Iontophoresis-targeted, follicular delivery of minoxidil sulfate for the treatment of alopecia

Guilherme Martins Gelfuso, Tais Gratieri, M. Begoña Delgado-Charro, Richard H. Guy, Renata Fonseca Vianna Lopez

Research output: Contribution to journalArticle

19 Citations (Scopus)

Abstract

Although minoxidil (MX) is a drug known to stimulate hair growth, the treatment of androgenic alopecia could be improved by delivery strategies that would favor drug accumulation into the hair follicles. This work investigated in vitro the potential of iontophoresis to achieve this objective using MX sulfate (MXS), a more water-soluble derivative of MX. Passive delivery of MXS was first determined from an ethanol–water solution and from a thermosensitive gel. The latter formulation resulted in greater accumulation of MXS in the stratum corneum (skin's outermost layer) and hair follicles and an overall decrease in absorption through the skin. Anodal iontophoresis of MXS from the same gel formulation was then investigated at pH 3.5 and pH 5.5. Compared with passive delivery, iontophoresis increased the amount of drug reaching the follicular infundibula from 120 to 600 ng per follicle. In addition, drug recovery from follicular casts was threefold higher following iontophoresis at pH 5.5 compared with that at pH 3.5. Preliminary in vivo experiments in rats confirmed that iontophoretic delivery of MXS facilitated drug accumulation in hair follicles. Overall, therefore, iontophoresis successfully and significantly enhanced follicular delivery of MX suggesting a useful opportunity for the improved treatment of alopecia.
Original languageEnglish
Pages (from-to)1488-1494
JournalJournal of Pharmaceutical Sciences
Volume102
Issue number5
Early online date28 Feb 2013
DOIs
Publication statusPublished - 1 May 2013

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Iontophoresis
Alopecia
Minoxidil
Sulfates
Hair Follicle
Pharmaceutical Preparations
Gels
Skin Absorption
Therapeutics
Water
Pituitary Gland
Hair
Cornea
Ethanol
minoxidil sulfate ester
Skin
Growth

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Iontophoresis-targeted, follicular delivery of minoxidil sulfate for the treatment of alopecia. / Gelfuso, Guilherme Martins; Gratieri, Tais; Delgado-Charro, M. Begoña; Guy, Richard H.; Vianna Lopez, Renata Fonseca.

In: Journal of Pharmaceutical Sciences, Vol. 102, No. 5, 01.05.2013, p. 1488-1494.

Research output: Contribution to journalArticle

Gelfuso, Guilherme Martins ; Gratieri, Tais ; Delgado-Charro, M. Begoña ; Guy, Richard H. ; Vianna Lopez, Renata Fonseca. / Iontophoresis-targeted, follicular delivery of minoxidil sulfate for the treatment of alopecia. In: Journal of Pharmaceutical Sciences. 2013 ; Vol. 102, No. 5. pp. 1488-1494.
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