Abstract
Abstract
The effects of the percutaneous transport of vehicles and the transport of β-aminopropionitrile (βAPN) in vehicles were studied in rats. The bioavailability of topically administered βAPN was determined by measuring the degree of collagen cross-linking inhibition in the underlying granuloma tissue. Granulomas were induced by subcutaneous implantation of polyvinylalcohol sponges. From the 4th to 12th days postimplantation, a 20 mg/cm2 dose of βAPN fumarate was applied. Vehicles employed included dimethylsulfoxide (DMSO), urea, and occlusion. DMSO significantly enhanced the effect of βAPN in reducing the cross-linking of collagen. βAPN administered onto urea-pretreated skin and followed by occlusion in the granuloma tissue was more effective than βAPN in 30% DMSO, but only in the parameter reflecting extractibility of collagen into urea or thiocyanate solutions. The results suggest that βAPN administered topically in an appropriate vehicle penetrates the granuloma tissue and affects collagen polymerization. Though βAPN was topically administered, a systemic effect from the drug was evident, as documented by lower body weight of treated rats.
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