Permeability and Anticataract Effects of a Topical Ocular Drug Delivery System of Disulfiram

Immortalized human corneal epithelial cells (HCECs) were cultured in vitro. Cells were observed under phase-contrast microscope and the integrity of cells monolayer was determined by transepithelia electrical resistance (TEER). A permeability of diethyldithiocarbamate (DDC) through a HCECs monolayer was compared with that of DDC through an excised rabbit cornea. The permeability coefficients of DDC through a HCECs monolayer and a excised rabbit cornea were (29.5plusmn4.8)times10-6 cmmiddots-1 and (34.7plusmn5.2)times10-6 cmmiddots-1 respectively. The result demonstrates that the permeability of DDC through in vitro cornea may be predicted using HCECs monolayer. In vivo trans-corneal transit of DDC from DSF eye drops was performed. Eye drops with HPMC has 2.8-fold greater for area under the curve (AUC) than eye drops without HPMC, which was attributed to the complex formation of DSF/HPbetaCD inclusion with HPMC. The lenses opacity was monitored using a slit lamp and results show DSF eye drops can effectively prevent the cataracts development.