Jh. Saurat et al., TOPICAL RETINALDEHYDE ON HUMAN SKIN - BIOLOGIC EFFECTS AND TOLERANCE, Journal of investigative dermatology, 103(6), 1994, pp. 770-774
The present study was designed to explore retinaldehyde, a natural met
abolite of vitamin A, has any biologic activity and is tolerated by hu
man skin. Biologic activity was shown by the induction of cellular ret
inoic acid-binding protein type 2 (CRABP 2) mRNA and protein; the rank
order for CRABP-2 increase was retinoic acid > retinaldehyde > 9 cis
retinoic acid > retinol > beta carotene. In volunteers treated 1-3 mon
ths with 0.5, 0.1, and 0.05% retinaldehyde, there was a dose-dependent
and significant increase in epidermal thickness, keratin 14 immunorea
ctivity, and Ki67-positive cells. The area of distribution of involucr
in, transglutaminase, and filaggrin immunoreactivity was also increase
d in a dose-dependent manner, and keratin 4 immunoreactivity was induc
ed in the upper epidermis. In pilot clinical tolerance studies, 229 pa
tients received topical retinaldehyde at different concentrations; the
1% preparation was tolerated by up to 70% of the treated subjects; to
lerance of the 0.5% preparation was slightly better, whereas both 0.1
and 0.05% preparations applied on facial skin were well tolerated and
allowed prolonged use (up to 3 years) in patients with inflammatory de
rmatoses. These findings indicate that topical retinaldehyde has biolo
gic activity and is well tolerated on human skin.