Department of Chemistry, ‡Center for Bioactive Delivery, Institute for Applied Life Sciences, and §Molecular and Cellular Biology Program, University of Massachusetts , Amherst, Massachusetts 01003, United States.
Biomacromolecules. 2017 Dec 11;18(12):4163-4170. doi: 10.1021/acs.biomac.7b01220. Epub 2017 Nov 14.
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.
在靶向药物输送系统中，期望将疏水性药物递送到细胞或组织中，而几乎没有副作用。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封装稳定性至关重要。在本文中，我们报告了一种改良的基于 FRET 的方法，用于评估血清中两亲组装体和交联聚合物组装体的封装稳定性。我们的结果表明，血清成分可以作为疏水分子的储库。我们还表明，血清白蛋白很可能是这种性质的主要决定因素。这项工作强调了根据客体分子的动力学评估封装稳定性的重要性，因为它提供了疏水分子结合在两亲组装体内和结合在血清白蛋白疏水性口袋内的分子之间的关键区别。
