Abstract
Purpose :
To develop a new antiglaucoma ophthalmic solution containing agmatine in the pre-commercialization stage.
Methods :
A new antiglaucoma ophthalmic solution containing 1.0 mM agmatine sulfate has been developed in the pre-commercialization stage. Three candidate eye drops were formulated and their stability was checked for 6 months at both room temperature as well as in the refrigerator. Their ocular safety was carefully evaluated on the cornea of Sprague Dawley rats for 4 weeks. For the most promising agmatine candidate, its ocular hypotensive and neuroprotective effects were assessed for 3 weeks. In addition, its antiglaucoma effects were compared to a currently used antiglaucoma agent of brimonidine which is supposed to have most similar action mechanisms with agmatine among all commercialized antiglaucoma eye drops.
Results :
Among 7 available sources of raw agmatine sulfate, the highest one with a purity of 99.92% as determined by high-performance liquid chromatography (HPLC) was selected. All three agmatine formulations were completely stable for at least 6 months and did not cause any apparent ophthalmic complications for 4 weeks. In the chronic ocular hypertensive Sprague Dawley rat models established by episcleral vein cauterization, the candidate agmatine eye drops decreased the intraocular pressures by 19.86% (from 36.50±2.38 mmHg to 29.25±2.06 mmHg) and preserved the intensity of retinal ganglion cell axon as assessed by immunofluorescence for alpha-tubulin.
Conclusions :
A new antiglaucoma ophthalmic solution containing 1.0 mM agmatine sulfate has been successfully developed in the pre-commercialization stage. These promising eye drops have excellent ocular hypotensive and neuroprotective effects.
This is an abstract that was submitted for the 2018 ARVO Annual Meeting, held in Honolulu, Hawaii, April 29 - May 3, 2018.