Membrane determinants for the passive translocation of analytes through droplet interface bilayers.,Soft Matter

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Membrane determinants for the passive translocation of analytes through droplet interface bilayers.
Soft Matter ( IF 2.9 ) Pub Date : 2020-06-16 , DOI: 10.1039/d0sm00667j
Vincent Faugeras ₁ , Olivier Duclos , Didier Bazile , Abdou Rachid Thiam

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Understanding how small molecules cross cell membranes is crucial to pharmaceutics. Several methods have been developed to evaluate such a process, but they need improvement since many false-positive candidates are often selected. Robust tools enabling rapid and reproducible screening can increase confidence on hits, and artificial membranes based on droplet interface bilayers (DIBs) offer this possibility. DIBs consist in the adhesion of two phospholipid-covered water-in-oil droplets which reproduce a bilayer. By having donor and acceptor droplets, the permeability of an analyte can be studied. However, the relevance of this system relies on the comprehension of how well the physical chemistry of the produced bilayer recapitulates the behavior of cell membranes. This information is missing, and we address it here. Taking small fluorophores as model analytes, we studied their permeation through DIBs made of a wide range of phospholipids. We found that both the phospholipid acyl chain and polar head affect permeability. Overall, these parameters impact the phospholipid shape and thereupon the membrane lateral pressure, which is a major factor modulating with permeability in our system. These results depend on the nature of the chosen oil. We thereupon identified relevant physical chemistry conditions that best mimic the compactness and subsequent permeability of biological membranes.

中文翻译：

通过液滴界面双层被动转移分析物的膜决定因素。

了解小分子如何穿过细胞膜对药物至关重要。已经开发了几种方法来评估这种过程，但是由于经常选择许多假阳性候选者，因此需要改进。强大的工具可实现快速，可重复的筛选，从而增加了对样品的信心，基于液滴界面双层（DIB）的人造膜提供了这种可能性。DIBs包含两个磷脂覆盖的油包水液滴的粘附，这些液滴重现了双层。通过具有供体和受体液滴，可以研究分析物的渗透性。然而，该系统的相关性取决于对所产生的双层的物理化学如何很好地概括细胞膜行为的理解。该信息丢失，我们在这里解决。以小型荧光团为模型分析物，我们研究了它们通过多种磷脂制成的DIB的渗透性。我们发现磷脂酰基链和极性头都影响渗透性。总体而言，这些参数会影响磷脂的形状，进而影响膜的侧向压力，这是在我们系统中渗透率调节的主要因素。这些结果取决于所选油的性质。因此，我们确定了相关的物理化学条件，可以最好地模拟生物膜的紧实度和随后的渗透性。这是我们系统中渗透率调节的主要因素。这些结果取决于所选油的性质。因此，我们确定了相关的物理化学条件，可以最好地模拟生物膜的紧实度和随后的渗透性。这是我们系统中渗透率调节的主要因素。这些结果取决于所选油的性质。因此，我们确定了相关的物理化学条件，可以最好地模拟生物膜的紧实度和随后的渗透性。

更新日期：2020-07-01

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