Formulation and evaluation of 4-benzylpiperidine drug-in-adhesive matrix type transdermal patch

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Graphical abstractThe objective of our study was to develop a transdermal patch of 4-benzylpiperidine and to evaluate its in vitro transdermal permeation profile. Appropriate pressure sensitive adhesives and additives were selected based on solubility and slide crystallization studies. Release liners and backing membranes were selected based on their ability to peel without leaving a residue and their affinity to formulation respectively. Drug-in-adhesive patches developed were investigate for their in vitro drug permeation over 48 h across dermatomed human skin using Franz diffusion cells. Silicone based pressure sensitive adhesive along with colloidal silicon dioxide as viscosity builder, fluoropolymer coated membranes as the release liner and polyester based membranes as backing were chosen to develop a drug in silicone adhesive patch. Polyisobutylene adhesive based patch was developed with drug in polyisobutylene adhesive, along with oleic acid and oleyl alcohol as permeation enhancers, polyester for the release liner and polyethylene as backing. Among the patches developed, polyisobutylene adhesive based patch with higher drug concentration exhibited superior transdermal permeation (1608.5 ± 53.4 μg/cm2 over 48 h). The final patch was further tested for uniformity in coat weight, shear strength, tack and peel adhesion.

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