The generation of fluorometholone nanocrystal eye drops, their metabolization to dihydrofluorometholone and penetration into rabbit eyes

Fluorometholone is a widely used anti-inflammatory ophthalmic formulation, which elicits lower ocular hypertensive response than other glucocorticoid medications. This serves to mitigate against the risk of steroid-induced glaucoma. Based on hypothesis that an improved corneal permeability can increase bioavailability drug, we sought obtain fluorometholone in suspension with small particle size. Accordingly, describe formulation nanocrystal eye drops, have mean size 201.2 ± 14.1 nm (standard deviation (s.d.)) when measured by dynamic light scattering. Scanning electron microscopy further indicates nanocrystals are predominantly rectangular shape. microcrystals, hand, 9.24 4.51 µm (s.d.), tend rod-like morphology. Powder x-ray diffraction revealed microcrystal and formulations same crystal structure, main peaks at 2θ = 10.4 15.3°. The was found be stable, long-term, stored 10 °C for up 6-months. High pressure liquid chromatography (HPLC) aqueous humor rabbit eyes 15–240 mins after vivo application drops surface molecule had been converted 20α-dihydrofluorometholone (with no evidence 20β-dihydrofluorometholone fraction), penetration 2–6 fold higher longer lasting nanocrystal, rather microcrystal, formulation. In current study show how newly generated administered as enter anterior chamber become metabolized dihydrofluorometholone.