Highlights
- •A novel liposome-based, in situ gelling artificial tear formulation was developed.
- •Physicochemical properties, in vitro and in vivo tolerance were evaluated.
- •The formulation showed suitable properties for topical ophthalmic administration.
- •Good in vitro and in vivo tolerance was observed.
- •The novel artificial tear may be beneficial in the treatment of dry eye disease.
Abstract
Purpose
Artificial tears are widely used in the treatment of dry eye disease, although current
formulations do not closely resemble natural tears. The purpose of this study was
the design and characterization of a novel in situ gelling artificial tear formulation, containing both lipid and aqueous components,
in order to resemble natural tears and replenish the tear film.
Methods
Liposomes, containing phosphatidylcholine, cholesterol, vitamins A and E, were prepared
by the thin-film hydration method. The aqueous phase of the formulation was comprised
of gellan gum, hydroxypropyl methylcellulose, levocarnitine, electrolytes (sodium
chloride and potassium chloride), trehalose, and borates. The artificial tear was
characterized in terms of liposome size, pH, surface tension, and viscosity. In vitro tolerance studies were performed in a human epithelial carcinoma cell line (HeLa)
and a murine macrophage cell line (J774). In vivo tolerance was assessed in rabbits.
Results
Liposomes presented a unimodal distribution with a mean size of 200.1 ± 4.4 nm. The
resulting surface tension was 53.4 ± 1.1 mN/m (at 33 °C) and the pH was 7.6 ± 0.1.
The viscosity of the formulation presented a mean value of 4.0 ± 0.1 mPa s within
the shear rate interval of 200–1000 s−1 at 33 °C. Cell viability remained higher than 90% in both cell lines. No discomfort
or clinical signs were observed in rabbits.
Conclusions
The liposome-based and in situ gelling artificial tear formulation presented good tolerance and suitable properties
for topical ophthalmic administration. It may be beneficial in the treatment of dry
eye disease.
Keywords
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Article info
Publication history
Published online: December 06, 2017
Accepted:
November 28,
2017
Received in revised form:
November 22,
2017
Received:
July 5,
2017
Identification
Copyright
© 2017 British Contact Lens Association. Published by Elsevier Ltd. All rights reserved.