Hair loss abstract
A preparation for topical use containing benzyl nicotinate and
having the function of combating and/or delaying hair loss, whose
composition comprises:--two amino acids, hydroxyproline and aspartic
acid, complexed with a silanol,--an enzyme activator, comprising
octyl butyrate is described.
Hair loss claims
1. Preparation for topical use containing benzyl nicotinate and
having the function of combating and/or delaying hair loss, characterised
in that its composition comprises: two amino acids, hydroxyproline
and aspartic acid, complexed with a silanol, an enzyme activator,
comprising octyl butyrate.
2. Preparation according to claim 1, the composition of which also
includes glutamine peptides.
3. Preparation according to claim 1, the composition in which also
comprises pantenol.
4. Preparation according to claim 3, characterised in that its
composition comprises: a) octyl butyrate in an amount between 0.001
and 0.2% by weight, b) glutamine peptides in an amount between 0.001
and 0.2% by weight, c) monomethylsilanol-hydroxyproline aspartate
in an amount between 0.001 and 0.5% by weight, d) benzyl nicotinate
in an amount between 0.05 and 0.15% by weight, e) pantenol in an
amount between 0.05 and 0.5% by weight.
5. Preparation according to claim 4, in which a liquid vehicle,
one or more perfumed substances and preservatives are added.
6. Preparation according to claim 5, to which ethyl alcohol, water,
menthol and preservatives are added.
7. Preparation according to claim 2, the composition in which also
comprises pantenol.
Hair loss description
[0001] This invention relates to the field of preparations for
topical use used to combat and/or delay hair loss.
[0002] Hair loss represents detachment of the hair from the follicle
and is a physiological phenomenon which forms part of the normal
cyclical reproduction of hair.
[0003] On average physiological hair loss does not exceed 50-80
hairs per day. If the number of hairs lost is greater than this
average then this constitutes anomalous hair loss.
[0004] Hair loss is a phenomenon causing extreme anxiety, for which
remedies are sought through the use of products to prevent it.
[0005] This is the background to this invention; it relates in
fact to a preparation for topical use, for cosmetic use, which is
capable of combating hair loss through of its action targeted on
the hair follicle, that is the structure which contains the root
of the hair. The original feature of the preparation comprises its
method of action which: 1) helps to promote the elasticisation of
the follicle walls, 2) increases the anchoring of the hair root
in the follicle, to hold it in place and prevent detachment.
[0006] In hair distinction is made between the shaft of the hair,
or the free part, which projects from the external surface of the
skin, and the root, which is implanted in the skin and held in the
follicle. The deepest part of the root is called the bulb of the
hair.
[0007] The hair therefore grows within an invagination in the epidermis
of the skin, or the follicle, which therefore comprises an epidermal
part and an external part which is continuous with the dermis. The
hair follicle wall is therefore formed externally of a layer of
connective tissue and internally of an epithelial layer.
[0008] From the outside inwards the follicle during anagen therefore
comprises the following structures: connective tissue sheath, outer
epithelial sheath, inner epithelial sheath.
[0009] The connective tissue sheath surrounds the follicle throughout
its entire length continuing below into the connective tissue of
the dermal papilla. Damage to the sheath may prevent a follicle
engaging in normal anagen.
[0010] The connective tissue sheath is formed by a thickening of
the connective tissue in which it is possible to distinguish, depending
upon the orientation, collagen fibres and elastic fibres, an outer
layer, an inner layer and a vitreous layer in contact with the cells
of the follicle's epidermis.
[0011] The outer epithelial sheath continues the skin's epidermis
and extends from the mouth of the follicle, that is from the point
where the hair emerges, to the bulb, where it continues within the
matrix. In the upper portion it has a structure similar to that
of the epidermis; further down it is only formed by the basal and
spinous layers. The follicle epidermis with the spinous layer is
therefore in contact with the outermost layer of the sheath of the
root (Henle's layer).
[0012] The inner epithelial sheath surrounds and covers the hair
root as far as the mouth of the follicle, where it disintegrates
and is removed. From the outside inwards it comprises three layers:
Henle's layer (in contact with the epidermis of the follicles),
Huxley's layer and the cuticle which adheres closely to the cuticle
of the hair. The inner epithelial sheath can be regarded as being
similar to the granular and lucid layers of the epidermis. Given
the structural complexity of follicles it is obvious that satisfactory
functioning of the biological components which are directly or indirectly
involved in the follicle's structure is fundamental in order to
hold the root within the follicle and to allow the hair to experience
a correct life cycle, that of growth, involution and rest prior
to falling out.
[0013] Transglutaminases are enzymes which are found in many cell
compartments. The intermolecular cross-linking catalysed by transglutaminases
is of extreme importance in the keratinisation of the epidermis
and hairs.
[0014] Epidermal transglutaminases are located in the granular
layer, where they have an important part to play; they stabilise
the bond between lysine and glutamine residues in order to form
bridges between different structural proteins. This protein-protein
link is necessary to form the corneocytes' enclosure during the
process of keratinisation. The glutamyl-lysine links represent an
important marker for normal differentiation of the epidermis. In
fact many of the characteristics attributed to these tissues, such
as strength, stability and impermeability, are due in part to the
presence of transglutaminases.
[0015] Follicular transglutaminases are located in the inner sheath
of the root. These enzymes help through forming links between structural
proteins, and consequent cross-linking, increasing the strength
of the hair, especially at the base, where it is attached to the
scalp. Disturbances in the formation of these cross-links may result
in hairs having diminished cohesion or tensile strength.
[0016] Because qualitative and quantitative damage to collagen
and elastic fibres (fundamental components of the connective tissue)
due to causes of various natures has an effect on the elasticity
of the tissues, it is important to maintain the nutrition of the
epidermal and connective tissue structures present in the sheaths
forming the follicle and the tissues receiving and surrounding the
follicle in the scalp. Cross-linking of the protein structures which
helps to secure the root in the follicle through the formation of
glutamyl-lysine bonds during the process of keratinisation which
takes place in the sheaths is also important.
[0017] Disturbance or damage to these configurations may bring
about major structural changes and diminished cohesion between the
root and the follicle.
[0018] The preparation to which the invention relates is designed
to slow down hair loss through the synergistic action of its functional
components.
[0019] From a formulative point of view the invention makes use
of all the known loss-preventing potential of a vasodilator, benzyl
nicotinate, (which is fundamental to action to combat hair loss
in that by locally increasing the blood flow it provides an adequate
input of nutrient substances and oxygen to the hair) included in
a water-alcohol vehicle enriched with pantenol and menthol.
[0020] However the original feature of the invention lies in its
method of action and above all in the target of the action to combat
hair loss, which is specifically the hair follicle. This action
takes the following forms:
[0021] it encourages elasticisation of the follicle walls in order
to prevent them from hardening, thanks to the presence of two amino
acids, hydroxyproline and aspartic acid, which maintain the function
of the connective tissue structure surrounding and supporting the
follicle,
[0022] it helps to anchor the hair root in the follicle by holding
it in its seat, delaying detachment and therefore loss thanks to
the presence of an enzyme activator which acts on the transglutaminases.
[0023] It is known that skin damage is the result of exogenous
and endogenous factors which are specific to each individual. Some
harmful exogenous factors are UV rays, free radicals, ageing.
[0024] Cell activity as a whole decreases, causing qualitative
and quantitative damage to the collagen and elastic fibres. Tissue
regeneration decreases and hardening of the tissues occurs through
damage to the cellular components making up the connective tissue
which prevents sclerosis. All this is reflected in a diminution
of the elasticity of the skin.
[0025] The two amino acids hydroxyproline and aspartic acid, included
in a silanol, monomethylsilanol-hydroxyproline aspartate (silanols
are organic derivatives of silicon, very rich in hydroxyl groups
and synthesised in the presence of different radicals which give
them stability and specificity), have a cytostimulant effect. They
in fact encourage the process of cell division in the fibroblasts.
The fibroblasts present in the dermis synthesise collagen, elastin
and components of the extracellular matrix; an increase in their
number may result in greater synthesis of these molecules.
[0026] It can therefore be said that hydroxyproline and aspartic
acid when complexed in a silanol can contribute to improving and
normalising the connective tissue structures restoring elasticity
to skin tissues.
[0027] The inventors have considered it important to apply this
action to the scalp by selecting monomethyl silanol-hydroxyproline
aspartate as one of the active ingredients of the preparation according
to the invention. As previously described, hair follicles are derived
from an invagination in the skin and comprise an epidermal part
and a connective tissue part in continuity with the dermis of the
skin itself. This is the seat of action of the two amino acids,
hydroxyproline and aspartic acid, which form part of the complex
with the silanol.
[0028] Its purpose is to limit hardening of the tissues encouraging
elasticisation of the follicle walls. In this way follicles are
helped to maintain optimum physiological conditions for holding
the hairs which they contain in their seats.
[0029] The cell-stimulating action of the complex of amino acids
with silanol has been tested on human fibroblast cultures. The increase
in cell growth was 46% when that active ingredient was present in
the culture medium.
[0030] It is also pointed out that silicon, as a component of the
complex described above, is an essential element in the mucopolysaccharide-protein
complexes of connective tissue. Acting as a cross-linking agent,
silicon can contribute to the structural integrity of the connective
tissue which comes in contact with the hair bulb.
[0031] The inventors then identified octyl butyrate as the so-called
enzyme activator, that is the molecule capable of stimulating the
activity of transglutaminases in the cells of the scalp in order
to help increase the anchoring of hairs at their attachment sites.
[0032] The choice of octyl butyrate came from the observation that
some molecules are capable of inducing transglutaminase synthesis;
this led the researchers to investigate the case of sodium butyrate.
This substance is capable of stimulating the synthesis of transglutaminases
in keratinocytes and formation of the corneified enclosure of the
corneocytes (keratinocytes in the final stage of differentiation).
[0033] Being a substance which cannot be used in cosmetics because
of its bad smell, its effects have been reproduced by an ester of
butyric acid, octyl butyrate, an ester of octanol and butyric acid,
which is then hydrolysed by skin enzymes such as esterases.
[0034] The role of octyl butyrate, the enzyme activator in the
invention in question, is that of stimulating the activity of transglutaminases
in the cells of the scalp in order to help increase the anchoring
of hairs to their sites of attachment.
[0035] Peptides rich in glutamine, derived from cereals, enrich
the preparation to which the invention relates and contribute synergistically
to the activity of the octyl butyrate. They in fact represent an
excellent substrate for transglutaminases.
[0036] An additional comment concerning the above glutamine peptides:
the amino acid glutamine is regarded as being the "fuel"
of cell emergence, both when glucose is deficient and when the cells
are in a stage of strong growth and multiplication. This is the
situation of the hair follicle cells during the anagen phase. The
glutamine peptides therefore support the octyl butyrate in the preparation
in question by acting as an energy supplement for the cells which
are undergoing strong multiplication.
[0037] With the specific object of evaluating the hair loss-combating
activities of this specific active ingredient a self-assessment
trial was performed on 20 volunteers for three months against placebo,
which revealed the following:
[0038] in the case of the treated group:
[0039] before treatment most of the volunteers had visible alopecia.
The amount of hair loss was great in 22%, average in 67% and small
in 11%.
[0040] After 3 months treatment with the lotion containing enzyme
activator 67% of the volunteers observed a decrease in hair loss.
[0041] in the case of the placebo group:
[0042] 77% of the volunteers had visible alopecia. The amount of
hair loss was average for 66% and small for 33%.
[0043] After 3 months use of the placebo lotion the amount of hair
loss appeared to be unchanged. No visible improvements were observed.
[0044] The hair loss-combating effectiveness of the preparation
in its entire formulation was tested through a clinical trial conducted
by a specialised institute. 20 volunteers of the male and female
sex having telogen effluvium problems were selected for the purpose
and used the preparation once a day on alternate days for 60 consecutive
days.
[0045] At the start of the test, after 1 month's treatment, and
after 60 days of use, the degree of resistance to traction was clinically
evaluated by the Pull test and hairs lost after washing of the scalp
under controlled conditions were counted (Wash test).
[0046] An objective examination of the condition of the scalp,
a subjective evaluation of effectiveness by the volunteers and a
psychological evaluation relating to satisfaction were also performed.
[0047] Analysis of the results revealed:
[0048] a statistically significant increase in resistance to traction
both after 30 days and after 60 days application of the-preparation
[0049] a statistically significant decrease in the number of hairs
lost during washing both after 30 days and after 60 days of application
of the preparation
[0050] from the subjective point of view the volunteers observed
a decrease in the fall-out of hairs as well as a decrease in the
level of seborrhoea.
[0051] The subject matter of this invention therefore comprises
a preparation as described in appended claim 1.
[0052] A description of a preferred embodiment of the preparation
according to the invention in which all the components and active
ingredients described previously are present will now be provided.
[0053] The composition of this embodiment comprises:
[0054] between 0.001 and 0.2% by weight of octyl butyrate,
[0055] between 0.001 and 0.2% by weight of glutamine peptides,
[0056] between 0.001 and 0.5% by weight of monomethylsilanol-hydroxyproline
aspartate,
[0057] between 0.05% and 0.15% by weight of benzyl nicotinate,
[0058] between 0.05% and 0.5% by weight of pantenol.
[0059] A liquid vehicle, for example ethyl alcohol and water, one
or more perfumed essences, such as menthol and the like, and preservatives
are added to this composition. The preparation may find specific
indication for different stages of severity of hair loss using increasing
percentages of the active ingredients (octyl butyrate, glutamine
peptides, monomethylsilanol-hydroxyproline aspartate, benzyl nicotinate)
in proportion to the increased intensity of hair loss. |