title: Follicular and percutaneous penetration pathways of topically applied minoxidil foam.
abstract: In the past, it was assumed that the intercellular route was the only relevant penetration pathway for topically applied substances. Recent results on follicular penetration emphasize that the hair follicles represent a highly relevant and efficient penetration pathway and reservoir for topically applied substances. This study investigates a selective closure technique of hair follicle orifices in vivo assessing interfollicular and follicular absorption rates of topical minoxidil foam in humans. In delimited skin area, single hair orifices or interfollicular skin were blocked with a microdrop of special varnish-wax-mixture in vivo. Minoxidil foam (5%) was topically applied, and transcutaneous absorption was measured by a new surface ionization mass spectrometry technique in serum. Different settings (open, closed or none of both) enabled to clearly distinguish between interfollicular and follicular penetration of the topically applied minoxidil foam. Five minutes after topical application, minoxidil was detected in blood samples when follicles remained open, whereas with closed follicles 30 min were needed. Highest levels were found first when both pathways were open, followed by open follicles and subsequently by closed follicles. These results demonstrate the high importance of the follicular penetration pathway. Hair follicles are surrounded by a dense network of blood capillaries and dendritic cells and have stem cells in their immediate vicinity, making them ideal targets for drug delivery.
authors.affiliation: Department of Dermatology and Allergy, Charité-Universitätsmedizin Berlin, Berlin, Germany.
authors.forename: Ulrike
authors.initials: U
authors.lastname: Blume-Peytavi
authors.forename: Lida
authors.initials: L
authors.lastname: Massoudy
authors.forename: Alexa
authors.initials: A
authors.lastname: Patzelt
authors.forename: Jürgen
authors.initials: J
authors.lastname: Lademann
authors.forename: Ekkehart
authors.initials: E
authors.lastname: Dietz
authors.forename: Utkur
authors.initials: U
authors.lastname: Rasulev
authors.forename: Natalie
authors.initials: N
authors.lastname: Garcia Bartels
mesh_terms: D000279:Administration, Cutaneous; D000328:Adult; D016503:Drug Delivery Systems; D006197:Hair / Q000378:metabolism; D018859:Hair Follicle / Q000166:cytology / Q000378:metabolism*; D006801:Humans; D008297:Male; D008914:Minoxidil / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption; D013234:Stem Cells / Q000502:physiology; D014665:Vasodilator Agents / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D055815:Young Adult
chemical_list: D014665:Vasodilator Agents; D008914:Minoxidil