Fabrication and evaluation of selegiline HCl embedded transdermal film for management of Parkinson’s disease
Abstract
Purpose: Selegiline HCl (SGN) is indicated for treatment of Parkinson’s disease (PD). Its mode of action involves inhibition of MAO-B enzyme. It shows extensive hepatic first-pass metabolism and low biological half-life of 1.2 -2 hours. It results in 10 % bioavailability on oral administration. To circumvent these problems, it was envisaged to develop transdermal film of selegiline HCl for management of PD.
Method: The transdermal film were developed using ethyl-vinyl acetate (EVA) as a film former. Dibutyl phthalate (DBT) and triethyl citrate (TEC) were used as plasticizers in concentrations 10 to 20 % of polymer weight. Oleic acid and linoleic acid were used as penetration enhancers in concentrations 0.5 to 2 %. Effect of concentration of plasticizers and penetration enhancers were investigated on ex-vivo skin permeation of SGN. The films were subjected to evaluation parameters like weight variation, thickness, drug content, skin irritancy and stability studies.
Results: The transdermal film containing 20 % w/w of TEC of polymer weight has resulted in smooth flexible film. Maximum drug diffusion in ex-vivo permeation was observed. The transdermal film containing 2 % w/w of linoleic acid has shown maximum dug diffusion in ex-vivo permeation studies.
Conclusion: SGN embedded transdermal films were successfully developed using EVA as a film former. TEC and linoleic acid has shown enhanced skin diffusion of drug as compared to DBT and oleic acid. Hence it is a promising approach for transdermal delivery of SGN.
DOI
https://doi.org/10.22270/jddt.v9i2.2577Published
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