SKIN MICROCIRCULATION ACTIVATION AND SEX FLUSH
Menthyl nicotinate is a new, revolutionary substance that can be used as an active ingredient in sexual recreational products, thanks to its ability to penetrate through the skin barrier, optimize the interconnections between skin and nervous system and activate skin microcirculation significantly (cf. figure 4), without causing any annoying hyperemia or irritation. On the contrary, it produces a dual effect, i.e. modulated vasodilation and a pleasant hot-cold sensory effect in the area of application.
Once absorbed in the skin, menthyl nicotinate is readily hydrolyzed into its two initial components, niacin and menthol (cf. Figure 5).
The subcutaneous release of niacin (hot sensory effect) and menthol (cooling sensory effect) provides a “cell turgor” or “cool tingling” effect, which indicates a beneficial increase in the microcirculatory activity that is usually perceived a few minutes (3 to 5) after application, and can continue for up to one hour after application.
VAGINAL LUBRIFICATION AND SEXUAL AROUSAL
In a healthy female body, the stimulation/vasodilation function and the production of vaginal lubricant are physiologically concurrent and integrated.
“The first pelvic response to sexual stimulation is the production of vaginal lubrication… This material appears on the walls of the vaginal barrel within 10 to 30 seconds from the onset of any form of sexual stimulation. Clitoral reaction does not develop as rapidly as the production of vaginal lubrication.”1
“The postulated increase in blood flow to the clitoris is associated with increased sensation and enhanced sexual arousal including increased vaginal lubrication and labial engorgement.”2
Therefore, it is the excitement phase itself that triggers the dilation of perivaginal arterioles with the consequent sweeping of vascular transudate across the vaginal epithelium associated, almost simultaneously, to enlargement in the diameter and length of the clitoris and to the expansion of the upper half of the vagina. This explains why the vaginal lubrication is considered the primary physical signal of female arousal. Sexual excitement could then be summarized in the following interrelated functions: pelvic vasocongestion, vaginal lubrication and expansion, external genital engorgement.3
It is the stimulation of the very sensitive nerve endings situated in vaginal walls and surrounding tissues that causes vasocongestion and consequent production of lubricant transudate into the vaginal barrel.
Estrogen is the hormone responsible for maintaining the vaginal mucosa and allowing transudation and lubrication to occur.4
However, a continued lack of lubrication may lead to discomfort or even pain during sex, which may eventually be interpreted by her partner as a lack of interest and thus result in a distressed sexual relationship.
The numerous physical, psycho-social, emotional and/or relational causes of such situations are often very complex and composite. Therefore, they should be individually treated through the inter-disciplinary collaboration of professionals specifically dedicated to woman’s sexual health e well-being. There is however an extensive medical literature supporting the use of lubricants or topical products aiming at promoting or at least enhancing the sensorial characteristics and the related lubrication of the excitement phase. Such preparations are not exerting a pharmacological or metabolic function and therefore cannot be considered a definite solution in the treatment of FSD. However, they represent a valid supporting tool for the therapy, contributing to prevent the above mentioned impaired relationships and to restore sexual life to its original playful dimension.
In this regard, MENTHYL NICOTINATE (trade name NICOMENTHYL®) represents an active principle extremely interesting, usable in topical preparations for the prevention and treatment of vaginal dryness and generally indicated for all those subjects looking for a better sexual response.
NICOMENTHYL® is a multifunctional COSMETIC SENSORIAL AGENT, able to enhance skin microcirculation, optimizing the interconnections between the skin and the nervous system to intensify pleasure for deeper and more intense sexual performance and orgasm, with no irritation, no sensitization.
The following safety tests have been carried out on menthyl nicotinate:
- in vitro skin irritation test on 3D reconstructed human epidermis (OECD 439);
- in vitro model testing to predict skin sensitization through assessment of the stimulating potential on the immune cellular response mediated by monocyte/macrophage cells;
- in vitro eye irritation test through the Neutral Red Uptake Cytotoxicity Assay;
- in vitro eye irritation test using the Het Cam (Hen’s Egg Test Chorio-Allantoic Membrane) test method on embryonated chicken eggs;
- evaluation of vaginal mucosa tolerability using the in vitro reconstructed vaginal epithelium test method, both with pure substance and in different concentrations (1.5%, 2.0%, 2.5%, 3.0%), with measurements taken 1 hour and 4 hours after application.
All the tests above have confirmed the absence of irritating and/or sensitising effects on skin and vaginal mucosa.
Evaluation of the genotoxic potential of Salmonella typhimurium strains in the presence and in the absence of metabolic activation (Ames test). Nico-menthyl did not show any mutagenic potential.
In vitro studies
The antimicrobial efficacy of NICOMENTHYL®, i.e. its ability to inhibit the proliferation of microbial strains of different nature, pathogenic for humans, was assessed through a contact inhibition test on agar solid cultures. The following strains were tested: a Gram+ bacterium, Staphylococcus aureus, a yeast, Candida albicans, and Microsporum canis, a fungus. (S. aureus is a saprophyte of the skin, which can become pathogenic under certain conditions, such as immunosuppression, as C. albicans, whereas M. canis is a dermatophyte responsible for various forms of Tinea corporis).
NICOMENTHYL® has shown an excellent antimicrobial effect through contact with all three strains:
Staphylococcus aureus: 0,1% <MIC< 0,5%.
Microsporum canis: 0,5% <MIC< 1,0%.
Candida albicans: MIC ≈ 0,5%.
In vivo studies
A microcirculation stimulation activity test through Laser Doppler velocimetry was carried out on 20 voluntaries of both sexes (9 men and 11 women) with a mean age of 41.2 years, using a cosmetic cream containing 2% of NICO-MENTHYL®, compared to a negative control (placebo). The results showed a statistically significant increase in microcirculatory flow values after 15 minutes (+62.8% compared to the value at T0) and 30 minutes (+72.2% compared to the value at T0). This effect continued up to 60 minutes after application (+32.2% compared to the value at T0), as shown in the chart (Figure 11).
The same test has been carried out on other 20 subjects of both sexes, with a mean age of 44,9 years, using a topical preparation containing 3% of NICOMENTHYL®, compared to a negative control (placebo). Results are shown in figure 12.
It is to be noted that increases in microcirculatory flow values reached remarkable levels, i.e. +78,7% at 15 minutes, +147,1% at 30 minutes and +87,4% at 60 minutes after application, without any irritating and/or sensitising effects.
In conclusion, menthyl nicotinate, used in the recommended concentrations, represents an ideal and unique primary sensorial agent, a non-irritating and non-sensitizing effective vasodilator (as evidenced by safety and efficacy tests), biocompatible, beneficial to skin and through skin (releases vitamin B3 and menthol) and producing a long lasting unique exciting sensation.
To rediscover the purest and most intense physiological pleasure. Without side effects.
© 2018 Multichem R&D Srl - All rights reserved – NICOMENTHYL® is a registered trademark of MULTICHEM R&D Srl
Topical sexual stimulants containing NICOMENTHYL® (menthyl nicotinate) are protected by Italian, European and US patents.
1 William H. Masters, Virginia E. Johnson – Human Sexual Response – Ishi Press International, 1966, republished in January 2010, page 48.
2 Eleonora B. Pasqualotto, Fabio Firmbach Pasqualotto, Bernardo P. Sobreiro, Antonio Marmo Lucon – Female Sexual Dysfunction: the important points to remember – Clinics 60(I):51-60, 2005, page 58.
3 Simonelli C, Rossi R e Forleo R. - Le disfunzioni sessuali femminili - Encycl Méd Chir (Elsevier SAS, Paris, tutti i diritti riservati). Ginecologia-Ostetricia, 166-A-10, 2003, 10 p. See also: Kyan J. Allahdadi et al. - Female Sexual Dysfunction: Therapeutic Options and Experimental Challenges - Cardiovasc Hematol Agents Med Chem. 2009 Oct; 7(4): 260–269.
4 Eleonora B. Pasqualotto, et al. ibidem, page 54.