Design and Evaluation of Voriconazole Eye Drops for the Treatment of Fungal Keratitis

Table 2

Effect of preservatives on the transcorneal permeation of voriconazole from ophthalmic solutions through freshly excised goat cornea.

Preservatives	Amount of drug permeated in 120 min (mg)	% in vitro permeation	𝑃app   × 10^−6 (cm/s)	Corneal hydration (%)
Control	0.047±0.001	0.314±0.003	1.73±0.017	79.23±0.30
Benzyl alcohol	0.046±0.001	0.308±0.002	1.70±0.013	79.35±0.24
PMA	0.052±0.001^†	0.349±0.003^†	1.93±0.071^†	78.33±0.61
PMN	0.054±0.001^††	0.358±0.003^††	1.98±0.071^††	79.07±1.76
Thiomersal	0.058±0.001^†††	0.384±0.007^†††	2.12±0.021^†††	79.96±0.57
BAK	0.056±0.002^††	0.373±0.012^†††	2.06±0.067^†††	79.53±0.03
EDTA	0.060±0.001^†††	0.400±0.005^†††	2.21±0.025^†††	79.37±0.26
BAK + EDTA	0.317±0.001^††	2.120±0.003^††	30.72±0.055^†††	77.88±0.15

Values are mean ± SE of 3 corneas in each group.
^†Statistically significant difference at 𝑃<0.05; ^††statistically significant difference at 𝑃<0.01; ^†††statistically significant difference at 𝑃<0.001 from control (voriconazole 1.5%, pH 7.0 HP-β-CD based solution) as determined by one-way ANOVA followed by Dunnett’s test.