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Duygu Acar, Irene Teresa Molina-Martínez, José Javier López-Cano, Jose M Benitez Del Castillo, Rocio Herrero-Vanrell; Artificial tear with in situ gelling properties for the treatment of dry eye disease. Invest. Ophthalmol. Vis. Sci. 2018;59(9):3302. doi: https://doi.org/.
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© ARVO (1962-2015); The Authors (2016-present)
Artificial tears are commonly employed in the treatment of dry eye disease (DED); though current formulations in the market generally have a short ocular residence time and require repeated daily administration. The purpose of this study was to design and characterize an artificial tear formulation with in situ gelling properties, with the aim of extending the ocular residence time; and evaluate its tolerance in animals. The formulation incorporated components with antioxidant and osmoprotectant properties for their potential beneficial effects in DED treatment.
An unpreserved artificial tear formulation containing the in situ gelling polymer gellan gum, hydroxypropyl methylcellulose, levocarnitine, vitamin C, trehalose, borates and electrolytes was prepared. The formulation was characterized in terms of pH, osmolarity, surface tension, and viscosity. Once prepared, the formulation was put in contact with a simulated tear fluid, and the rheological properties were evaluated. In vivo tolerance studies were performed in six male New Zealand white rabbits (one eye of each animal was used as control), with macroscopic evaluation of animal discomfort and the ocular surface according to clinical signs, and in compliance with the ARVO Statement for the Use of Animals in Ophthalmic and Visual Research.
The formulation presented approximately neutral pH (7.06 ± 0.01), an osmolarity of 275.80 ± 0.35 mOsm/L , and a surface tension of 46.97 ± 0.50 mN/m (at 33°C). The viscosity of the artificial tear measured at 33°C had a mean value of 3.64 ± 0.02 mPa.s within the shear rate interval of 200-1000 s-1. After contact with the simulated tear fluid, gel behavior (G’>G’’) with viscoelastic properties was observed (with a stress threshold of 1.64 ± 0.01 Pa for deformation). The dynamic viscosity of the gel at high shear rates (800-1000 s-1) was in the interval of 2.80-3.00 mPa.s. No discomfort or clinical signs (grade 0) were observed in rabbits throughout the in vivo tolerance studies.
The results demonstrated that the artificial tear developed in this study has suitable physicochemical properties for topical ophthalmic administration, and is well tolerated in animals. The rheological data suggest that the formulation behaves as an in situ gelling system, which could provide extended ocular residence time after topical ophthalmic administration in DED treatment.
This is an abstract that was submitted for the 2018 ARVO Annual Meeting, held in Honolulu, Hawaii, April 29 - May 3, 2018.
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