moisture, decreased laxity, and impaired wound healing have all been characterized in reports on postmenopausal women.2 Studies have shown a decrease in estrogen levels leads to a 30% loss of collagen in the first 5 years of menopause.3 Estrogen has been found, at normal blood levels, to help retain and restore skin moisture through the promotion of sebum se- cretion, primarily by regulating the expression of insulin-like growth factor receptors and increasing the production of insu- lin-like growth factors from fibroblasts.4 Women of menopausal age seek alternatives to HRT regimens that are linked with an increase in systemic estrogen. By creating a non-hormonal es- trogen receptor activator (NERA), Ferndale Pharma Group has developed another approach to address aging in the estrogen deficient female. Emepelle (Biopelle, Ferndale Pharma Group, Ferndale, MI) is a new category of skin care. The signature ingredient, Methyl Estradiolpropanoate (MEP), is not a hormone. It is specifically a non-hormonal compound that can activate estrogen receptors on skin cells.Thus, MEP is an estrogen ana- log that activates the cutaneous estrogen receptor. Once that estrogen receptor activation takes place, the remaining com- pound has no further activity and is found to be an inactive metabolite.5
Methyl Estradiolpropanoate
Facial skin aging is accelerated in postmenopausal females due to decreased collagen, reduced hydration, and loss of skin elasticity constituting the characteristics of EDS. The presence of estrogen receptors on dermal fibroblasts and epidermal kera- tinocytes confirms the role of estrogen in skin health. A recent double-blind randomized pilot study evaluated the efficacy and tolerability of topical MEP as an anti-aging cosmeceutical with estrogen-like cutaneous effects in postmenopausal women who had never taken hormone replacement therapy (HRT). MEP was applied to the face twice daily for 14 weeks but was metabo- lized in the skin to an inactive compound avoiding estrogen side effects, as demonstrated by the safety study. The efficacy study investigator noted MEP induced statistically significant improvement from baseline at week 14 in dryness (P<0.001), laxity (P=0.001), atrophy (P=0.003), and dullness (P<0.001) as compared to vehicle. Four of nine subjects in the biopsy sub study demonstrated an increase in fibroblast's estrogen recep- tor staining. The novel concept of a safe and efficacious soft estrogen facial cosmeceutical may provide appearance ben-efits for postmenopausal women.
The safety of topical MEP was demonstrated by the lack of ac- tive MEP and the presence of the carboxylic acid MEP inactive metabolite in the serum of subjects who had used the formula- tion for 12 weeks. This soft effect allowed targeted delivery of the MEP to the skin without systemic side effects. Restoration of estrogen-like skin effects might induce the production of col- lagen I, responsible for the strength of the skin, and collagen III, contributing to the elastic skin properties, while reducing the expression of matrixmetalloprotease 1 (MMP-1).5
Methyl Estradiolpropanoate (MEP) is a synthetic estrogenic sterol ester, which has been shown to have estrogen-like cu- taneous effects but is metabolized in the skin to an inactive compound, thus avoiding estrogen side effects.4 Emepelle skin care regimen consists of Emepelle Serum and Night Cream containing MEP that is applied to the face to specifically target estrogen deficient skin.This skincare line takes a multifactorial approach to treat both intrinsic aging and photoaging by in- cluding a number of other cosmeceutical agents.
Emepelle Serum
The Emepelle Serum is a fast-absorbing, oil-free formulation that can be layered with sunscreen or under makeup. The serum contains 1% MEP to help activate estrogen receptors in the skin6,7 and is intended for use in either the morning, the evening, or both morning and evening.
The ingredient niacinamide helps induce collagen synthesis and reduce the signs of UVâ€induced skin aging. Topical nia- cinamide has shown significant skin appearance improvement effects for clinical signs of photoaging, hyperpigmentation, red blotchiness, and skin sallowness.8 The formula also contains the antioxidants vitamin C, vitamin E, and ferulic acid, which help neutralize free radicals and prevent cell damage from UV radiation.9,10,11 A blend of peptides helps combat oxidative stress and helps improve the appearance of fine lines, wrinkles, and skin laxity.4 Hyaluronic acid helps hydrate and maintain the skin’s moisture barrier.12
Night Cream
The key ingredients in Emepelle Night Cream include 2% MEP that helps to restore the natural function of estrogen deficient skin while utilizing the skin’s natural nighttime repair activities. Retinol 0.1% and hydroxypinacolone retinoate 0.05% aid in nightly rejuvenation and stimulate the production of new blood vessels in the skin, which help improve skin color and reduce the appearance of wrinkles.13 The niacinamide addresses skin tone and texture to help brighten and smooth the appearance of fine lines and wrinkles and provides additional antioxidant protection.8 The inclusion of tetrapeptide-26, palmitoyl oligo- peptide, and palmitoyl tetrapeptide-7 supports cell proliferation and helps combat oxidative stress14; and emollients and humec- tants help hydrate the skin and maintain its moisture barrier.
Methyl Estradiolpropanoate
Facial skin aging is accelerated in postmenopausal females due to decreased collagen, reduced hydration, and loss of skin elasticity constituting the characteristics of EDS. The presence of estrogen receptors on dermal fibroblasts and epidermal kera- tinocytes confirms the role of estrogen in skin health. A recent double-blind randomized pilot study evaluated the efficacy and tolerability of topical MEP as an anti-aging cosmeceutical with estrogen-like cutaneous effects in postmenopausal women who had never taken hormone replacement therapy (HRT). MEP was applied to the face twice daily for 14 weeks but was metabo- lized in the skin to an inactive compound avoiding estrogen side effects, as demonstrated by the safety study. The efficacy study investigator noted MEP induced statistically significant improvement from baseline at week 14 in dryness (P<0.001), laxity (P=0.001), atrophy (P=0.003), and dullness (P<0.001) as compared to vehicle. Four of nine subjects in the biopsy sub study demonstrated an increase in fibroblast's estrogen recep- tor staining. The novel concept of a safe and efficacious soft estrogen facial cosmeceutical may provide appearance ben-efits for postmenopausal women.
The safety of topical MEP was demonstrated by the lack of ac- tive MEP and the presence of the carboxylic acid MEP inactive metabolite in the serum of subjects who had used the formula- tion for 12 weeks. This soft effect allowed targeted delivery of the MEP to the skin without systemic side effects. Restoration of estrogen-like skin effects might induce the production of col- lagen I, responsible for the strength of the skin, and collagen III, contributing to the elastic skin properties, while reducing the expression of matrixmetalloprotease 1 (MMP-1).5
Methyl Estradiolpropanoate (MEP) is a synthetic estrogenic sterol ester, which has been shown to have estrogen-like cu- taneous effects but is metabolized in the skin to an inactive compound, thus avoiding estrogen side effects.4 Emepelle skin care regimen consists of Emepelle Serum and Night Cream containing MEP that is applied to the face to specifically target estrogen deficient skin.This skincare line takes a multifactorial approach to treat both intrinsic aging and photoaging by in- cluding a number of other cosmeceutical agents.
Emepelle Serum
The Emepelle Serum is a fast-absorbing, oil-free formulation that can be layered with sunscreen or under makeup. The serum contains 1% MEP to help activate estrogen receptors in the skin6,7 and is intended for use in either the morning, the evening, or both morning and evening.
The ingredient niacinamide helps induce collagen synthesis and reduce the signs of UVâ€induced skin aging. Topical nia- cinamide has shown significant skin appearance improvement effects for clinical signs of photoaging, hyperpigmentation, red blotchiness, and skin sallowness.8 The formula also contains the antioxidants vitamin C, vitamin E, and ferulic acid, which help neutralize free radicals and prevent cell damage from UV radiation.9,10,11 A blend of peptides helps combat oxidative stress and helps improve the appearance of fine lines, wrinkles, and skin laxity.4 Hyaluronic acid helps hydrate and maintain the skin’s moisture barrier.12
Night Cream
The key ingredients in Emepelle Night Cream include 2% MEP that helps to restore the natural function of estrogen deficient skin while utilizing the skin’s natural nighttime repair activities. Retinol 0.1% and hydroxypinacolone retinoate 0.05% aid in nightly rejuvenation and stimulate the production of new blood vessels in the skin, which help improve skin color and reduce the appearance of wrinkles.13 The niacinamide addresses skin tone and texture to help brighten and smooth the appearance of fine lines and wrinkles and provides additional antioxidant protection.8 The inclusion of tetrapeptide-26, palmitoyl oligo- peptide, and palmitoyl tetrapeptide-7 supports cell proliferation and helps combat oxidative stress14; and emollients and humec- tants help hydrate the skin and maintain its moisture barrier.
METHODS
An open-label study was designed to evaluate the efficacy and patient perception of Emepelle’s skin care regimen containing MEP on treating Estrogen-Deficient Skin (EDS).
Fourteen female subjects aged 53-68 years (mean, 60 years) in generally good health who have been amenorrheic for at least 1
Fourteen female subjects aged 53-68 years (mean, 60 years) in generally good health who have been amenorrheic for at least 1
