Interaction between PAMAM-NH2 G4 dendrimer and 5-fluorouracil in aqueous solution

被引:46
|
作者
Buczkowski, Adam [1 ]
Sekowski, Szymon [2 ]
Grala, Aleksandra [1 ]
Palecz, Danuta [2 ]
Milowska, Katarzyna [2 ]
Urbaniak, Pawel [3 ]
Gabryelak, Teresa [2 ]
Piekarski, Henryk [1 ]
Palecz, Bartlomiej [1 ]
机构
[1] Univ Lodz, Dept Phys Chem, PL-90236 Lodz, Poland
[2] Univ Lodz, Dept Gen Biophys, PL-90237 Lodz, Poland
[3] Univ Lodz, Dept Inorgan & Analyt Chem, PL-91403 Lodz, Poland
关键词
PAMAM-NH2; G4; dendrimer; 5-Flurouracil; Solubility enhancement; Equilibrium microdialysis; ISOTHERMAL TITRATION CALORIMETRY; POTENTIAL-DRUG CARRIERS; IN-VITRO RELEASE; POLY(AMIDOAMINE) DENDRIMERS; POLYAMIDOAMINE DENDRIMERS; BIOMEDICAL APPLICATIONS; SOLUBILITY ENHANCEMENT; SERUM-ALBUMIN; DELIVERY; ENCAPSULATION;
D O I
10.1016/j.ijpharm.2011.02.014
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The formation equilibrium of poly(amidoamine) dendrimer (PAMAM-NH2 G4) complex with an oncologic drug such as 5-fluorouracil (5-FU) in water at room temperature was examined. Using the results of the drug solubility in dendrimer solutions and the method of equilibrium dialysis, the maximal number of drug molecules in the dendrimer-drug complex and its equilibrium constant were evaluated. Solubility results show that PAMAM-NH2 G4 dendrimer can transfer tens 5-fluorouracil molecules in aqueous solution. The number of active sites in a dendrimer macromolecule being capable of combining the drug, determined by the separation method, amounts to n = 30 +/- 4. The calculated equilibrium constant of the 5-FU-active site bonding is equal to K = (400 +/- 120). (C) 2011 Elsevier B.V. All rights reserved.
引用
收藏
页码:266 / 270
页数:5
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