Nagai Noriaki, Sakurai Shunsuke, Seiriki Ryotaro, Minami Misa, Yamaguchi Mizuki, Deguchi Saori, Harata Eiji
Faculty of Pharmacy, Kindai University, 3-4-1 Kowakae, Higashi-Osaka, Osaka 577-8502, Japan.
Life Science Products Division, NOF Corporation, Yebisu Garden Place Tower, 20-3 Ebisu 4-chome, Shibuya-ku, Tokyo 150-6019, Japan.
Pharmaceutics. 2021 Jan 27;13(2):168. doi: 10.3390/pharmaceutics13020168.
The polymer that includes 2-methacryloyloxy ethyl phosphorylcholine (MPC) is well-known as an effectively hydrating multifunction agent. In this study, we prepared an MPC polymer (MPCP) using radical polymerization with co-monomers-MPC/Stearyl Methacrylate/,-dimethylacrylamide-and evaluated the MPCP's usefulness for dry eye treatment using a rabbit model treated with -acetylcysteine. The MPCP particle size was 50-250 nm, and the form was similar to that of micelles. The MPCP viscosity (approximately 0.95 mPa·s) was 1.17-fold that of purified water, and a decrease in the transepithelial electrical resistance value (corneal damage) was not observed in the immortalized human corneal epithelial cell line HCE-T cell (HCE-T cell layer). The MPCP enhanced the water maintenance on the cornea, and the instillation of MPCP increased the lacrimal fluid volume and prolonged the tear film breakup time without an increase in total mucin contents in the lacrimal fluid of the normal rabbits. The therapeutic potential of the MPCP for dry eye was evaluated using an -acetylcysteine-treated rabbit model, and, in our investigation, we found that MPCP enhanced the volume of lacrimal fluid and promoted an improvement in the tear film breakup levels. These findings regarding the creation and characteristics of a novel MPCP will provide relevant information for designing further studies to develop a treatment for dry eyes.
包含2-甲基丙烯酰氧乙基磷酰胆碱（MPC）的聚合物是一种众所周知的高效保湿多功能剂。在本研究中，我们使用自由基聚合法，以MPC/甲基丙烯酸硬脂酯/ N，N-二甲基丙烯酰胺作为共聚单体，制备了一种MPC聚合物（MPCP），并使用经N-乙酰半胱氨酸处理的兔模型评估了MPCP在干眼症治疗中的效用。MPCP的粒径为50-250nm，形态与胶束相似。MPCP的粘度（约0.95mPa·s）是纯净水的1.17倍，在永生化人角膜上皮细胞系HCE-T细胞（HCE-T细胞层）中未观察到跨上皮电阻值降低（角膜损伤）。MPCP增强了角膜上的水分保持能力，滴注MPCP可增加正常兔泪液体积并延长泪膜破裂时间，而泪液中总粘蛋白含量并未增加。我们使用经N-乙酰半胱氨酸处理的兔模型评估了MPCP对干眼症的治疗潜力，在我们的研究中，发现MPCP增加了泪液体积并促进了泪膜破裂水平的改善。这些关于新型MPCP的制备和特性的发现将为设计进一步的研究以开发干眼症治疗方法提供相关信息。
