Latanoprost-loaded cyclodextrin microaggregate suspension eye drops for enhanced bioavailability and stability

Area of Science:

• Ophthalmology
• Pharmaceutics
• Drug Delivery

Background:

• Conventional eye drops exhibit low bioavailability due to physiological barriers.
• Commercial latanoprost (LAT) eye drops require refrigeration and protection from light, impacting usability and stability.

Purpose of the Study:

• To develop novel latanoprost (LAT) eye drops with improved ocular bioavailability and stability.
• To utilize cyclodextrin (γCD) microaggregates for enhanced drug delivery.

Main Methods:

• Preparation and characterization of LAT/γCD aggregate ophthalmic suspensions.
• Evaluation of physical properties (pH, viscosity, osmolality, particle size) and in vitro release.
• Assessment of in vitro corneal permeability using Human Corneal Epithelial Cells.
• In vivo studies in rabbits for precorneal retention and ocular distribution.

Main Results:

• LAT/γCD aggregates were successfully formed and confirmed.
• LAT/γCD eye drops demonstrated sustained release, improved stability, and no significant cytotoxicity.
• In vivo studies showed significantly higher precorneal retention (3.98x AUC) and aqueous humor drug levels (2.60x AUC) compared to Xalatan®.

Conclusions:

• Cyclodextrin microaggregate suspension eye drops offer a promising strategy for enhancing latanoprost (LAT) ocular bioavailability.
• This novel formulation improves both drug stability and delivery, potentially overcoming limitations of conventional eye drops.