Volume XXVI - Nr.1 - November 2011
Filagrinol®
Active Epidermal Moisturization:
Filaggrin Modulator from Fractions of Vegetable Unsaponifiables
What is it?
Filagrinol
® is a clear liposoluble active ingredient, composed of
fractions of vegetable unsaponifiables, modulating filaggrin production, and carrying
out a specific epidermal moisturizing action.
It doesn’t contain any preservative.
Its INCI Name is: Pollen Extract, Glycine Soja (Soybean) Oil Unsaponifiables, Olea
Europaea (Olive) Oil Unsaponifiables, Triticum Vulgare (Wheat) Germ Oil Unsaponifiables.
What is filaggrin?
Filaggrin (FILament AGGRegating proteIN) is an epidermal protein synthesized
in the Stratum Granulosum. It has a key role in the keratinization process:
-
It promotes the organization and aggregation of keratinous protein chains
of the Stratum Corneum;
-
As a consequence of its degradation, it generates a pool of hydro-soluble
molecules which composes the Natural Moisturizing Factor (NMF).
This means integrity and good health of the Stratum Corneum and therefore of
all epidermis.
Which are its applications?
Cosmetic products
- Treatment of dehydrated, sensitive, dry and reddening skin;
- Treatment of skin blemishes and other forms of reddening;
- Treatment of skin aging, sun damages;
- Functional make-up preparations.
Dermopharmaceutical products
- Topic treatment of diskeratosis, parakeratosis and rhagades.
Since Filagrinol® exerts its activity in the upper layers of the skin,
it is recommended to be used in association with Hyaluramine-S®, an active
that carries out a deep and long lasting moisturizing action.
Moisturization of epidermis is efficient only if:
-
Water supplied by dermis is sufficient to balance the skin Perspiratio Insensibilis;
-
Water retention capacity of the upper layers of the skin system is effective
and constant;
Therefore, the correct management of the lipids used in the chosen cosmetic form
is involved too. This management necessarily shall take account of any modifications
of their ratio during the whole process of differentiation and maturation of keratinocytes.
It is also helpful against free radicals as it exerts a strong anti-lipoperoxidant
activity.
How should it be used?
Filagrinol
® should be added to the lipid phase.
The recommended use levels are between 3% and 10%, for the formulation of O/W and
W/O emulsions, lotions, masks, oils and ointments:
- Continuous use: 3% - 5%;
- Shock treatment: 6% - 10%.
How does it work?
Filagrinol
® accomplishes its action on specific metabolic steps of
the epidermal keratinization process.
ATPase [Adenosine TriPhosphatase] Activity
ATPase activity is involved in the maturation process from profilaggrin (precursor)
to filaggrin in epidermis.
The profilaggrin molecules contain ATP. It has been demonstrated that Filagrinol®
increases the ATPase activity. (See Figures 1 and 2)
Immunohistochemical Determination of Filaggrin
Filaggrin is a marker of the final process of keratinization and it states the
proper epithelial maturation.
Using a specific anti-filaggrin antiboby (Dale Method), the effect of Filagrinol®
has been studied by checking the production of filaggrin after topical application.
(See Figures 3 and 4)
Histochemical Determination of Bound Histidine
Profilaggrin and filaggrin are proteins with a high content of histidine. The
intensity of the red-brownish coloration clearly drawing the Stratum Granulosum
is proportional to the presence of Filaggrin (Pauly Method). (See Figures 5 and
6)
Clinical Evaluation
Treatment of 8% Filagrinol® O/W emulsion, applied on 30 volunteers
(40-50 year old women - Double Blind).
Corneometer
Increase of epidermis water content. Table A.
| Days |
Corneometer |
| 10 |
13% |
| 30 |
26% |
| 60 |
44% |
Dermatologist Evaluation
Improvement of skin conditions. (Evaluated Parameters: Skin wrinkling, Moisturization,
Elasticity and Appearance). Table B.
| Days |
Dermatologist Evaluation |
| 10 |
12% |
| 30 |
26% |
| 60 |
42% |
Protective Action Against Lipid Peroxidation Caused by UV Rays [Okawa]
Treatment with a 8% Filagrinol® O/W emulsion. A proportional decrease
in Malondialdehyde production was shown:
- 35.4% - single topical application;
- 49.8% - after 10 days of repeated topical application.
(See Table C).
MALONDIALDEHYDE (nmol / mgprotein)
| Mouse Number |
Vehicle* |
Filagrinol
*
|
Reduction (%) |
|
| 1 |
7.1 |
3.4 |
52.1 |
| 2 |
4.9 |
2.7 |
44.9 |
| 3 |
5.4 |
2.5 |
53.7 |
| 4 |
3.8 |
2.1 |
44.8 |
| 5 |
6.3 |
2.9 |
54.0 |
| 6 |
6.7 |
3.1 |
53.7 |
| 7 |
5.9 |
4.0 |
32.2 |
| 8 |
5.2 |
2.3 |
55.8 |
| 9 |
7.4 |
2.9 |
60.8 |
| 10 |
4.6 |
2.5 |
45.7 |
* Mean of 2 determinations on each sample
**p -value < 0.01 compared to control animals (vehicle only)
|
Examples of Formulations