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Altered skin permeation of a highly lipophilic molecule: tetrahydrocannabinol

1988; Elsevier BV; Volume: 43; Issue: 1-2 Linguagem: Inglês

10.1016/0378-5173(88)90053-1

1873-3476

Elka Touítou, Boris Fabin,

Cannabis and Cannabinoid Research

The effect of decylmethylsulfoxide (decylMSO) and oleic acid on the skin permeation of the highly lipophilic compound, tetrahydrocannabinol (THC), was investigated. The solvents were propylene glycol (PG)-ethanol (EtOH) and PG-EtOH-H2O mixtures. For comparison, similar compositions containing the hydrophilic drug 5-fluorouracyl (5FU) were also tested. Twenty-four-hour experiments were performed with diluted solutions of the drugs in Valia-Chien diffusion cells through hairless mouse skin. The results were treated using the Transderm computer program. The results show that the permeability coefficient of THC was: (1) increased by an order of magnitude by water; (2) increased 6 times by 3% oleic acid in PG-EtOH solutions; (3) increased fourteen times by 3% oleic acid in PG-EtOH-H2O solutions; (4) not affected by decylMSO in PG-EtOH solutions; and (5) decreased 25% by decylMSO in PG-ETOH-H2O solutions. A different behavior was observed when similar systems containing the hydrophilic 5FU were tested. The permeability coefficient of 5FU was: (1) not affected by presence of water; (2) not affected by oleic acid; (3) not affected by decylMSO in PG-EtOH; and (4) increased 14 times by decylMSO in PG-EtOH-H2O. These results emphasize that the selective effect of an enhancer is the result of a tridimensional interaction between the drug, the skin, and the enhancer, in a specific environment.