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Importance of Evaluating Dynamic Encapsulation Stability of Amphiphilic Assemblies in Serum
Biomacromolecules ( IF 5.5 ) Pub Date : 2017-11-14 00:00:00 , DOI: 10.1021/acs.biomac.7b01220
Bin Liu 1 , S. Thayumanavan 1
Affiliation  

In targeted drug delivery systems, it is desirable that the delivery of hydrophobic drugs to a cell or tissue is achieved with little to no side effects. To ensure that the drugs do not leak during circulation, encapsulation stability of the drug carrier in serum is critical. In this paper, we report on a modified FRET-based method to evaluate encapsulation stability of amphiphilic assemblies and cross-linked polymer assemblies in serum. Our results show that serum components can act as reservoirs for hydrophobic molecules. We also show that serum albumin is likely to be the primary determinant of this property. This work highlights the importance of assessing encapsulation stability in terms of dynamics of guest molecules, as it provides the critical distinction between hydrophobic molecules bound inside amphiphilic assemblies and the molecules that are bound to the hydrophobic pockets of serum albumin.

中文翻译:

评估两亲性组合物在血清中动态包封稳定性的重要性

在靶向药物递送系统中,期望以很少或没有副作用实现疏水性药物向细胞或组织的递送。为了确保药物在循环过程中不会泄漏,药物载体在血清中的包封稳定性至关重要。在本文中,我们报告了一种改进的基于FRET的方法,用于评估两亲组装体和交联聚合物组装体在血清中的包封稳定性。我们的结果表明,血清成分可以充当疏水分子的储存库。我们还显示,血清白蛋白可能是该特性的主要决定因素。这项工作强调了根据客体分子动力学评估包封稳定性的重要性,
更新日期:2017-11-15
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