The preclinical study of a new nasal spray with the anti-inflammatory properties: the effect on the leukotriene-induced inflammation




acute respiratory infections, acute rhinosinusitis, Enisamium Iodide (nasal spray), Ibuprofen, leukotriene-induced inflammation, anti-inflammatory activity


The use of medicines of the local action with complex effects on the pathogenic cascade of acute rhinosinusitis (ARS) is expedient. Farmak Joint-Stock Company (Ukraine) has developed a new original dosage form of a nasal spray, which contains an aqueous solution of the known pharmaceutical substance Enisamium Iodide (EI). The presence of the effect on the leukotriene link inflammation in EI can determine the high rate of the antiexudative action development in the topical (intranasal) application. This may be useful for pathogenetic therapy of ARS on the background of acute respiratory viral infections taking into account the potential effectiveness for nasal congestion relief.

Aim. To substantiate experimentally the expediency of application of a new nasal spray with EI under conditions of leukotriene-induced exudative inflammation.

Materials and methods. A new nasal spray EI (JSC Farmak (Ukraine)) – “Amizon” – with the active substance concentration of 10 mg/ml was chosen as the study object. Ibuprofen – “Nurofen” (Reckitt Benckiser Helchere International Limited (UK)), film-coated tablets, 200 mg – was used as the reference drug and was administered once daily in the dose of 48 mg/kg intragastrically. The study of anti-inflammatory properties of EI (nasal spray, 10 mg/ml) in the external (epicutaneous) application was performed on white nonlinear rats of both genders in the experimental zymosan-induced inflammation development. The anti-inflammatory activity (AIA) of EI (nasal spray, 10 mg/ml) compared to Ibuprofen was assessed in percentage in dynamics in 0.5, 1 and 2 hours of observation.

Results. According to the results of the studies conducted EI in the dosage form of a nasal spray in the active substance concentration of 10 mg/ml on the model of zymosan-induced inflammation of the rat foot showed the anti-inflammatory properties. According to the degree of its anti-inflammatory properties EI was not inferior to the reference drug Ibuprofen, but even exceeded its activity as of the 30th minute of observation after zymosan injection. The result obtained allows suggesting the presence of high rate of the antiexudative action in the experimental object in the topical (intranasal) application in the treatment of patients with ARS due to the ability to inhibit the lipoxygenase route of the arachidonic acid metabolism.

Conclusions. The presence of the anti-inflammatory activity of Enisamium Iodide (nasal spray) has been proven under conditions of leukotriene-induced inflammation reproduction on the model of the zymosan edema. By expression of the anti-inflammatory action during all periods of observation EI is not inferior to the reference drug Ibuprofen, exceeding the activity of the classical NSAID by 1.5 times as of the 30th minute after the pathology onset. The anti-inflammatory activity of Enisamium Iodide in the dosage form of nasal spray experimentally substantiates the expediency and perspectivity of its further preclinical studies.

Author Biography

T. S. Zhulai, National University of Pharmacy

teaching assistant of the Department of Clinical Pharmacology and Clinical Pharmacy


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Pre-clinical studies of new drugs