TRANSDERMAL DELIVERY OF THE TETRAPEPTIDE HISETAL (MELANOTROPIN (6-9)).1. EFFECT OF VARIOUS PENETRATION ENHANCERS - IN-VITRO STUDY ACROSS HAIRLESS MOUSE SKIN
A. Ruland et al., TRANSDERMAL DELIVERY OF THE TETRAPEPTIDE HISETAL (MELANOTROPIN (6-9)).1. EFFECT OF VARIOUS PENETRATION ENHANCERS - IN-VITRO STUDY ACROSS HAIRLESS MOUSE SKIN, International journal of pharmaceutics, 101(1-2), 1994, pp. 57-61
The percutaneous absorption of the tetrapeptide hisetal as well as the
effect of various penetration enhancers on the permeation of hisetal
across hairless mouse skin was evaluated by in vitro methods in side-b
y-side diffusion cells (infinite dose technique). Although the molecul
ar weight of the tetrapeptide is about 4-fold higher in comparison to
the amino acids, the permeability coefficient of hisetal was found to
be in the same order of magnitude as those of the amino acids. (5.58 x
10(-5) cm h(-1)). The permeation of hisetal was increased by enhancer
treatment with oleic acid (3%) by a factor of 28. The relatively new
permeation enhancer DDAA was found to increase the permeation of hiset
al in concentrations of 3% to a higher extent (1.5-fold) than Azone(R)
at the same concentration. The mode of action of DDAA could not be de
termined by these investigations. However, it was shown that the DDAA
effects as well as those of the other penetration enhancers were not r
eversible within 12 h. These findings lead to the assumption that DDAA
induces its permeability enhancing effect on the basis of changes in
the lipid structure of the stratum corneum similarly to Azone(R) and o
leic acid.