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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