Design, Development and Evaluation of Selegiline Hydrochloride Transdermal Patch

Abstract

Many monoamine oxidase inhibitors (MAOIs) have been used to treat major depressive disorder (MDD). However, the prescription of MAOIs has decreased considerably as a result of side effects such as tyramine-induced hypertensive crisis, known as “Cheese Effect”. The drug delivery system itself can affect the effi cacy and bioavailability of certain drugs when medications are given by oral, intravesical and intravaginal routes. Therefore there is a need for advanced drug delivery techniques that can avoid toxic effects and improve the bioavailability at the same time. In this context, the transdermal patches of selegiline hydrochloride (SH) were prepared by the solvent casting method using hydroxy propyl methyl cellulose (HPMC), polyvinyl alcohol (PVA) and methyl cellulose (MC) as reservoir polymers in different ratios (1:1, 1:2 and 1:3). Rate controlling membrane was caste by using 2% ethyl cellulose (EC) membrane. The prepared patches possessed satisfactory physicochemical characteristics. The formulation exhibited fl exibility, uniform weight, thickness, smoothness, drug content (93 to 97 %), little moisture loss and moisture absorption. The in-vitro permeation studies in phosphate buffer (pH 7.4) revealed formulations released drug in the range of 86.77 to 96.79% and followed diffusion mechanism. Formulations with 1:1 and 1:2 ratio released drug up to 10 to 20 h only. The optimized formulation F6 containing PVA (1:3) showed good release rate of 90.08% for 24 h. The patches were seemingly free of potential hazardous skin irritation. FT-IR and DSC studies revealed no interaction between the drug and polymers used.