title: Pharmacological evaluation of anti-inflammatory pyrrole-acetic acid derivative eye drops.
abstract: The effects of mucoadhesive eye drops containing a pyrrole-acetic acid derivative (tolmetin) at 0.5% concentration on ocular inflammation produced by sodium arachidonate in the rabbit's eye were evaluated. Furthermore, the bioavailability of the mucoadhesive formulation in the aqueous humor against an aqueous-based solution was compared. Tolmetin eye drops significantly reduced the signs of ocular inflammation elicited by sodium arachidonate on conjunctiva and iris. Tolmetin treatment significantly reduced the levels of prostaglandin E2, polymorphonuclear leukocytes and protein concentration in aqueous samples obtained from the eyes treated with arachidonate. The de novo production of prostaglandin E2 by corneas obtained from rabbits sacrificed 2 hours after arachidonate instillation were significantly higher in samples taken from controls than in corneas obtained from the eyes treated with tolmetin eye drops. Furthermore, the drug treatment significantly reduced the rise in intraocular pressure arachidonate-induced. The mucoadhesive formulation showed a higher bioavailability in aqueous humor compared to the aqueous-based solution both in the uninflamed and in the inflamed rabbit eyes.
authors.affiliation: Institute of Pharmacology, University of Catania, Italy.
authors.forename: C
authors.initials: C
authors.lastname: Bucolo
authors.forename: A
authors.initials: A
authors.lastname: Spadaro
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*; D001082:Aqueous Humor / Q000378:metabolism; D016718:Arachidonic Acid; D001682:Biological Availability; D003231:Conjunctivitis / Q000139:chemically induced / Q000188:drug therapy*; D016861:Cyclooxygenase Inhibitors / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*; D015232:Dinoprostone / Q000378:metabolism; D005136:Eye Proteins / Q000378:metabolism; D005260:Female; D007429:Intraocular Pressure / Q000187:drug effects; D007500:Iritis / Q000139:chemically induced / Q000188:drug therapy*; D009504:Neutrophils / Q000378:metabolism; D009883:Ophthalmic Solutions; D011817:Rabbits; D014046:Tolmetin / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D016861:Cyclooxygenase Inhibitors; D005136:Eye Proteins; D009883:Ophthalmic Solutions; D016718:Arachidonic Acid; D014046:Tolmetin; D015232:Dinoprostone