Department of Mathematics, University of Bergen, Bergen, Norway.
Biophys J. 2013 Sep 3;105(5):1276-84. doi: 10.1016/j.bpj.2013.07.040.
The presence of collagen and charged macromolecules like glycosaminoglycans (GAGs) in the interstitial space limits the space available for plasma proteins and other macromolecules. This phenomenon, known as interstitial exclusion, is of importance for interstitial fluid volume regulation. Physical/mathematical models are presented for calculating the exclusion of electrically charged and neutral macromolecules that equilibrate in the interstitium under various degrees of hydration. Here, a central hypothesis is that the swelling of highly electrically charged GAGs with increased hydration shields parts of the neutral collagen of the interstitial matrix from interacting with electrically charged macromolecules, such that exclusion of charged macromolecules exhibits change due to steric and charge effects. GAGs are also thought to allow relatively small neutral, but also charged macromolecules neutralized by a very high ionic strength, diffuse into the interior of GAGs, whereas larger macromolecules may not. Thus, in the model, relatively small electrically charged macromolecules, such as human serum albumin, and larger neutral macromolecules such as IgG, will have quite similar total volume exclusion properties in the interstitium. Our results are in agreement with ex vivo and in vivo experiments, and suggest that the charge of GAGs or macromolecular drugs may be targeted to increase the tissue uptake of macromolecular therapeutic agents.
间质空间中存在胶原和带电荷的大分子(如糖胺聚糖[GAG]),这限制了可用于血浆蛋白和其他大分子的空间。这种现象称为间质排斥,对于间质液体积的调节很重要。本文提出了物理/数学模型,用于计算在不同水合程度下在间质中达到平衡的带电荷和中性大分子的排斥,其主要假设是,高度带电荷的 GAG 在增加水合时的膨胀会使间质基质中的部分中性胶原与带电荷大分子相互作用,从而使带电荷大分子的排斥因空间位阻和电荷效应而发生变化。人们还认为 GAG 允许相对较小的中性大分子,也允许被非常高的离子强度中和的带电荷大分子,扩散到 GAG 的内部,而较大的大分子可能无法扩散。因此,在该模型中,相对较小的带电荷大分子(如人血清白蛋白)和较大的中性大分子(如 IgG)在间质中的总体积排斥特性非常相似。我们的结果与离体和体内实验一致,并表明 GAG 或大分子药物的电荷可以被靶向以增加大分子治疗剂在组织中的摄取。