Design of transdermal matrix patch containing ondansetron

Abstract

Ondansetron was formulated into a transdermal matrix patch to reduce side effects and improve patient compliance. The effects of adhesive (polyisobutylene rubber, acrylic, and styrene butadiene rubber), crosslinker content (aluminum), vehicle (lactic acid), and drug amount on ondansetron skin permeation rate were investigated using excised hairless mouse skin with a flow-through diffusion cell system. Acrylic adhesive resulted in a higher ondansetron permeation rate than that of other adhesives. The ondansetron matrix patch prepared with acrylic adhesive without the crosslinker showed the highest permeation rate of 0.92 µg/cm2/h. Adding the crosslinker to the matrix patch reduced ondansetron skin permeation rate. The molecular weight and functional group of adhesive did not affect skin permeation of ondansetron from the matrix patch. As the amount of ondansetron in the matrix patch was increased (2.0–6.5 %), skin permeation rate increased up to 5 % of the drug, which was unchanged beyond this concentration. Based on these results, the optimum formulation for an ondansetron matrix patch consisted of 5 % ondansetron, 5 % lactic acid, 19.9 % N-methyl-2-pyrrolidone, 5 % ethyl oleate, 2 % glycerol monooleate, and 63.1 % acrylic adhesive (SK 1570-50F). This optimized matrix patch resulted in a skin permeation rate of 1.01 ± 0.21 µg/cm2/h through excised hairless mouse skin. © 2016, The Korean Society of Pharmaceutical Sciences and Technology.