Preventative Effect of Topical Rebamipide Against Corneal Epithelium Disorders Caused by Diclofenac Sodium

J Ocul Pharmacol Ther. 2024 Sep;40(7):428-434. doi: 10.1089/jop.2024.0025.

Abstract

Purpose: This study aimed to investigate the relationship between diclofenac sodium ophthalmic solution (DFNa) and corneal epithelial cell damage and to evaluate the preventive effect of rebamipide (RBM) on it. Methods: DFNa, DFNa/preservative-free (PF), or 0.5% chlorobutanol (CB) solution was instilled into the conjunctival sac of a normal rabbit eye, and corneal resistance measurement (using a corneal resistance device [CRD]) was performed 120 min after the end of instillation. Then, fluorescent staining (FL), corneal tissue staining (hematoxylin and eosin [H&E]), and immunostaining (zona occlusion-1) were performed (RBM-untreated group). However, RBM was instilled into the eyes of another group of normal rabbits, followed by each of the solutions; 120 min after the end of instillation, all evaluations were performed for this group (RBM treatment group). Results: Using the CRD method, in the RBM-untreated group, corneal resistance (CR; %) was found to be significantly reduced in DFNa (79.9 ± 19.4%), DFNa/PF (89.1 ± 17.3%), and 0.5% CB (83.8 ± 10.6%). In addition, DFNa and 0.5% CB solutions showed positive staining in the FL staining method. In the H&E staining method, some clear voids were observed in the outermost layer of the cornea using DFNa and 0.5% CB solutions. However, corneal epithelial damage was suppressed in the RBM treatment group. ZO-1 immunostaining in DFNa and 0.5% CB solutions revealed discontinuous localization of ZO-1 at the cell periphery. Conclusions: RBM eye drops were effective in preventing corneal epithelial damage caused by DFNa eye drops, and CB was considered to be the main causative agent of this damage.

Keywords: chlorobutanol; corneal epithelial damage; diclofenac Na ophthalmic solution.

MeSH terms

  • Administration, Topical
  • Alanine* / administration & dosage
  • Alanine* / analogs & derivatives
  • Alanine* / pharmacology
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology
  • Corneal Diseases* / chemically induced
  • Corneal Diseases* / drug therapy
  • Corneal Diseases* / pathology
  • Corneal Diseases* / prevention & control
  • Diclofenac* / administration & dosage
  • Epithelium, Corneal* / drug effects
  • Epithelium, Corneal* / metabolism
  • Epithelium, Corneal* / pathology
  • Male
  • Ophthalmic Solutions* / administration & dosage
  • Quinolones* / administration & dosage
  • Quinolones* / pharmacology
  • Rabbits

Substances

  • rebamipide
  • Diclofenac
  • Quinolones
  • Ophthalmic Solutions
  • Alanine
  • Anti-Inflammatory Agents, Non-Steroidal