The effects of skin-to-skin contact, application site washing, and sunscreen use on the pharmacokinetics of estradiol from a metered-dose transdermal spray

Abstract

The use of a transdermal estradiol spray did not result in a significant transfer of estradiol by skin-to-skin contact. Washing the application site did not significantly affect absorption of estradiol. Estradiol absorption was slightly decreased due to the application of sunscreen after study drug application, but was unaffected when sunscreen was applied before study drug.

Transdermal Estradiol and Testosterone Transfer in Man: Existence, Models, and Strategies for Prevention

“…The AUC 0-24 was calculated to evaluate serum estradiol concentration of the men at 4,8,12,16,20, and 24 h after the attempted transfer. In this trial, significant transfer did not occur as determined by a 90% CI for the ratio of post-contact mean AUC 0-24 (556.5) to pre-contact mean AUC 0-24 (538.0) of 1.00-1.07, which was entirely contained within a pre-determined 90% CI equivalence range of 0.80 to 1.25 [41] .…”

“…Clinical trials [36,38,39,41,42] and FDA data [40,[43][44][45][46][47] have examined the possibility of transdermal hormone transfer. However, the type of exposure, amount of transdermal hormone applied (i.e.…”

“…0.021) for estrone sulfate, indicating that sig- Table 1. In vivo human studies of transdermal transfer of topical estradiol and testosterone products [36,38,39,41,42] Wester et al [36] ZumBrunnen et al [ nificant transfer did occur by means of vigorous skin-toskin contact at the application site [39,40] . While clinical in vivo human trials of a transdermal estradiol gel and emulsion formulation have reported measurable transfer of the applied hormone dose, a spray formulation study yielded opposite results.…”

“…While clinical in vivo human trials of a transdermal estradiol gel and emulsion formulation have reported measurable transfer of the applied hormone dose, a spray formulation study yielded opposite results. Schumacher et al [41] conducted a single-center, open-label study to evaluate the amount of transfer between 20 postmenopausal women dosed with a 4.59-mg transdermal estradiol spray (Evamist ) and a group of 20 untreated, healthy men. Attempted transfer was by forearm contact of 5 min without movement, occurring 1 h after estradiol application, and was measured by pre-contact and post-contact serum estradiol levels in the healthy men.…”

The role of transdermal estrogen sprays and estradiol topical emulsion in the management of menopause-associated vasomotor symptoms

“…20 It has been shown that significant transfer of estradiol via skin-to-skin contact does not occur; washing the application site 1 hour after application does not affect absorption; and applying sunscreen 1 hour prior to application also does not affect absorption. 21 In a phase III, randomized, double-blind, placebo-controlled, parallel-group trial, Buster et al investigated the safety and efficacy of a transdermal e stradiol spray. 20 Postmenopausal women (n = 454) with at least 8 moderate-to-severe hot flashes per day (recorded in a daily diary) were randomly assigned to receive 1, 2, or 3 sprays of estradiol; or 1, 2, or 3 sprays of placebo to the inner forearm.…”