Abstract
The permeation of radiolabeled lidocaine through full-thickness hairless mouse skin and dermatomed human epidermis was studied under infinite-dose conditions using a flow-through diffusion apparatus. The donors consisted of 5% suspensions in 40% propylene glycol gelled with 1% hydroxypropyl cellulose and preserved with 0.25% chlorobutanol. The pH was adjusted to several values and the solubility in each donor was measured. Steady-state flux values were subjected to mathematical treatment to estimate the permeability coefficients ( P) of the ionized and unionized forms of lidocaine. The permeability coefficient for unionized lidocaine through hairless mouse skin was no more than 15 times greater than for the ionized form; a 50-fold difference was obtained with human epidermis. The permeability differences indicate that hairless mouse skin is not an adequate in vitro substitute for human skin when considering lidocaine penetration.
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