Novel nanostructured lipid carriers loading Apigenin for anterior segment ocular pathologies

Area of Science:

• Ophthalmology
• Nanotechnology
• Pharmacology

Background:

• Dry eye disease (DED) is a prevalent ocular condition with unsatisfactory treatment options.
• Current treatments like artificial tears do not address the root causes of DED.
• Apigenin (APG), a natural anti-inflammatory compound, has limited efficacy due to poor solubility and bioavailability.

Purpose of the Study:

• To develop and evaluate a novel nanoparticle formulation of apigenin (APG-NLC) for improved dry eye disease treatment.
• To enhance APG stability, bioavailability, and ocular retention time.
• To assess the therapeutic efficacy and safety of APG-NLC for ocular administration.

Main Methods:

• Optimization and characterization of apigenin-loaded nanostructured lipid carriers (APG-NLC).
• Evaluation of biopharmaceutical properties including particle size, surface charge, encapsulation efficiency, and drug release kinetics.
• In vitro and in vivo studies for ocular tolerance, cytotoxicity, cell internalization, and therapeutic efficacy in a DED model.

Main Results:

• Optimized APG-NLC showed particle size <200 nm, positive charge, and >99% encapsulation efficiency.
• APG-NLC demonstrated sustained APG release and stability for over 25 months.
• Formulation proved safe for ocular use, non-toxic to corneal cells, and effectively reversed DED symptoms in vivo, reducing damage and increasing tear volume.

Conclusions:

• APG-NLC represents a stable, biocompatible, and effective system for topical ocular delivery of apigenin.
• The formulation significantly improves therapeutic efficacy for dry eye disease and associated ocular inflammation.
• APG-NLC offers a promising advancement in managing DED and preventing ocular inflammatory conditions.