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Trikenol Plus
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CENTERCHEM, INC. NORWALK, CT
Ph: 203-822-9800 Fax: 203-822-9820
www.centerchem.com
TRIKENOL PLUS
Dandruff is a scalp problem that is manifested by excessive desquamation, forming aggregates of corneal
cells as a result of acceleration in the renewal of epidermal cells. TRIKENOL PLUS is a new complex of
natural origin active ingredients for the treatment of dandruff.
SCALP AND DANDRUFF
The scalp is an area with a high number of hair follicles, sebaceous glands and sweat glands, and a vast and
complex innervation and vasculature. The sebaceous glands attached to hair follicles secrete sebum, which
is deposited on the scalp and provides it with protection and lubrication, being the main responsible for hair
flexibility and brightness.
Dandruff is defined as excessive desquamation of the
scalp accompanied by mild itching without signs of
inflammation. The appearance of dandruff is the result of
an increase in the rate of desquamation of the epidermis,
where cells of the basal layer require half the time
needed in a normal scalp to reach the stratum corneum.
This rapid proliferation causes an increase in the number
of corneal cells, accompanied by an anomalous
cementation and the appearance of large aggregates of
corneal cells (Hay RJ, 1997).
Figure 1. Pilosebaceous canal
Types of dandruff
1. Dry form or Pityriasis simplex
It is the most common form. People who suffer it have a dry, lackluster and rough scalp. The scales are
thin, white-gray in color, more or less adherent, and they can be detached after combing or
spontaneously. No inflammatory signs are present.
2.
Seborrheic form or Pityriasis steatoides
It is a desquamation state associated with the existence of seborrhea. The hair has a greasy and shiny
appearance, with yellowish and thicker scales. It can be accompanied by erythema, with more or less
intense itching, and inflammation of the scalp. It can also cause hair loss.
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Triggering mechanisms
A number of factors influence this functional disorder:

Environmental conditions. Dandruff manifests more acutely in winter and decreases in summer.

Hyperproliferative activity of the epidermis. There is an increase in mitotic activity of cells in the
basal layer of the epidermis of the scalp, so that the path of the keratinocytes to the stratum corneum
takes half the time (14 days).

Hormonal imbalance. Dandruff usually appears at puberty and progressively increases until the age
of 30.

3
Microbial flora. The scalp is colonized by microorganisms with a density of around 10 -10
5
2
microorganisms/mm , formed by species of Staphylococcus, Propionibacterium and Malassezia. Due
to the appearance of dandruff, the relative proportion of Malassezia is multiplied by 1.5-2.0, up to
75% of existing flora. The presence of excess fat promotes the multiplication and development of this
microorganism, because it can degrade sebum triglycerides. This leads to an increase in the amount
of free fatty acids existing in the scalp, especially oleic acid, which has a strong irritating ability that
can cause the stimulation of mitosis in cells of the basal layer.
Malassezia
The Malassezia genus comprises lipophilic yeasts differentiated in two species with defined physiological
properties: lipophilic strains such as Malassezia pachydermatis able to grow on routine laboratory media and
lipophilic yeasts that require the addition of long-chain fatty acids to the culture medium for their development,
such as the Malassezia furfur (=Pityrosporum ovale) species.
Recent studies on their characteristics have led to the classification of lipid-dependent strains in six genetically
distinct species: M. furfur (=Pityrosporum ovale), M. globosa, M. sympodialis, M. obtusa, M. restricta and M.
slooffiae (Aspiroz MC et al., 1997).
Other recent studies on dandruff show that the species of Malassezia detected in the scalp have been M.
restricta and M. globosa, while M. furfur (=P. ovale) has not been detected and therefore could be ruled out as
a potential dandruff agent (Gemmer et al., 2002)
Another study indicates that M. restricta, M. globosa and rarely M. sympodialis, have been detected in the
scalp, but not M. furfur (=P.ovale), M. obtusa, M. slooffiae and M. pachydermatis. It is explained that the
mechanism causing the dandruff is the presence of Malassezia globosa, which hydrolyzes sebum triglycerides
from the scalp using its lipase, resulting in the release of oleic acid. This irritating fatty acid penetrates the
stratum corneum of the scalp breaking the barrier function, triggering the hyperproliferation of the scalp and
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inducing a greater sebum secretion, so that it continues to feed the population of Malassezia (EHRS
Conference, 2002).
Anti-dandruff treatment
Current anti-dandruff formulations usually contain one or more active ingredients to correct each one of the
causes, such as:

Anti-fungal ingredients: azole family (climbazole).

Germicides: undecylenic acid, hexachlorophene, ketoconazole, quaternary ammonium compounds,
etc.

Cytostatic action germicides: sulfur, selenium, zinc pyrithione, piroctone olamine, etc.

Anti-seborrheic ingredients: sulfur compounds, some plant extracts.

Keratolytic ingredients: -hydroxy acids, salicylic acid, selenium sulfide, sulfur derivatives, urea.

Anti-itch ingredients: panthenol, some plant derivatives.
In all cases, effectiveness depends on the type of cosmetic formulation and the contact time of the active
principle with the scalp.
COMPOSITION
TRIKENOL PLUS is a synergistic blend of two plant origin ingredients, terpinen-4-ol and willow extract,
enriched with salicylic derivatives and developed to provide an effective anti-dandruff active ingredient
obtained from natural sources.
Terpinen-4-ol
Terpinen-4-ol is obtained by fractional distillation of tea tree oil (Melaleuca alternifolia). Its
color varies from transparent to pale yellow and it has a very characteristic odor mixture of
earth, wood and pepper.
Figure 2. Terpinen-4-ol
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Efficacy
Antimicrobial
It has been evaluated to observe its action against a wide range of microorganisms:
ORGANISM
MIC (%)
Staphylococcus aureus
0.25
Coryneform spp.
0.01
Propionibacterium acnes
0.10
Escherichia coli
0.25
Pseudomonas aeruginosa
0.50
Aspergillus niger
0.05
Pityrosporum ovales (M. furfur)
0.05
Tricophyton mentagrophytes
0.05
Trichophyton rubrum
0.05
Table 1. Efficacy of Terpinen-4-ol against microorganisms
Anti-inflammatory
The anti-inflammatory efficacy was evaluated by studying the reduction of erythema, induced by ultraviolet
radiation using solar simulation. Results show that, in addition to antimicrobial activity, terpinen-4-ol has an
anti-inflammatory action (Hart PH, 2000).
Inflammation reduction of Terpinen-4-ol
66
70
60
60
50
45
44
40
30
20
10
10
0
Indometacin 1%
Natural α-bisabolol Natural α-bisabolol
0.5%
0.25%
Terpinen-4-ol 1% Terpinen-4-ol 0.5%
Figure 3. Anti-inflammatory efficacy versus control
The benefits of Terpinen-4-ol are its stability, broad spectrum activity and anti-inflammatory action.
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Willow extract
Willow, Salix alba, is an evergreen tree belonging to the salicaceae
family up to 25 m high, with an erect trunk and a dark gray bark with large
grooves, ending in a narrow crown. Its leaves have a silvery-gray color
and they are serrated, up to 10 cm in length and covered with soft hairs
on both sides. The flowers arranged in catkins appear before the leaves.
The parts used in cosmetics are the dried leaves and bark of branches of
Salix alba.
The main constituents are polyphenols, flavonoids and salicylic derivatives. Polyphenols (8-20%) are
represented by catechic type tannins. Flavonoids (0.2-1.5%) are characterized by the glucosides of
isoquercitrin, naringin, isosalipurposide, quercetin and isorhamnetin.
Salicylic derivatives (1.5-11%) are represented by salicin or salicoside,
which is a glucoside in saligenin, salicortin, tremulacin and salireposide. It
also contains organic acids (salicylic, vanillic, syringic, caffeic, phydroxybenzoic, coumaric and ferulic acid), as well as oligo- and
polysaccharides (pectins, galactans and arabinans).
Willow extract is widely used in cosmetics and dermatology due to its moisturizing, keratolytic and purifying
properties. It also has properties to be used as an astringent, analgesic, anti-inflammatory and antimicrobial
active ingredient (Council of Europe, 2001).
In this case, it has been incorporated to TRIKENOL PLUS due to its anti-irritant, anti-seborrheic and
keratolytic action.
Salicylic derivatives
One of the best known and most representative is salicylic acid (2-hydroxybenzoic
acid), with the molecular formula C7H6O3 and CAS number: 69-72-7. This
substance is described in many pharmacopoeias (F. Eur, USP 25, F China, F Int.,
F. Japan, F Pol.).
Salicylic acid is applied topically to treat keratolytic and skin desquamation
Figure 4. Salicylic acid
disorders.
Its keratolytic properties (Huber et al., 1977) are also widely demonstrated in the literature. The exfoliating
action resulting from a decrease in cohesion between corneocytes and a normalization of the desquamation of
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the stratum corneum is due to the inhibition of enzymes involved in the cementation of corneocytes (Béani JC,
2002).
IN VITRO EFFICACY
Antifungal Activity
The activity of TRIKENOL PLUS was studied against Malassezia globosa and Malassezia furfur (=P. ovale),
determining the values of:

Minimum Inhibitory Concentration (MIC): minimum concentration that produces a total inhibition of
growth.

Strong Inhibition (SI): concentration that produces a considerable decrease in growth without
causing total inhibition.
This information is of great interest, because the aim is not a total action by the active ingredient, but an
inhibition which is enough so that skin's defense mechanisms can act.
Malassezia globosa
Malassezia furfur (=Pityrosporum ovale)
MIC
SI
MIC
SI
0.098%
0.024%
0.195%
0.024%
Table 2. Results of TRIKENOL PLUS in vitro test
TRIKENOL PLUS is active against the two Malassezias involved in dandruff, M. furfur and M. globosa, but it
shows greater activity against M. globosa, which has a more relevant role in dandruff, according to the recent
studies mentioned above.
Anti-irritating Activity
In order to evaluate the anti-irritant efficacy of the Willow Extract in TRIKENOL PLUS, the inhibition of
cyclooxygenase (COX), enzyme that catalyzes the formation of inflammatory mediators from arachidonic acid,
was measured.
The assay was performed on primary cultures of keratinocytes determining the content of prostaglandins
(PGE2) using an immunoassay and acetylsalicylic acid as a positive control. The results of this enzymatic
assay are shown in figure 5. It can be seen that Willow Extract (0.1%) produces an important reduction in the
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amount of prostaglandin (PGE2), which leads to a marked inhibition of cyclooxygenase. This effect is
comparable to those caused by acetylsalicylic acid used as control in the assay (0.1 mM).
% Cyclooxygenase inhibition
70
63.9
60
49.8
50
43.4
40
30
20
10
0
AS 1 mM
AS 0.1 mM
Willow extract
Figure 5. Results of the anti-irritant action of willow extract.
COSMETIC APPLICATIONS
TRIKENOL PLUS is a new natural origin active ingredient for the treatment of dandruff and the various factors
involved, both in dry dandruff and in seborrheic or greasy dandruff.
ACTION
ACTIVE INGREDIENT
EFFICACY
Microbial proliferation
Set of active ingredients of TRIKENOL
MIC=0.098 (M globosa) and 0.195 (M.
inhibitor
PLUS
furfur)
Anti-irritant
Willow extract
Cyclooxygenase inhibition=43.4%
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RECOMMENDED DOSAGE
TRIKENOL PLUS can be used to formulate transparent shampoos and lotions at different doses depending
on the desired effect or activity.

Anti-dandruff treatment:
0.25 %

Continued integral anti-dandruff treatment:
0.50 %

Shock integral anti-dandruff treatment:
1.00 %
BIBLIOGRAPHY
Aspiroz MC, et al. Taxonomía de Malassezia furfur: estado de cuestión. Rev Iberoam Micol 1997; 14: 147-149
(ref.5971).
Béani JC. L’acide salicylique comme agent coricide. Ann Dermatol Venereol 2002 ; 129 :933-935 (ref. 6973).
Committee of Experts on Cosmetic Products. Plants in cosmetics. Plants and plant preparation used as
ingredients for cosmetic products Volume II. Strasbourg: Council of Europe Publishing, 2001: 139-142
(68*1ANT).
Dandruff, part III: efective treatment requires products based on potent actives optimized for effective delivery
to scalp. P61. EHRS Conference. Brussels 2002.
Garrote A, et al. Caspa y seborrea (I). El farmacéutico 2003; 292: 81-86 (ref.5980).
Garrote A, et al. Caspa y seborrea (II). El farmacéutico 2003; 293: 65-72 (ref. 5866).
Gemmer CM, et al. Fast, noninvasive method for molecular detection and differentiation of Malassezia yeast
species on human skin and application of the method to dandruff microbiology. Journal of Clinical
Microbiology 2002; 40 (9): 3350-3357 (ref.5975)
Hart, PH et al. Terpinen-4-ol, the main component of the essential oil of Melaleuca alternifolia (tea tree oil),
suppresses inflammatory mediator production by activated human monocytes. Inflammation Research: official
journal of the European Histamine Research Society, 2000. 49(11):619-26.
Hay RJ, et al. Dandruff and seborrhoeic dermatitis: causes and management. Clinical and Experimental
Dermatology 1997; 22: 3-6 (ref. 4108).
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Huber C, Christophers E. « Keratolytic » effect of salicylic acid. Arch. Derm. Res. 1977; 257;293-297 (ref.
6972).
Websites:
http://www.scs.leeds.ac.uk/cgi-bin/pfaf/arr_html?Salix+alba&CAN=COMIND
http://www.ars-grin.gov/cgi-bin/npgs/html/taxon.pl?32674
http://www.ars-grin.gov/cgi-bin/duke/farmacy-scroll3.pl?type=taxon&name=Salix%20alba
http://www.nlm.nih.gov/medlineplus/druginfo/uspdi/202516.html
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