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H. Liang, F. Brignole-Baudouin, M. Faure, G. Lambert, C. Baudouin; In vivo Studies of Toxic Profiles of Antiglaucomatous Prostaglandin Analogues in Cationic Emulsion Formulation. Invest. Ophthalmol. Vis. Sci. 2009;50(13):4781.
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© ARVO (1962-2015); The Authors (2016-present)
Using an established rabbit toxicological model, this study compared in vivo the ocular toxicity of five topical intraocular pressure (IOP)-lowering agents: the commercial benzalkonium chloride (BAC)-containing solutions of 0.005% latanoprost, 0.004% travoprost, 0.03% bimatoprost (containing respectively 0.02%, 0.015%, 0.005% BAC), BAC-free 0.004% travoprost Z, and 0.005% latanoprost in a new cationic emulsion (LCEm) formulation.
Thirty adult male New Zealand albino rabbits were used in this study. They were randomly divided into five groups: 50 µl of each formulation were applied onto rabbit eyes 15 times at 5-min intervals. The ocular surface changes were investigated using slit-lamp examination, corneal in vivo confocal microscopy (IVCM), flow cytometry (FCM), and conjunctival impression cytology (IC).
Antiglaucoma eye drops induced an ocular surface toxicity primarily related to the concentration of their common preservative BAC (latanoprost>travoprost>bimatoprost). LCEm did not induce obvious toxicity to rabbit ocular surface, just as BAC-free travoprost, by showing almost normal aspect of conjunctiva/cornea by clinical observation, CALT-IVCM analysis and IC evaluation.
These in vivo and ex vivo experimental toxicological studies confirmed the ocular surface toxicity of antiglaucomatous BAC-containing eye drop solutions. BAC-free cationic emulsion of latanoprost (LCEm) and travoprost Z were well tolerated and did not induce ocular surface damages. The IOP-lowering eye drop LCEmwill most likely have fewer ocular surface adverse effects than formulations containing preservative BAC.
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