Tacrine (9-amino-l,2,3,4-tetrahydroacridine), a reversible acetylcholinesterase inhibitor, is used for treating the symptoms of mild to moderate Alzheimer's disease. On per oral administraton, however, tacrine appears to exhibit side-effects such as d...
Tacrine (9-amino-l,2,3,4-tetrahydroacridine), a reversible acetylcholinesterase inhibitor, is used for treating the symptoms of mild to moderate Alzheimer's disease. On per oral administraton, however, tacrine appears to exhibit side-effects such as dose-dependent and reversible hepatotoxicity. To overcome this disadvantage, we investigated the feasibility of developing transdermal drug delivery system for tacrine. The effects of various solvents on the permeation rate of tacrine salt across hairless mouse skin were examined using flow-through diffusion cell system. The solubility of tacrine salt in the solvents used in percutaneous absorption study was obtained using equilibrium solubility method. Among tested vehicles, octanol and propylene glycol/oleyl alcohol mixtures showed the highest permeability of tacrine salt. Theoretically, the higher the solubility, the lower the permeation rate. However, it was not possible to demonstrate any correlationship between the solubility and the percutaneous absorption rate of tacrine salt. The results indicate that some of the solvents may change the barrier property of the skin and/or carrier mechanism may be involved.