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Abstract

USE OF PRONISOME GEL IN ANTIDEPRESSANT THERAPY: DESIGN AND EVALUATION

Sarfaraz Md*, Vasantakumar D, Doddayya Hiremath, Prakash Goudannavar

ABSTRACT

Selegiline is an irreversible monoamine oxidase (MAO)-B inhibitor used at low doses for the adjunctive treatment of Parkinson's disease. Mouth ulcers and stomatitis may occur with the oral lyophilisate. Selegiline is interacted with tyramine in food. Early studies suggested that oral selegiline was effective as an antidepressant in a dose range that preserved the selectivity of MAO-B inhibition. However further open trial studies have indicated that dose of oral selegiline required for clinical antidepressant like activity in most patients are relatively high (≥30 mg/day) and nonselective producing inhibition of MOA-A. Such a loss of specificity would mean that patients taking selegiline for depression would need to observe dietary restriction applicable to nonselective MAOIs. Unlike oral MAO inhibitors, transdermal selegiline delivers antidepressant drug concentrations to the central nervous system without substantially impairing gastrointestinal MAO-A activity. At the target dose of 6 mg per 24 hours, tyramine dietary restrictions are not needed. Dermal therapeutic formulation like proniosome gel of selegiline was developed and evaluated for effective treatment of depression. The present work deals with the formulation and characterization of selegiline hydrochloride Proniosome gel with an aim to enhance drug permeation through the barriers of skin and to maintain the controlled plasma level concentration. The optimized proniosomal gel P8 containing selegilne hydrochloride showed significant anti-depressant activity at P < 0.05, Primary Dermal Irritation Index (PDII) value of 0 and drug release of 92.41% over a period of 24 hrs. The results led to conclude that proniosomes offers an effective alternative colloidal carrier approach in transdermal drug delivery.

Keywords: Selegiline hydrochloride, Spans, Tweens, antidepressant activity, in-vitro release and in-vivo studies


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