Tranylcypromine (logP = 1.34, MW = 133.19 g/mol) is a
monoamine oxidase inhibitor used in treating
major depressive disorder and is available only as oral
tablets. Transdermal delivery of
tranylcypromine minimizes hepatic and gastrointestinal side effects associated with oral dosing and prevents systemic side effects improving patient compliance. A two-day
suspension-based transdermal delivery method was developed in this study, and the delivery of
tranylcypromine across dermatomed porcine ear skin was evaluated. Different penetration enhancers were screened, namely,
isopropyl myristate,
oleyl alcohol,
oleic acid, and a combination of
oleic acid and
oleyl alcohol.
Isopropyl myristate was chosen as the penetration enhancer, and
suspension-based transdermal patches were formulated with
acrylate and
polyisobutylene pressure-sensitive adhesives by the
solvent evaporation method. The release liner and backing membrane were chosen, and the drying time for each patch was optimized. The optimized patches were characterized for their adhesive properties, drying time, peel test, shear strength, and uniformity in drug content. In vitro permeation studies were performed on dermatomed porcine ear skin using vertical static Franz diffusion cells, and the receptor samples were collected at predetermined time points for 48 h. The samples were analyzed in a validated UPLC method.
Acrylate-based
suspension patch delivered a significantly higher amount of drug (712 ± 21.46 μg/cm2) as compared to passive delivery from drug dissolved in
propylene glycol (461.49 ± 75.55 μg/cm2), reaching the two-day therapeutic target. However, the PIB-based
suspension patch delivered 559.25 ± 12.37 μg/cm2 of
tranylcypromine across the skin but did not reach the required target.