Nicomenthyl - Activator of the cutaneous microcirculation with a hot-cold sensorial effect

Cover Cosmetic Technology 2015 (18)1

NICOMENTHYL® is composed of pure MENTHYL NICOTINATE, with no residues of other nicotinates, obtained through a new and exclusive industrial synthesis process developed over 20 years of research at Multichem & Pink Frogs Laboratory in Rozzano (Milan) - Italy.
NICOMENTHYL® represents a new and revolutionary substance for cosmetic use that can significantly activate the cutaneous microcirculation without causing bothersome hyperaemia or irritations, on the contrary it generates a pleasant hot-cold sensation focused on the area of application.

It is derived from the chemical reaction between two natural components:

  • Menthol, obtained from the essential oil of mint, has a refreshing and soothing effect on the skin. It is also, as recently found by researchers at the Faculty of Medicine of the University of Padova, capable of turning the white adipose tissue into brown tissue, i.e. burning fats therein stored and consequently producing heat.
  • Nicotinic acid, also known by the names of Niacin or Vitamin B3 or Vitamin PP (Pellagra-Preventing), is used by the organism for forming enzymes (NAD and NADP) that are essential for energy metabolism.

These coenzymes take part in over 200 enzymatic reactions within the organism. Nicotinic acid helps break down and assimilate proteins, fats and glucosides. It plays a fundamental role in the formation of erythrocytes, in optimizing blood circulation and in providing oxygen to the cells. Its properties are used in topical applications for improving the barrier effect, oxygenating and nourishing the skin, accelerating cellular differentiation and cicatrisation, as well as for its anti-inflammatory and detoxifying effects (i.e. capable of eliminating, through the microcirculation, toxins and residues of foreign chemical compounds accumulated in the subcutaneous adipose tissue).

REACTION MECHANISM

Menthyl nicotinate is easily absorbed by the skin and metabolized into its primary components: menthol and nicotinic acid. Since menthol is a vasoconstrictor and nicotinic acid is a vasodilator, there is a soft and pleasant sensation of freshness (due to the menthyl component of the molecule) and a simultaneous sensation of tingling warmth (due to the nicotinic component of the molecule) a few minutes following the application of a cosmetic product containing NICOMENTHYL® in the recommended dosages. The result is an absolutely unique sensorial effect, a pleasant sensation of cellular turgor or hot-cold subcutaneous micro massage, a “cool tingling”, indicating a beneficial increase of microcirculation, that can even last up to one hour from application. These sensorial effects are quite different from those caused by formulations containing free menthol and the common dimethyl, ethyl or benzyl nicotinates or other menthol esters, which may occasionally cause excessive hyperaemia and sensitivity.

PROPERTIES AND TECHNICAL SPECIFICATIONS

NICOMENTHYL® (INCI Name: Menthyl nicotinate; CAS 40594-65-8; EINECS 254-991-1) is the menthyl ester of nicotinic acid, i.e. the product resulting from the esterification reaction of the nicotinic acid with the menthol.
The tecnichal characteristics of NICOMENTHYL® are found in Table 1.

ORGANOLEPTIC PROPERTIES
Appearance Liquid
Colour White transparent, slight yellowish reflections
Smell Odourless
PHYSICO-CHEMICAL PROPERTIES
Specific gravity (at 20°C) 1,04
Solubility Insoluble in water; soluble in alcohol, polar oils, esters
Boiling point at atmospheric pressure 292,23°C
Refractive index 1,5060-1,5074
Heavy metals (ppm) < 0,5
Arsenic (ppm) < 0,5
MICROBIOLOGICAL PROPERTIES
Total bacterial load (cfu/g) < 10
Moulds/Yeasts(cfu/g) < 10
Pathogens Absent
Shelf life: Thermostable. No added preservatives or antioxidants are required nor any special condition for storage.

Table 1 Technical Properties of NICO-MENTHYL®

EFFICACY

In vitro studies

The antimicrobial effectiveness of NICO-MENTHYL® was assessed, i.e. its capacity to inhibit the proliferation of some human pathogenic microbial strains, through a contact inhibition assay on solid agar cultures. The strains tested were a Gram + bacteria or Staphylococcus aureus, a yeast, Candida albicans and a mould, Microsporum canis (S. aureus is a skin saprophyte that can become pathogenic in certain situations e.g. immunedepression. C. albicans as well can become pathogenic, while M. canis is a dermatophyte that causes various types of Tinea corporis).
NICO-MENTHYL® has shown excellent antimicrobial effect towards all three of the strains:
Staphylococcus aureus: 0,1% <MIC< 0,5%
Microsporum canis: 0,5% <MIC< 1,0%
Candida albicans: MIC ≈ 0,5%

In vivo studies

Doppler Laser Blood-flow Velocity Meter on twenty volunteers of both sexes (9 males, 11 females), with an average age of 41.2 years, with a cosmetic cream containing 2% NICO-MENTHYL®, in comparison with a placebo. The results obtained displayed a statistically significant increase in the microcirculatory flow values after 15 minutes (+62.8% with respect to the value of T0) and 30 minutes (+72.2% with respect to the value of T0). The effect persisted up to 60 minutes from application (+32.2% with respect to the value of T0), as shown in the bar chart in Figure 1.

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Figure 1 – Summary chart of the placebo controlled clinical and instrumental assessment test of the effect of a cosmetic product containing 2% NICO-MENTHYL® on the superficial cutaneous microcirculation.

SAFETY

The following assessment tests were conducted on NICO-MENTHYL®: in vitro cutaneous irritation testing on 3D reconstructed human epidermis (according to OCED 439); in vitro model testing to predict skin sensitization through assessment of the stimulating potential of the investigated substance on the immune cellular response mediated by monocyte/macrophage cells; in vitro assessment of the ocular irritancy potential through cytotoxicity assay Neutral Red Uptake on cell culture and Het Cam testing on fertilized chicken eggs.
All tests have confirmed the absence of irritative and/or sensitizing effects.

APPLICATIONS AND POSOLOGY

The results of the studies conducted, its function of oxygenation of the tissues and its cutaneous microcirculatory action make of NICO-MENTHYL® an active substance that is absolutely safe and effective. Its properties are particularly indicated in products for cellulite treatment, hair loss prevention, anti-age formulations (hinders the slowdown of the cutaneous microcirculation caused by ageing or slackening of the tissues), sports massage products and as an adjuvant in the treatment of gingivitis and sensitive gums.
The recommended dosages are, depending on the formulation, from 0.5 to 3%. It is liposoluble. During manufacturing cycle, it can be processed either hot or cold.


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