perfluorobutylpentane and Disease-Models--Animal

Dry eye disease (DED) is one of the most prevalent ocular surface disorders that presents clinically. Recently, the semifluorinated alkane (SFA) perfluorohexyloctane (NovaTears. Interactions of both SFAs with the corneal surface were evaluated ex vivo using high-speed photography. The in vivo influence of SFAs on tear fluid dynamics was evaluated in healthy rabbit eyes observing changes in lipid layer grade, tear evaporation rate, tear volume and tear osmolarity. Furthermore, ocular tolerability was confirmed by clinical scoring and sodium fluorescein staining.. Ex vivo studies demonstrated that both SFAs rapidly spread on the ocular surface with their contact angle on the cornea being virtually zero. A significant improvement in lipid layer grade was observed immediately after instillation of both SFAs in vivo, although the improvement was more sustained upon instillation of perfluorohexyloctane with a statistically significant difference compared to saline instillation evident from day five onwards. No significant changes in tear evaporation rate, volume or osmolarity, nor any signs of ocular irritation were observed after application of either SFA over the seven-day study period.. Both SFAs showed excellent spreading on the ocular surface. Perfluorohexyloctane improved the lipid layer grade significantly after topical application supporting its potential to stabilise the tear film lipid layer and thus provide symptomatic relief in evaporative DED.

Topics: Animals; Cornea; Disease Models, Animal; Dry Eye Syndromes; Fluorocarbons; Ophthalmic Solutions; Osmolar Concentration; Rabbits; Tears

Cyclosporine A (Cs) has been used as effective topical therapy for inflammatory dry eye disease since more than a decade. However, due to its lipophilic character, Cs is formulated as emulsions or oily solutions for topical application. This experimental study aimed to test if the use of semifluorinated alkanes (SFAs) as a preservative-free, well-tolerated non-stinging or burning vehicle maintains or even improves the benefits of Cs in the topical therapy of dry-eye disease.. Desiccating stress was applied to C57BL/6 mice for 14 consecutive days to induce experimental dry-eye. Cs dissolved in SFA (perfluorobutylpentane = F4H5with 0.5% Ethanol), F4H5 with 0.5% ethanol only, 0.05% Cs (Restasis®), and dexamethasone (Monodex®) were applied three times daily beginning either at day 4 or day 11 of desiccating stress for up to 3 weeks after end of dry-eye induction.. In comparison to other groups, Cs/F4H5 demonstrated high efficacy and earlier reduction of corneal staining. In this study, Cs/F4H5 had the ability to maintain conjunctival goblet cell density once applied on day 4. Flow cytometry analysis from cervical lymphnodes demonstrated a significantly lower CD4+ and CD8+ T-cells in the Cs/F4H5 group following 3 weeks of therapy than at baseline, but no difference in regulatory T cells from regional lymphnodes were seen.. Overall, compared to a commercially available Cs formulation (Restasis®) and dexamethasone, Cs/F4H5 was shown to be equally effective but with a significantly faster therapeutic response in reducing signs of dry-eye disease in an experimental mouse model.

Topics: Administration, Topical; Animals; Cell Count; Conjunctiva; Cyclosporine; Dexamethasone; Disease Models, Animal; Drug Carriers; Drug Therapy, Combination; Dry Eye Syndromes; Female; Flow Cytometry; Fluorocarbons; Glucocorticoids; Goblet Cells; Immunosuppressive Agents; Mice; Mice, Inbred C57BL; Ophthalmic Solutions; Treatment Outcome