Development of a Transdermal Delivery System for Tacrine

Abstract

Tacrine has several mechanisms of action. The putative primary mechanism of action of tacrine for Alzheimer's disease is reversible inhibition of acetylcholinesterase (AChE), which thus slows the breakdown of the chemical messenger acetylcholine (ACh) in the brain. Tacrine also inhibits butyrylcholinesterase activity. In accumulation, tacrine blocks sodium and potassium channels. Tacrine also acts as a histamine N-methyltransferase inhibitor. This study was carried out to develop matrix based transdermal patches containing Tacrine to overcome the first pass metabolism and to reduce frequency of dosing compared to oral route. . Matrix type of transdermal patches was developed by using Methocel K4M, Methocel K15M, Methocel K100M and Xanthan gum polymers. Transdermal patches were prepared by employing solvent casting method. Drug excipients compatibility studies were carried out by using FTIR, and it was observed that there were no interactions. Formulations were prepared with the varying concentrations polymers ranging from F1-F16, and all the formulations were evaluated for various physical parameters Physical appearance, Flatness, Weight variation, Thickness, Folding endurance, Drug content, Moisture uptake, Moisture content and Swelling study and all the results were found to be within the pharmacopeial limits, invitro drug release studies by using dialysis membrane. Among all the 16 Tacrine transdermal patches formulations F5 formulations which contain Methocel K15M 100 mg had shown 97.61% % cumulative drug release within 12 hours.