Topical alprostadil cream (Vitaros) is approved in Canada and Europe for the treatment of erectile dysfunction. To determine the effects on the female urogenital tract with repeated administration of the entire dose (300 μg alprostadil containing 2.5% dodecyl-2-n,n-dimethylaminopropionate hydrochloride), the vaginal pH, flora, and histology were assessed as a model for 100% transference from male to the female during unprotected sexual intercourse. Female cynomolgus monkeys were administered the entire dose of Vitaros for 14 days with a 7-day recovery. Relative to vehicle and placebo cream, the vaginal pH and microflora were determined at baseline and weekly, thereafter. Vaginal biopsies were evaluated at the end of dosing and recovery. All animals were clinically normal for the study duration, and the vaginal pH was consistent between dose groups and the dosing period. Vaginal microflora and histopathology findings of mild inflammation were generally similar across treatment groups. In conclusion, repeated vaginal exposure to Vitaros did not alter the pH, microflora, or histology after 14 daily doses, supporting the safety of Vitaros transference to the female partner.

No abstract

Transdermal delivery of topically applied compounds is limited by the stratum corneum (SC) protective barrier. Penetration enhancers have been employed to perturb the skin barrier and enhance the transdermal flux of drugs. The novel excipient, dodecyl-2-N, N-dimethylaminopropionate hydrochloride (DDAIP-HCl), was evaluated for penetration activity of minoxidil in human cadaver skin. Minoxidil skin flux through human cadaver skin mounted on Franz cells was investigated with and without the presence of DDAIP-HCl. Enhanced minoxidil permeation levels were observed with DDAIP-HCl at concentrations of 0.05% and 0.5% through human cadaver skin relative to the formulation of the marketed hair loss product Rogaine ® (5% minoxidil) over a 24-hour period. Increased minoxidil penetration may lead to a better efficacy and clinical response in the treatment of male pattern hair loss or Androgenetic alopecia.