL-91403 Lodz, Poland
关键词
PAMAM-NH2; G4; dendrimer; 5-Flurouracil; Isothermal titration calorimetry; H-1 NMR spectroscopy; Binding parameters; ISOTHERMAL TITRATION CALORIMETRY; POTENTIAL-DRUG CARRIERS; HUMAN GROWTH-HORMONE; IN-VITRO RELEASE; POLY(AMIDOAMINE) DENDRIMERS; BIOMEDICAL APPLICATIONS; SOLUBILITY ENHANCEMENT; SERUM-ALBUMIN; DELIVERY; ENCAPSULATION;
D O I
10.1016/j.ijpharm.2012.03.004
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The equilibrium of the formation of polyamidoamine dendrimer (PAMAM-NH2 G4) and an oncological drug, 5-fluorouracil (FU) in water at room temperature has been examined. Using calorimetric titration, the number of active sites in the dendrimer combining the drug molecules and the equilibrium constant of the dendrimer-drug complex were estimated. The addition of the drug to the dendrimer active sites is an exothermic process. This process is accompanied by a beneficial change in entropy. The number of drug molecules combined by the polymer was confirmed by means of H-1 NMR spectroscopy. (HNMR)-H-1 measurements show that the dendrimer macromolecule binds the drug molecules with superficial protonated or unprotonated amine groups. (C) 2012 Elsevier B.V. All rights reserved.
引用
收藏
页码:178 / 182
页数:5
相关论文
共 36 条
  • [1] Dendrimers as potential drug carriers; encapsulation of acidic hydrophobes within water soluble PAMAM derivatives
    Beezer, AE
    King, ASH
    Martin, IK
    Mitchell, JC
    Twyman, LJ
    Wain, CF
    [J]. TETRAHEDRON, 2003, 59 (22) : 3873 - 3880
  • [2] A PEGylated dendritic nanoparticulate carrier of fluorouracil
    Bhadra, D
    Bhadra, S
    Jain, S
    Jain, NK
    [J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2003, 257 (1-2) : 111 - 124
  • [3] Interaction between PAMAM-NH2 G4 dendrimer and 5-fluorouracil in aqueous solution
    Buczkowski, Adam
    Sekowski, Szymon
    Grala, Aleksandra
    Palecz, Danuta
    Milowska, Katarzyna
    Urbaniak, Pawel
    Gabryelak, Teresa
    Piekarski, Henryk
    Palecz, Bartlomiej
    [J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2011, 408 (1-2) : 266 - 270
  • [4] External electrostatic interaction versus internal encapsulation between cationic dendrimers and negatively charged drugs: Which contributes more to solubility enhancement of the drugs?
    Laboratory of Functional Membranes, Department of Chemistry, University of Science and Technology of China, Hefei, Anhui 230026, China
    不详
    [J]. J Phys Chem B, 2008, 30 (8884-8890): : 8884 - 8890
  • [5] Dendrimers as drug carriers: Applications in different routes of drug administration
    Cheng, Yiyun
    Xu, Zhenhua
    Ma, Minglu
    Xu, Tongwen
    [J]. JOURNAL OF PHARMACEUTICAL SCIENCES, 2008, 97 (01) : 123 - 143
  • [6] Dendrimers as potential drug carriers. Part I. Solubilization of non-steroidal anti-inflammatory drugs in the presence of polyamidoamine dendrimers
    Cheng, YY
    Xu, TW
    [J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2005, 40 (11) : 1188 - 1192
  • [7] Dendrimer-drug interactions
    D'Emanuele, A
    Attwood, D
    [J]. ADVANCED DRUG DELIVERY REVIEWS, 2005, 57 (15) : 2147 - 2162
  • [8] Conformational and structural analysis of bovine β lactoglobulin-A upon interaction with Cr+3
    Divsalar, A.
    Saboury, A. A.
    Moosavi-Movahedi, A. A.
    [J]. PROTEIN JOURNAL, 2006, 25 (02) : 157 - 165
  • [9] Poly(amidoamine) (PAMAM) dendrimers: from biomimicry to drug delivery and biomedical applications
    Esfand, R
    Tomalia, DA
    [J]. DRUG DISCOVERY TODAY, 2001, 6 (08) : 427 - 436
  • [10] NMR methods for the determination of protein-ligand dissociation constants
    Fielding, Lee
    [J]. PROGRESS IN NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY, 2007, 51 (04) : 219 - 242