Department of Applied Chemistry (R&D), Contipro a.s., Dolní Dobrouč 401, 561 02 Dolní Dobrouč, Czech Republic.
Department of Tribology, Faculty of Mechanical Engineering, Brno University of Technology, Technická 2896/2, 616 69 Brno, Czech Republic.
Biomolecules. 2021 Sep 30;11(10):1431. doi: 10.3390/biom11101431.
Hyaluronan (HA) is widely used for eye drops as lubricant to counteract dry eye disease. High and low molecular weight HA are currently used in ophthalmology. However, a large portion of the current literature on friction and lubrication addresses articular (joint) cartilage. Therefore, eye drops compositions based on HA and its derivatized forms are extensively characterized providing data on the tribological and mucoadhesive properties. The physiochemical properties are investigated in buffers used commonly in eye drops formulations. The tribological investigation reveals that amphiphilic HA-C12 decreases the friction coefficient. At the same time, the combination of trehalose/HA or HAC12 enhances up to eighty-fold the mucoadhesiveness. Thus, it is predicted a prolonged residence time on the surface of the eye. The incorporation of trehalose enhances the protection of human keratinocytes (HaCaT) cells, as demonstrated in an in-vitro cell-desiccation model. The presence of trehalose increases the friction coefficient. Medium molecular weight HA shows significantly lower friction coefficient than high molecular weight HA. This research represents a first, wide array of features of diverse HA forms for eye drops contributing to increase the knowledge of these preparations. The results here presented also provide valuable information for the design of highly performing HA-formulations addressing specific needs before preclinic.
透明质酸(HA)被广泛用作眼药水的润滑剂,以对抗干眼症。高分子量和低分子量的 HA 目前在眼科中使用。然而,目前关于摩擦和润滑的大部分文献都涉及关节(关节)软骨。因此,基于 HA 及其衍生形式的眼药水成分被广泛表征,提供了关于摩擦学和粘膜粘附特性的数据。理化性质在眼药水配方中常用的缓冲液中进行研究。摩擦学研究表明,两亲性 HA-C12 降低了摩擦系数。同时,海藻糖/HA 或 HAC12 的组合将粘膜粘附性提高了八十倍。因此,可以预测在眼睛表面的停留时间延长。海藻糖的加入增强了对人角质形成细胞(HaCaT)的保护作用,如在体外细胞干燥模型中所证明的。海藻糖的存在增加了摩擦系数。中分子量 HA 的摩擦系数明显低于高分子量 HA。这项研究代表了用于眼药水的各种 HA 形式的第一个广泛特征,有助于增加对这些制剂的了解。这里呈现的结果还为高表现 HA 制剂的设计提供了有价值的信息,以满足临床前的特定需求。