Department of General Biophysics, University of Lodz, 141/143 Pomorska St., 90-236 Lodz, Poland.
J Fluoresc. 2013 Mar;23(2):349-56. doi: 10.1007/s10895-012-1153-y. Epub 2013 Jan 11.
The aim of this study was to investigate the interactions between poly(propylene imine) (PPI) dendrimers and 2'-/3'-O-(N'-methylanthraniloyl)-ATP (Mant-ATP). Mant-ATP was used as a model molecule. Purine and pyrimidine nucleoside analogues are antimetabolites commonly used in therapy for cancer. Drug molecules can complex with dendrimers in two ways: therapeutic agents may be attached in dendrimer interior or bind to functional groups on the surface. Drugs attached to nanoparticles are characterized by improved solubility, pharmacokinetics and stability. Here, we have used poly(propylene imine) dendrimers of the 4th and 5th generations (PPI G4 and PPI G5) with primary amino surface groups partially modified with maltose (PPI-m) or without modification (PPI). We assessed the efficiency of complex formation in relation to dendrimer generation, pH of solution and the type of dendrimer used. A double fluorimetric titration method was used to estimate the binding constant (K b ) and the number of binding centers per molecule of the binding agent (n).
本研究旨在研究聚(丙烯亚胺)(PPI)树枝状大分子与 2'-/3'-O-(N'-甲基邻氨基苯甲酰基)-ATP(Mant-ATP)之间的相互作用。Mant-ATP 被用作模型分子。嘌呤和嘧啶核苷类似物是癌症治疗中常用的抗代谢物。药物分子可以通过两种方式与树枝状大分子结合:治疗剂可以附着在树枝状大分子内部或结合到表面的官能团上。与纳米颗粒结合的药物具有提高的溶解度、药代动力学和稳定性。在这里,我们使用了第四代和第五代聚(丙烯亚胺)树枝状大分子(PPI G4 和 PPI G5),其具有部分用麦芽糖(PPI-m)修饰的伯氨基表面基团或未修饰的(PPI)。我们评估了与树枝状大分子代、溶液 pH 值和所用树枝状大分子类型相关的复合物形成效率。双荧光滴定法用于估计结合剂的结合常数(K b )和每个结合剂分子的结合中心数(n)。