Abstract

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/N,N-dimethylacrylamide—and evaluated the MPCP’s usefulness for dry eye treatment using a rabbit model treated with N-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 N-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.

Highlights

  • Dry eye disease is a complex and multifactorial ocular disease, and tear film instability, visual disturbance, and discomfort are commonly observed, with potential damage to the ocular surface [1]

  • We designed the MPC polymer (MPCP) structure based on three points: (1) the methacryloyloxy ethyl phosphorylcholine (MPC), indicating the zwitterionic group, shows the hydrophilic part and gives hydrophilicity to MPCP; (2) stearyl methacrylate including the long-chain alkyl group shows its hydrophobic part and forms a hydrous polymer nano-sphere in an aqueous solution; (3) coupled with the acryl group as a highly reactive functional group, N,N-dimethylacrylamide accelerates the polymerization between MPC and stearyl methacrylate and strengthens the structure of polymer nano-sphere in an aqueous solution

  • We investigated whether the ocular surface stability in a normal rabbit was increased via the instillation of MPCP

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Summary

Introduction

Dry eye disease is a complex and multifactorial ocular disease, and tear film instability, visual disturbance, and discomfort are commonly observed, with potential damage to the ocular surface [1]. It was reported that dry eye disease has multiple causes, such as air pollution, medication, androgen deficiency, contact lens usage, and excessive computer use [2]. Inflammation and enhanced osmolarity on the ocular surface are important factors in the onset of dry eye disease [3]. It has been reported that oxidant stress and aging are other factors that contribute to dry eye disease [4]. The prevalence of dry eye disease is estimated at approximately 5–50% of the global adult population [5], and it is expected that the economic burden from the disease will increase as the population ages [6]. Current treatments for dry eye disease aim to prevent the objective signs and clinical symptoms of the disease and recover the quality of life of the patients. The main approved treatments are as follows: Mucosta®

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