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Ronald A. Wassel, Didier Nuno, Alexander Quiambao, Fadee Mondalek, Rafal Farjo; Development of Microemulsions for Enhanced Topical Delivery to the Eye. Invest. Ophthalmol. Vis. Sci. 2012;53(14):497.
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MSH-1001, a novel highly insoluble small molecule, is an ATP-sensitive K channel opener and has been shown to reduce intraocular pressure. The purpose of this study was to develop a microemulsion based eye drop that can deliver therapeutic drug concentrations to the retina better than a micronized suspension.
Twelve different nano- and micro-emulsions were prepared. There formulations were made up of oils and surfactants that are commonly used in ophthalmic formulations. Quantification of MSH-1001 in rabbit aqueous humor at 1 hour following a 60 ul eye drop of the aqueous humor performed using LC-MS/MS.
Following topical administration of the various eye drops it was observed that a 0.5% MSH-1001 microemulsion delivered the same drug levels to the aqueous humor as a 3% nanoemulsion and the 10% micronized suspension.
MSH-1001 can be formulated into optically transparent and thermodynamically stable microemulsion eye drops. These eye drops, while having two orders of magnitude lower concentrations of the active ingredient, have demonstrated the ability to deliver the same concentration to the aqueous humor as more traditional eye drop formulations. These results suggest that this eye drop formulation platform technology could be applied to increase ocular delivery of other lipophilic active pharmaceutical ingredients.
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