Article Nicomenthyl

Laboratories R&D - Multichem
NICO-MENTHYL®
menthyl
nicotinate
A
-
ctivator of the cutaneous microcirculation with a hot cold sensorial effect
O
O
Functions
General Activator of the cutaneous microcirculation,
particularly indicated for:
• Cellulitis treatment
• Hair loss prevention treatment
• Anti-age formulations (inhibit the slowdown
of cutaneous microcirculation associated with
ageing or slackening of the tissues)
• Sport massage products
• Adjuvant in the treatment of gingivitis and
sensitive gums
• Refreshing products for feet and legs
• Intimate hygiene products
• Cosmetic lip plumping treatments
• Spa treatment products
• Deodorant/antiperspirants
• Pre/after shave products
• Body lotions
NICO-MENTHYL® 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.
NICO-MENTHYL® 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.
R&D
Multichem
N
Origin
Obtained by a synthesis process from natural
components
INCI name Menthyl nicotinate
Formulation
Liposoluble. Can be processed either hot or cold
Recommended usage
0,5 - 3%
•
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
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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%
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 NICO-MENTHYL®
in the recommended dosages. The result is an absolutely unique
sensorial effect, a pleasant sensation of cellular turgor or hotcold 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.
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.
Properties and technical specifications
NICO-MENTHYL® (INCI Name: Menthyl nicotinate; CAS 40594-658; 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.
Safety
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
362,4°C
Refractive index
1,515
Heavy metals (ppm)
< 0,5
Arsenic (ppm)
< 0,5
The following assessment tests were conducted on NICOMENTHYL®: 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
Microbiological properties
The results of the studies conducted, its function
of oxygenation of the tissues and its cutaneous
Total bacterial load (cfu/g)
< 10
microcirculatory action make of NICO-MENTHYL® an
Moulds/Yeasts(cfu/g)
< 10
active substance that is absolutely safe and effective.
Pathogens
Absent
Its properties are particularly indicated in products
Shelf life: Thermostable. No added preservatives or antioxidants are required nor any
for cellulite treatment, hair loss prevention, anti-age
special condition for storage.
formulations (hinders the slowdown of the cutaneous
Table 1 Technical Properties of NICO-MENTHYL®
microcirculation caused by ageing or slackening of
the tissues), sports massage products and as an adjuvant in the
Efficacy
treatment of gingivitis and sensitive gums.
In vitro studies
The recommended dosages are, depending on the formulation,
The antimicrobial effectiveness of NICO-MENTHYL® was assessed,
from 0.5 to 3%. It is liposoluble. During manufacturing cycle, it can be
i.e. its capacity to inhibit the proliferation of some human
processed either hot or cold. Sold in 2kg or 5kg PE-HD packages.
pathogenic microbial strains, through a contact inhibition assay
O
30
NICO-MENTHYL 2%
+62,8%
25
O
N
PLACEBO
+72,2%
+32,2%
20
15
10
5
0
T 0
T 15m
T 30m
T 60m
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.
NICO-MENTHYL® is a registered trademark of MULTICHEM sas