Open AccessNovel approach to improve permeation of ondansetron across shed snake skin as a model membrane
Author(s) -
Takahashi Koichi,
Rytting J. Howard
Publication year - 2001
Publication title -
journal of pharmacy and pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.745
H-Index - 118
eISSN - 2042-7158
pISSN - 0022-3573
DOI - 10.1211/0022357011776135
Subject(s) - azone , ondansetron , permeation , chemistry , oleic acid , chromatography , transdermal , pharmacology , ethanol , stratum corneum , membrane , biochemistry , anesthesia , medicine , nausea , pathology
The purpose of this study was to investigate the feasibility of transdermal drug delivery of ondansetron, an antagonist of the 5‐HT 3 receptor, used for the treatment of chemotherapy‐induced emesis. The permeability of ondansetron 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. Ethanol increased the flux at a concentration of 40% or more. The solubility of ondansetron also increased as the ethanol concentration increased. The permeability coefficient increased after pretreatment of the shed snake skin with Azone, oleic acid or lauryl alcohol. Further improvement of the permeability was observed when ethanol was combined with other enhancers and was maximum for the combination of ethanol and oleic acid. Oleic acid dramatically 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 direct effect on the stratum corneum or via counterion formation of an ion‐pair. The maximum flux obtained from the combination of ethanol and other enhancers seems to be high enough to obtain a therapeutic effect.