The cytotoxic effects of latanoprost, travoprost, and bimatoprost were dependent on the BAC concentration in their formulations. BACmix was cytotoxic at the concentrations above those corresponding to 0.001% BAC in ophthalmic medications. PF tafluprost was the least toxic of the drugs tested. Within studied BAC homologs, those with longer alkyl chain and higher lipophility penetrated effectively into rabbit external ocular tissues.
Background: Some studies have shown that benzalkonium chloride (BAK), a preservative used in antiglaucoma medications, can increase corneal permeability by acting as a penetration enhancer. Tafluprost is a new prostaglandin F2α analog in clinical use for the treatment of ocular hypertension and glaucoma. Methods: This study evaluated the corneal penetration of preservative-free tafluprost 0.0015% eye drops and tafluprost 0.0015% eye drops preserved with 0.01% BAK into the aqueous humor of rabbits. Results: After the administration of a single topical dose (30 μl), the maximum concentrations at 45 min of tafluprost acid in aqueous humor were 4.50 ng/ml for preservative-free tafluprost and 3.99 ng/ml for preserved tafluprost. The area under the concentration-time curves from 45 min to 3 h was 5.14 ng h/ml for the preservative-free formulation and 4.54 ng h/ml for the preserved formulation. Conclusions: These data indicate that BAK does not affect the corneal penetration of tafluprost into the rabbit aqueous humor.
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