首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Cobalt bis(dicarbollide) derivatives: solubilization and self-assembly suppression.
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Cobalt bis(dicarbollide) derivatives: solubilization and self-assembly suppression.

机译:双(双咔唑)钴衍生物:增溶和自组装抑制。

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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.
机译:双(二咔唑)钴衍生物是有前途的治疗剂,但由于其低溶解度和在水中的自组装性,因此其使用十分复杂。先前我们已经表明,通过使用合适的生物相容性赋形剂(药物活性化合物的载体)可以提高其溶解度。预期的增溶机理是自组装的分解和单体的复合。最近,我们的时变光散射研究结果纠正了这一假设。通过使用各种赋形剂可以轻松改善所有衍生物的不良溶解性,但是只有七(2,6-二-O-甲基)-β-环糊精显示出能够分解所有衍生物的自组装并抑制其自组装的能力。出乎意料的是,其他赋形剂参与了衍生物/赋形剂复合物或盖组合物的混合装配的形成,以使它们更易溶而不减小其尺寸。

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