External electrostatic interaction versus internal encapsulation between cationic dendrimers and negatively charged drugs: Which contributes more to solubility enhancement of the drugs?

被引：83
作者：
Laboratory of Functional Membranes, Department of Chemistry, University of Science and Technology of China, Hefei, Anhui 230026, China [1 ]
不详 [2 ]
机构：
[1] Laboratory of Functional Membranes, Department of Chemistry, University of Science and Technology of China, Hefei
[2] Hefei National Laboratory for Physical Sciences at Microscale, School of Life Sciences, University of Science and Technology of China, Hefei
来源：
J Phys Chem B | 2008年 / 30卷 / 8884-8890期
关键词：
Nuclear magnetic resonance;
D O I：
10.1021/jp801742t
中图分类号：
学科分类号：
摘要：
Relationships of electrostatic interaction and encapsulation between poly(amidoamine) (PAMAM) dendrimers and negatively charged drug molecules have been investigated by aqueous solubility and NMR (1H NMR and two-dimensional nuclear Overhauser effect spectroscopy (2D-NOESY)) studies. PAMAM dendrimers significantly increased the solubilities of phenobarbital and sulfamethoxazole, but scarcely influenced those of primidone and trimethoprim. Moreover, 1H NMR and 2D-NOESY measurements indicated that few phenobarbital or sulfamethoxazole molecules were entrapped in the cavities of low-generation dendrimers (generation 3, G3). These results suggest that external electrostatic interaction contributes more to the solubility enhancement of drugs than internal encapsulation. © 2008 American Chemical Society.
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页码：8884 / 8890
页数：6
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