Novel Nano-Liposome Formulation for Dry Eyes with Components Similar to the Preocular Tear Film

Dry eye is commonly treated with artificial tears; however, developing artificial tears similar to natural tears is difficult due to the complex nature of tears. We characterized and evaluated a novel artificial tear formulation with components similar to the lipid and aqueous constituents of natural tears. Nano-liposomes, composed in part of phosphatidylcholine, were dispersed in an aqueous solution of bioadhesive sodium hyaluronate. Liposome size, zeta potential, and physicochemical properties of the fresh and stored (4°C) liposomal formulation were analyzed. In vitro tolerance was tested using human corneal and conjunctival cell lines by exposures of 15 min to 4 h. The tolerance of the liposomal formulation was evaluated in animals (rabbits). The average liposome size was 186.3 +/- 7.0 nm, and the zeta potential was negative. The osmolarity of the formulation was 198.6 +/- 1.7 mOsm, with a surface tension of 36.5 +/- 0.4 mN/m and viscosity of 3.05 +/- 0.02 mPa·s. Viability values in the human corneal and conjunctival cell lines were always >80%, even after liposomal formulation storage for 8 weeks. Discomfort and clinical signs after instillation in rabbit eyes were absent. The new formulation, based on phosphatidylcholine-liposomes dispersed in sodium hyaluronate has suitable components and characteristics, including high in vitro cell viability and good in vivo tolerance, to serve as a tear substitute.
Ministerio de Economía y Competitividad (España)
Instituto de Salud Carlos III
Federación Española de Enfermedades Raras
Depto. de Farmacia Galénica y Tecnología Alimentaria
Depto. de Farmacología, Farmacognosia y Botánica
Fac. de Farmacia
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