Pc. Lerk et H. Sucker, APPLICATION OF SUCROSE LAURATE IN TOPICAL PREPARATIONS OF CYCLOSPORINE-A, International journal of pharmaceutics, 92(1-3), 1993, pp. 203-210
The skin irritating potential of sucrose laurate was studied in the no
rmal guinea pig model. The results showed that sucrose laurate exhibit
ed no skin irritating effect at all. The application of sucrose laurat
e as an excipient in hydrophilic dermal preparations was investigated,
by measuring the inhibition of contact sensitivity skin reactions to
dinitrofluorobenzene (DNFB), after topical application of a cyclospori
n A hydrogel. The findings showed that the sucrose laurate hydrogel fo
rmulation was somewhat less effective as compared to a sucrose laurate
or ethanolic solution, but still superior to a reference paraffin sus
pension. The sucrose laurate/cyclosporin A hydrogel significantly redu
ced the skinfold thickness after 24, 32, 48 and 56 h of sensitization
(p < 0.01-0.001). Skin permeability experiments indicated that the suc
rose laurate has some intermediate skin permeability enhancing propert
ies. Conclusively, these findings showed that sucrose laurate is a sui
table, non irritating excipient for the dermal formulation of the poor
ly water soluble cyclosporin A. In order to obtain an optimal sucrose
laurate (trans)dermal hydrogel formulation, however, the effect of sur
factant or cyclosporin A concentration and the presence or absence of
occlusion must be subjected to further investigation.