Abstract
Among various acylated β-cyclodextrins where all hydroxyl groups are substituted with different acyl groups, trivaIeryl β-cyclodextrin (TV-β-CyD) preferentially formed a transparent, adhesive thin-film. For example, when ethanol solution of TV-β-CyD was spread on the backing membranes such as polyethylene terephthalate film, polyethylene film and aluminium foil, a transparent film was formed, the film being tightly stuck on the membranes. The detaching force of TV-β-CyD film was higher and the decrease in the force by the addition of oleic acid was smaller than those of a commercial silicone pressure-sensitive adhesive which is used in transdermal drug delivery system. A vasodilator, isosorbide dinitrate (ISDN), was incorporated in TV-β-CyD film in molar ratios of 1 : 1 and 2 : 1 (ISDN : TV-β-CyD). The release rate of ISDN from TV-β-CyD film increased with increase in the film area, and slightly increased by the addition of oleic acid in the film. The plasma levels of ISDN after topical application of TV-β-CyD film containing ISDN to abdominal skin of rats were maintained 100 ng/ml for about 10 hours. The results suggests that TV-β-CyD film can serve as a drug reservoir for prolonged release of water-soluble drugs in transdermal preparations.
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