Bb. Michniak et al., IN-VITRO EVALUATION OF A SERIES OF AZONE ANALOGS AS DERMAL PENETRATION ENHANCERS .3. ACYCLIC AMIDES, International journal of pharmaceutics, 110(3), 1994, pp. 231-239
A series of acyclic amides was synthesized and tested for enhancement
properties using excised hairless mouse skin and hydrocortisone 21-ace
tate as the model drug. All compounds were applied at 0.4 M (or at the
ir respective saturation solubilities) in propylene glycol. Atone (0.4
M) was used as a standard enhancer. Enhancement ratios were calculate
d for flux, 24 h diffusion cell receptor concentrations (Q(24)) and 24
h full-thickness mouse skin steroid content. Enhancer 5 showed the hi
ghest activity for flux (35.22-fold over control), 24 h receptor conce
ntration (79.86-fold over control) and skin drug content (4.3-fold ove
r control). These enhancement ratios were higher than those for Atone
which were 19.51, 38.30 and 1.5-fold over control, respectively. Enhan
cers 4, 10 and 11 showed similar Q(24) values to Atone, and 3, 9 and 1
0 increased skin steroid content to a greater extent than Atone.