Volume XXVI - Nr.1 - November 2011


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)

Skin of mice untreated (control)

Fig. 1. Skin of mice untreated (control). ATPase reac-tion 5 minutes. At 5 minutes incubation the Stratum Granulosum is not yet evident as is the case of treated skin samples.

Skin of mice treated with Filagrinol

Fig. 2. Skin of mice treated with Filagrinol® for 1 month. ATPase reaction 5 minutes. At the Stratum Granulosum level the presence of lead sulfide granules (the appearance resembles to a necklace of pearls) is highlighted, index of ATPase activity in this site. The overlying Stratum Corneum is colorless.

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)

Normal mouse skin appearance.

Fig.3. Normal mouse skin appearance. Immunohisto-chemical reaction marking a scarce presence of filaggrin.

Mouse tail skin treated with Filagrinol

Fig. 4. Mouse tail skin treated with Filagrinol®. Immunohistochemical reaction marking abundant filaggrin into Stratum Granulosum.

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).


Increase of epidermis water content. Table A.

Days Corneometer
10 13%
30 26%
60 44%

Table A

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%

Table B

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)

Table C

Examples of Formulations
Xalifin-15 ® Emulsifier 20.0
Trioxene-LV ® Citric Ester Eudermic Antilipoperoxidant 5.0
Filagrinol ® Epidermal Powerful Moisturizer 5.0
Undebenzofene-C ® Preservative 1.3
Propylene Glycol Humectant 5.0
Demineralized Water 61.4
Idroramnosan ® Viscosity Modifier 1.0
Siliconed Oil 350 Anti Foam 1.0
Hydroessential Matricaria ® Natural Fragrance 0.3
Total 100.0

Filagrinol ® Epidermal Powerful Moisturizer 10.0
Keratoplast ® Keratoplastic Agent 10.0
Trioxene-LV ® Citric Ester Eudermic Antilipoperoxidant 15.5
Isostearene ® Eudermic Oil 13.0
Undebenzofene-C ® Preservative 0,5
Nesatol ® Eudermic Oil 3.0
Syntesqual ® Eudermic Oil 7.5
Hydroessential Thymus ® Natural Fragrance 0.5
Lipogelag ® Gelling Agent 40.0
Total 100.0



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