Permeability and anticataract effects of a topical ocular drug delivery system of disulfiram

In vitro trans-corneal transit studies of disulfiram/hydroxypropyl-ß-cyclodextrin (DSF/HPßCD) eye drops were performed to evaluate the effects of drug doses, buffers (PBS and BBS), thickening agents (HPMC, PVP, PVA and NaHA) and enhancers (F68, Brij 35 and DC) on the trans- corneal permeability. The area under the aqueous humor concentration versus time curve (AUC) of eye drops was significantly increased due to the addition of HPMC as a thickening agent and F68 as a penetration enhancer. The slit images and opacity of lenses illustrated the degree of cataract development in treated rats. Biochemical indicators (including the contents of soluble protein, insoluble protein, NP-SH, P-SH insoluble, protein disulfide bonds, MDA and calcium) in lenses of DSF treated animals approached that of normal lenses, but exhibited significant differences compared with model controls. The results showed that DSF optimized eye drops can effectively prevent cataract development.