Abstract
Purpose :
Due to a poor solubility of cyclosporine A in water, conventional eyedrops for dry eye syndrome (DES) include surfactants that may cause burning sensation, stinging pain, blurred vision, and eye redness. To develop a patient-friendly eyedrop for DES, we prepared a surfactant-free dispersion of cyclosporine A (D-CsA) and evaluated its efficacies in a murine model.
Methods :
D-CsA was prepared as a surfactant-free dispersion in water based on our proprietary technology. DES of 12- to 16-week-old NOD.B10.H2b mice was induced by daily injections of scopolamine hydrobromide in a low humidity (30~40%) environment for 10 days. Efficacies were evaluated with three eyedrops (Vehicle, 0.05% Restasis, and 0.001% D-CsA) that were bilaterally given 5 μL/eye each twice a day, over 10 treatment days. (n=4 for each group)
Results :
When treated with D-CsA, tear production increased more than 4-fold on day 5 already (cf. 10 days required for Restasis) and reached 6.3-fold on day 10. While scores of Restasis in corneal smoothness, fluorescein staining, and epithelial cell detachment, did not or barely changed over 10 days, those of D-CsA were drastically improved by 42.6%, 50.5% and 52.4%, respectively. Their conjunctival efficacies were confirmed to be comparable in goblet cell density and mucin-stained cell density, which increased around 2.2-fold and 2.5-fold, respectively.
Conclusions :
We have demonstrated enhanced overall efficacies of D-CsA eyedrop for DES, particularly in tear production, goblet cell density, and corneal recovery. Given the fact that there is no surfactant used in the eyedrop, this demonstration exhibits the true intrinsic efficacies of CsA for DES which have been inevitably veiled in oils and surfactants. We expect that this formulation would provide a pain-free solution to chronic DES patients worldwide.
This is a 2021 ARVO Annual Meeting abstract.