Therapeutic Potential of Water-Soluble Resveratrol-Loaded Polyethylene Glycol Monostearate Micelles in a Mouse Model of Dry Eye Disease.

BACKGROUND

Dry eye disease (DED) is a multifactorial ocular surface condition that causes damage and discomfort, significantly impairing the quality of life of patients. Recently, phytochemicals such as trans-resveratrol (Res) have attracted growing interest due to their potential therapeutic effects against the DED-related pathophysiology. To enable the therapeutic application of water-insoluble Res, this study aimed to evaluate the efficacy of a previously developed water-soluble micelle formulation (stPEG/Res) containing polyethylene glycol monostearate (stPEG) in treating DED.

METHODS

The antioxidant activity of stPEG/Res was assessed using the 2,2-diphenyl-1-picrylhydrazyl radical-scavenging assay, and its cytotoxicity was evaluated in a human corneal epithelial cell line. Furthermore, an in vivo efficacy study was performed using a mouse model of DED induced by lacrimal gland excision. Tear volume, corneal histopathological changes, inflammatory responses, and apoptosis in the cornea were evaluated.

RESULTS

The stPEG/Res formulation exhibited antioxidant activity and a cytotoxicity profile against corneal epithelial cells comparable to that of free Res. Furthermore, in the mouse model of DED, stPEG/Res alleviated dry eye symptoms not by restoring tear volume, but by suppressing inflammation and apoptosis in the cornea.

CONCLUSIONS

These findings indicate that stPEG/Res has potential as a novel therapeutic option for corneal disorders associated with DED.