K. Takahashi et Jh. Rytting, Novel approach to improve permeation of ondansetron across shed snake skinas a model membrane, J PHARM PHA, 53(6), 2001, pp. 789-794
The purpose of this study was to investigate the feasibility of transdermal
drug delivery of ondansetron, an antagonist of the 5-HT3 receptor, used fo
r the treatment of chemotherapy-induced emesis. The permeability of ondanse
tron from an aqueous suspension through shed snake skin as a model membrane
was very low and in order to improve it, several enhancers were tested. Et
hanol increased the flux at a concentration of 40% or more. The solubility
of ondansetron also increased as the ethanol concentration increased. The p
ermeability coefficient increased after pretreatment of the shed snake skin
with Azone, oleic acid or lauryl alcohol. further improvement of the perme
ability was observed when ethanol was combined with other enhancers and was
maximum for the combination of ethanol and oleic acid. Oleic acid dramatic
ally increased the partition of ondansetron to n-hexane and shed snake skin
. Oleic acid may enhance the permeation of ondansetron in two ways: by a di
rect effect on the stratum corneum or via counterion formation of an ion-pa
ir. The maximum flux obtained from the combination of ethanol and other enh
ancers seems to be high enough to obtain a therapeutic effect.