EFFECTS OF MIPRAGOSIDE(R) ON OCULAR ALLERGIC INFLAMMATION IN THE RABBIT

We evaluated the pharmacodynamic and pharmacokinetic profile of Miprag oside(R), a monosialoganglioside isopropyl-ester (as 0.5% w/w ophthalm ic gel), on allergic inflammation of the eye induced by reverse passiv e Arthus reaction, on a non-immune mast cell degranulation elicited by compound 48/80 and on ocular inflammation produced by horse serum. Co njunctiva was sensitized by injection of rabbit antisera to bovine pro teins and the allergic conjunctivitis was triggered by intravenous adm inistration of bovine gamma globulin. The permeability of the blood-co njunctival barrier was evaluated by a fluorometric method. Compound 48 /80 was topically administered at concentration of 50mg/ml and histolo gical analysis of conjunctiva was performed. Horse serum was administe red by intravenous injection at different days. The pharmacokinetic pr ofile of topical H-3-Mipragoside(R) on 48/80 model was investigated an d compared with untreated animals. Mipragoside(R) treatment significan tly reduced (p<0.05 vs placebo) the conjunctival vasopermeability indu ced by reverse passive Arthus reaction as well as successfully reduced the eosinophil levels in the conjunctival epithelium (p<0.01 vs place bo) elicited by compound 48/80. Further, Mipragoside(R) successfully r educed the primary signs of ocular inflammation produced by horse seru m administration. A radiotracer technique was used to evaluate the dis position of H-3-Mipragoside(R) in the rabbit ocular tissues. Dispositi on of the drug was monitored at 30, 60, 120 and 240 min. H-3-Mipragosi de(R) levels in the inflamed conjunctiva were significantly higher (p< 0.01) than in the control eye.