Study of the interactions of PAMAM G3-NH2 and G3-OH dendrimers with 5-fluorouracil in aqueous solutions
Study of the interactions of PAMAM G3-NH2 and G3-OH dendrimers with 5-fluorouracil in aqueous solutions
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DOI：
10.1016/j.ijpharm.2016.03.061
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发表时间：
2016-05-30
影响因子：
5.8
通讯作者：
Palecz, Bartlomiej
中科院分区：
文献类型：
--
作者：
Buczkowski, Adam;Waliszewski, Dariusz;Palecz, Bartlomiej
光谱测量（溶解度增加、平衡透析、H-1 NMR滴定）和量热测量（等温滴定ITC）的结果表明，5-氟尿嘧啶在水溶液中通过阳离子PAMAM G3-NH 2树枝状聚合物和羟基PAMAM G3-OH树枝状聚合物自发（Δ G < 0）键合。PAMAM G3-NH 2树枝状聚合物键合约n = 25 +/- 8个药物分子。它们中的一些n（1）= 5 +/- 1通过平衡常数K-1 = 3890 +/- 930的末端胺基团键合，而其余的n（2）= 24 +/- 3通过平衡常数K-2 = 110 +/- 30的酰胺基团键合。羟基PAMAM G3-OH树枝状聚合物通过叔胺基团键合n =6.0 +/- 1.6分子的5-氟尿嘧啶，平衡常数K=65 +/- 10。比较了G3-NH 2和G3-OH树枝状大分子与5-氟尿嘧啶的键合参数，以及G4-NH 2、G5-NH 2和G5-OH代大分子与5-氟尿嘧啶的键合参数。(C)© 2016 Elsevier B. V.版权所有。
The results of spectroscopic measurements (increase in solubility, equilibrium dialysis,H-1 NMR titration) and calorimetric measurements (isothermal titration ITC) indicate spontaneous (Delta G < 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 n(1) = 5 +/- 1 are bonded by terminal amine groups with equilibrium constant K-1 = 3890 +/- 930, while the remaining ones n(2) = 24 +/- 3 are bonded by amide groups with equilibrium constant K-2 = 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. (C) 2016 Elsevier B.V. All rights reserved.