Novel approach to improve permeation of ondansetron across shed snake skinas a model membrane

Citation
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
Citations number
21
Categorie Soggetti
Pharmacology & Toxicology
Journal title
JOURNAL OF PHARMACY AND PHARMACOLOGY
ISSN journal
00223573 → ACNP
Volume
53
Issue
6
Year of publication
2001
Pages
789 - 794
Database
ISI
SICI code
0022-3573(200106)53:6<789:NATIPO>2.0.ZU;2-W
Abstract
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.