Effects of Sodium Naproxen Eye Drops on Rabbit Ocular Inflammation Induced by Sodium Arachidonate

Spampinato, Santi; Marino, Andreana; Bucolo, Claudio; Canossa, Marco; Bachetti, Tiziana; Mangiafico, Sebastiano

doi:10.1089/jop.1991.7.125

Cited by 23 publications

(11 citation statements)

References 15 publications

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“…A study reports the use of oxyethylated methyl esters of rape oil fatty acids (Rofams) as solubilizer in naproxen eye drops (79). Topical administration of aqueous naproxen sodium eye drops was found to provide a significant protection against sodium arachidonate-induced rise in aqueous humor PGE 2 , protein and polymorphonuclear leukocytes (80). Naproxen was also found to afford protection in rabbits against inflammatory response induced by anterior chamber paracentesis (81).…”

Section: Naproxenmentioning

confidence: 99%

Topical Ocular Delivery of NSAIDs

Ahuja

Dhake²,

Sharma

et al. 2008

AAPS J

188

148

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Abstract. In ocular tissue, arachidonic acid is metabolized by cyclooxygenase to prostaglandins which are the most important lipid derived mediators of inflammation. Presently nonsteroidal anti-inflammatory drugs (NSAIDs) which are cyclooxygenase (COX) inhibitors are being used for the treatment of inflammatory disorders. NSAIDs used in ophthalmology, topically, are salicylic-, indole acetic-, aryl acetic-, aryl propionicand enolic acid derivatives. NSAIDs are weak acids with pKa mostly between 3.5 and 4.5, and are poorly soluble in water. Aqueous ophthalmic solutions of NSAIDs have been made using sodium, potassium, tromethamine and lysine salts or complexing with cyclodextrins/solubilizer. Ocular penetration of NSAID demands an acidic ophthalmic solution where cyclodextrin could prevent precipitation of drug and minimize its ocular irritation potential. The incompatibility of NSAID with benzalkonium chloride is avoided by using polysorbate 80, cyclodextrins or tromethamine. Lysine salts and α-tocopheryl polyethylene glycol succinate disrupt corneal integrity, and their use requires caution. Thus a nonirritating ophthalmic solution of NSAID could be formulated by dissolving an appropriate water-soluble salt, in the presence of cyclodextrin or tromethamine (if needed) in mildly acidified purified water (if stability permits) with or without benzalkonium chloride and polyvinyl alcohol. Amide prodrugs met with mixed success due to incomplete intraocular hydrolysis. Suspension and ocular inserts appear irritating to the inflamed eye. Oil drop may be a suitable option for insoluble drugs and ointment may be used for sustained effect. Recent studies showed that the use of colloidal nanoparticle formulations and the potent COX 2 inhibitor bromfenac may enhance NSAID efficacy in eye preparations.

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Section: Naproxenmentioning

confidence: 99%

Topical Ocular Delivery of NSAIDs

Ahuja

Dhake²,

Sharma

et al. 2008

AAPS J

188

148

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“…As previously described [10] ocular inflammation was induced by topical administration of 0.5% (w/v) sodium arachidonate (50 Ìl), dissolved in a phosphate buffer solution (pH 7.4). Inflammation was quantified using a slit lamp (model 4179T, Sbisà, Florence, Italy), at various times according to a modified Draize scoring system [11], by two observers who were unaware of the treatments.…”

Section: Ocular Inflammationmentioning

confidence: 99%

Enhanced Ocular Anti-Inflammatory Activity of Ibuprofen Carried by an Eudragit RS100<sup>®</sup> Nanoparticle Suspension

et al. 2002

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Purpose: To investigate the ocular pharmacodynamic profile of a polymer nanoparticle system loaded with sodium ibuprofen (IBU-RS) in comparison to an aqueous solution of ibuprofen lysinate (IBL) in the rabbit eye both being applied topically. Methods: Ocular inflammation was elicited by topical application of sodium arachidonate. Inflammation was quantified according to a modified Draize test. The protein level and the number of polymorphonuclear leukocytes in the aqueous humor were assessed after 2 h from arachidonate instillation. The ibuprofen concentration in the aqueous humor was evaluated by HPLC assay. The physico-chemical properties of nanoparticles were also evaluated. Results: The IBU-RS nanosuspension formulation significantly reduced the primary signs of ocular inflammation as well as significantly reducing the protein level and the number of polymorphonuclear leukocytes in the aqueous humor compared with the IBL formulation. Furthermore, the aqueous humor drug concentration from the group treated with IBU-RS was significantly higher compared to the IBL-treated group. The IBU-RS nanosuspensions showed very interesting size and surface charge values, adequate for ophthalmic administration. Conclusions: The pharmacological profile of the topical IBU-RS nanosuspension formulation described in this study indicates that the dispersion of the drug within RS polymer nanoparticles increased its ocular bioavailability and ultimately its pharmacological activity.

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“…The anti‐inflammatory efficacy of the developed FB loaded PLGA NPs was evaluated in an ocular inflammation model previously described,18 using sodium arachidonate (SA) to induce corneal inflammation in rabbits. The activity of the NPs was compared to a FB phosphate buffer solution, commercial eye‐drops, and empty NPs with or without surfactant.…”

Section: Introductionmentioning

confidence: 99%