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

    Year: 2018

    Journal: Polymers, Volume 10, APR

    Authors: Vicario-de-la-Torre, Marta; Caballo-Gonzalez, Maria; Vico, Eva; Morales-Fernandez, Laura; Arriola-Villalobos, Pedro; de las Heras, Beatriz; Manuel Benitez-del-Castillo, Jose; Guzman, Manuel; Millar, Thomas; Herrero-Vanrell, Rocio; Molina-Martinez, Irene T.

    Organizations: Research Group UCM [920415]; Sanitary Research Institute of the San Carlos Clinical Hospital (IdISSC) [FEDER-CICYT FIS-PI17/00079, PI17/00466]; MINECO/AEI/FEDER, UE [MAT2013-43217R, MAT2017-83858-C2]; ISCII-FEDER RETICS (OFTARED) [RD16/0008]

    Keywords: artificial tears; preocular tear film; tear break-up time; liposomes; mucoadhesive polymers

    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 degrees 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.
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