Ophthalmic Nanoemulsion Fingolimod Formulation for Topical Application

Area of Science:

• Ophthalmology
• Nanotechnology
• Pharmaceutics

Background:

• Fingolimod (FTY720; FT), a sphingosine analog, shows promise for treating ocular conditions.
• Efficient delivery of FT to the posterior eye segment is challenging with conventional methods.

Purpose of the Study:

• To develop a novel FT-loaded nanoemulsion (FT-NE) for sustained topical ocular delivery.
• To evaluate the physicochemical properties, stability, and ocular bioavailability of the FT-NE formulation.

Main Methods:

• FT-NE formulations were prepared using homogenization and probe sonication.
• Evaluated physicochemical characteristics, in vitro release kinetics, and stability for 180 days.
• Assessed ocular bioavailability in Sprague-Dawley rats after topical application.

Main Results:

• The FT-NE formulation exhibited desirable physicochemical properties, including a spherical shape and nanometric size distribution.
• The formulation demonstrated stability for 180 days under refrigerated conditions and prolonged in vitro FT release over 24 hours.
• In vivo studies confirmed effective FT concentrations in the vitreous humor and retina following topical FT-NE application.

Conclusions:

• The developed FT-NE formulation is a promising platform for efficient topical ocular delivery of fingolimod.
• This nanoemulsion system facilitates sustained drug release and enhanced bioavailability in the posterior eye segment.