Purpose
To test the hypothesis that mucoadhesive microdiscs formulated in a rapidly dissolving tablet can increase preocular residence time.
Methods
Microparticles, smaller than 10 μm in diameter, were fabricated by emulsification with poly(lactic-co-glycolic acid) (PLG) as a core material and, in some cases, poly(ethylene glycol) (PEG) as a mucoadhesion promoter. To examine the effect of particle geometry, microparticles were also cut to possess flat surfaces (i.e., microdiscs) and compared with spherical particles (i.e., microspheres). In vitro mucoadhesion of microparticles was tested on a mucous layer under shear stress mimicking the human blink. The resulting microparticles were also formulated in two dosage forms – an aqueous suspension and dry tablet to – test the effect of formulation on the retention capacity of microparticles on the preocular space of rabbits in vivo.
Results
Mucoadhesive microdiscs adhered better to the simulated ocular surface than the other types of microparticles. When a dry tablet embedded with mucoadhesive microdiscs was administered in the cul-de-sac of the rabbit eye in vivo, these microdiscs exhibited longer retention than the other formulations tested in this work. More than 40% and 17% of mucoadhesive microdiscs remained on the preocular surface at 10 min and 30 min after administration, respectively. Fluorescence images from the eye surface showed that mucoadhesive microdiscs remain for at least 1 h in the lower fornix.
Conclusion
This study demonstrated that mucoadhesive microdiscs formulated in a dry tablet can achieve a prolonged residence time on the preocular surface and thus are a promising drug delivery system for ophthalmic applications.