Comparison of two ophthalmic solutions of olopatadine hydrochloride (0.1%) and epinastine hydrochloride (0.05%) on clinical signs of vernal keratoconjunctivitis and side effects of the two drugs

Background: Vernal keratoconjunctivitis (VKC) is a recurrent, bilateral, external, ocular inflammation primarily affecting young adults living in warm dry climates. The objectives of the research was to compare the two ophthalmic solutions of olopatadine hydrochloride (0.1%) and epinastine hydrochloride (0.05%) on clinical signs of vernal keratoconjuntivitis and to determine side effects of both the drugs.Methods: The study was carried out in 40 patients who attended the out-patient department (OPD) Ophthalmology, Darbhanga Medical College and Hospital, Laheriasarai from July 2007 to December 2008.  Forty patients with symptoms of VKC (ocular itching, ropy discharge, papillary hypertrophy, gelatinous thickening and horner-trantas spots were selected and included in our study.Results: Mean score of palpebral hyperemia at 0, 14, 28 and 42 days in olopatadine treated eye were 2.1, 1.4, 0.8 and 0.4 respectively having p value <0.01, and <0.01 and <0.05 respectively, while mean score at same stages in placebo eye were 2.1, 2, 1.9, and 1.5 having value >0.05. Epinastine treated group mean score of palpebral hyperemia were <0.01 and <0.01 respectively in epinastine treated eye whereas in placebo treated eye, mean score were 2.1, 2.0, 1.8 and 1.6 respectively having p value >0.05 in all stages. Statistically insignificant reduction at day 14 while very significant reduction at day 28 and 42 was observed in epinastine treated eye as compared to placebo.Conclusions: The present study had shown that both olopatadine and epinastine were effective in treating clinical signs of VKC as compared to placebo.

Development and in vitro/in vivo evaluation of thermo-sensitive in situ gelling systems for ocular allergy

Ocular allergy is one of the most common disorders of the eye surface. Following diagnosis this condition is typically treated with preparations containing antihistamines. However, anatomy of the eye and its natural protective mechanisms create challenges for ocular drug delivery. Rapid elimination of antihistamine substances due to short residency times following application can lead to insufficient treatment of ocular allergies. With this in mind, the aim of this study was to prepare a controlled ocular delivery system to extend the retention time of olopatadine hydrochloride (OLO) and in doing so to reduce the need for frequent application. We developed extended-release ocular in situ gelling systems for which in vivo retention times were determined in sheep following in vitro characterization and cytotoxicity studies. In vivo results were then compared to commercially available Patanol eye drops. the transparent gels formulated using appropriate amounts of polymers and having longer ocular retention times appear to be a viable alternative to commercially available eye drops.

Olopatadine ophthalmic solution suppresses substance P release in the conjunctivitis models

BACKGROUND: Olopatadine hydrochloride ophthalmic solutions are treated for allergic conjunctival diseases that are a selective histamine H1 receptor antagonist and an inhibitor of the release of mediators including histamine from the human mast cells. Substance P (SP) levels are increased in tears of patients with allergic conjunctivitis. However, little is known about the regulation of SP release by anti-allergic ophthalmic solutions. OBJECTIVE: We investigated that the effect of olopatadine hydrochloride ophthalmic solutions (olopatadine 0.1% and olopatadine 0.2%) on rat conjunctivitis models compared with other anti-allergic ophthalmic solutions. METHODS: Conjunctivitis was induced by subconjunctival injection of histamine or intravenous injection of ovalbumin in rats passively sensitized with anti-ovalbumin anti-serum. The releases of SP were determined in the conjunctiva and tears using rat antigen-induced conjunctivitis models. RESULTS: Olopatadine 0.1% and 0.2% significantly inhibited the increased conjunctival dye leaked in the histamine- or antigen-induced hyperpermeability. The inhibitory effects by olopatadine were more potent than by other tested anti-allergic ophthalmic solutions. Moreover, olopatadine significantly inhibited the release of SP from the conjunctiva. CONCLUSION: These results indicate that olopatadine ophthalmic solutions appear to exert additional SP release inhibition besides dual-action such as selective histamine H1 receptor antagonistic action and mast cell stabilization action.