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Cobalt bis(dicarbollide) derivatives: Solubilization and self-assembly suppression

  作者 Rak, J; Jakubek, M; Kaplanek, R; Matejicek, P; Kral, V  
  选自 期刊  European Journal of Medicinal Chemistry;  卷期  2011年46-4;  页码  1140-1146  
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[摘要]Cobalt bis(dicarbollide) derivatives are promising therapeutic agents however their utilization is complicated due to their low solubility and self-assembling in water. Earlier we have shown that their solubility can be increased by using of suitable biocompatible excipients - carriers of pharmaceutically active compounds. Expected mechanism of solubilization was disassembling of self-assemblies and complexation of unimers. Newly our results of time-dependent light scattering study correct this presumption. Poor solubility of all derivatives can be easily improved by using various excipients, however only heptakis(2,6-di-O-methyl)-beta-cyclodextrin displays ability to disassemble self-assemblies of all derivatives and suppress their self-assembling. Surprisingly, the other excipients participate on formation of mixed assemblies of derivative/excipient complex or cover assemblies to make them more soluble without decreasing their size. (C) 2011 Elsevier Masson SAS. All rights reserved.

 
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