Skin distribution and pharmaceutical aspects of adapalene gel.
BACKGROUND
The formulation of topical dermatologic products must take into account efficacy, safety, and patient compliance.


OBJECTIVE
We describe how an aqueous gel containing adapalene, a novel naphthoic acid derivative was selected for the topical treatment of acne.


RESULTS
Dose selection was made using established in vivo models. In the Rhino mouse the comedolytic effect of adapalene 0.1% gel was similar or superior to that of a reference formulation containing 0.025% tretinoin. Qualitative distribution of adapalene after topical application was assessed on cryosections of human skin. They showed rapid penetration of adapalene into the pilosebaceous unit. A liberation/penetration study demonstrated that significant quantities of adapalene were present in epidermis and dermis, but only 0.01% of the applied dose penetrated through the skin.


CONCLUSIONS
This formulation should result in effective and well-tolerated treatment of acne vulgaris with good patient compliance.
Allec
J
J
CIRD Galderma, Sophia Antipolis, France.
Chatelus
A
A
Wagner
N
N
D000068816:Adapalene; D000287:Administration, Topical; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D002478:Cells, Cultured; D016503:Drug Delivery Systems; D005260:Female; D005782:Gels; D006801:Humans; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D009281:Naphthalenes / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D011817:Rabbits; D012867:Skin / Q000378:metabolism*
D000894:Anti-Inflammatory Agents, Non-Steroidal; D005782:Gels; D009281:Naphthalenes; D000068816:Adapalene