Self-polymerized polyphenol-based platform for the management of dry eye pathogenesis

Area of Science:

• Biomaterials Science
• Ophthalmology
• Nanotechnology

Background:

• Ocular surface inflammation, including dry eye disease (DED), presents management challenges due to complex causes and ocular barriers.
• Conventional eye drops offer limited, short-term relief, often requiring combination therapies to address oxidative stress and inflammation.
• Existing treatments struggle to overcome ocular barriers and provide sustained therapeutic effects.

Purpose of the Study:

• To develop a novel polyphenol-based nanoparticle formulation for enhanced ocular drug delivery.
• To investigate the therapeutic efficacy of self-assembled rosmarinic acid-hyaluronic acid-cerium nanoparticles (RHC NPs) in preclinical models of DED.
• To improve ocular retention and therapeutic outcomes through nanoparticle surface modification.

Main Methods:

• Self-polymerization of rosmarinic acid with hyaluronic acid, followed by co-assembly with cerium ions to create RHC NPs.
• Surface decoration of RHC NPs with thiol groups to create thiol-modified RHC NPs (s-RHC NPs) for enhanced ocular retention.
• Topical administration of s-RHC NPs in two distinct mouse models of DED to evaluate therapeutic effects.

Main Results:

• Topical application of s-RHC NPs demonstrated comprehensive symptom relief in DED mouse models.
• Significant suppression of ocular inflammatory responses was observed post-treatment.
• Effective repair of corneal epithelial defects and recovery of tear secretion were achieved with s-RHC NP administration.

Conclusions:

• The developed s-RHC NPs show significant potential for treating dry eye disease by addressing inflammation and promoting ocular surface repair.
• The self-polymerization strategy offers a promising approach for designing polyphenol-based nanoparticles for ophthalmic applications.
• This work may pave the way for advanced nanoparticle-based therapies for various ocular surface inflammatory conditions.