Development of ‘certified’ organic actives

But what is the “natural”? If we look up “natural” in a dictionary, the definition is: present in or produced by nature, not altered, treated, or disguised: natural colouring; natural produce.

In cosmetics, the “natural” concept should reflect what everyone wants to be. “Natural” is synonymous with authenticity and wellbeing. It can also link to a more exotic approach through plant origins and give consumers a way to “dream” and “escape”.

Last, but not least, a technical and scientific approach to natural cosmetics is based on the simple notion that, in nature, we find everything – and opposites.

We have to isolate molecules from plants in the best conditions, in order to conserve their natural state. This is the principle on which the company’s reputation was built.

Creating a natural active ingredient involves a set of factors including the selection of raw materials by respecting certain specifications (sustainability, ethics, safety etc); and the use of technologies to extract molecules of interest (biochemistry, green chemistry, non-denaturing steps, environmental impact control measures).

The largest worldwide trend in 2008 is to put forward “natural” and/or “organic” personal care products, and Silab has two strategic points to emphasise. Firstly, its ecological and organic range is certified by Ecocert, which is widely recognised internationally. This defines a requirement level guaranteeing the genuine practice of environmental respect throughout the production line, from the raw material (coming from “certified” organic farming) to the finished product. All must be in accordance with the standard of certification: processes, traceability, preservatives, packaging, labelling, transport and storage of ingredients and finished products, hygiene and cleaning of manufacturing and packaging zones, management of energy, discharges and waste. The company is audited twice a year (Fig. 1). Its certified ecological and organic active ingredients are closely scrutinised – more than 99% of the total of ingredients is of natural origin, and more than 99% of the total of ingredients are derived from organic farming as is indicated on labelling. Secondly, the company’s certified ecological and organic range is, as with its other products, safe and effective. It was decided to develop three certified ecological and organic active ingredients which previously had standard ingredient counterparts. The new ingredients, like the previously created ones, have the same efficacy and cover the main cosmetic claims of anti-ageing: immediate tensor effect (certified organic oat extract named OSILIFT BIO), hydrating effect (certified organic white lupin extract named STRUCTURINE BIO), and antiwrinkle effect (certified organic alfalfa extract named VITANOL BIO).

Results

Certified organic oat extract
For several years anti-ageing products have incorporated tensor active ingredients capable of smoothing the skin immediately and visibly. They restore radiance to the skin and lift it. To cover this important market, the company is developing a number of tensor active ingredients. Benefiting from its expertise, and in order to maintain its position in this market, the company has investigated new molecular structures in the form of sugars – little used until now as tensor active ingredients – to put forward a certified organic oat extract. A purified fraction of natural polyoses obtained from oats produced by certified organic farming, the certified organic oat extract has a high molecular weight threedimensional configuration capable of matching skin microrelief perfectly, binding strongly and lastingly, and spreading to form a lifting, cohesive and continuous biological film. The certified organic oat extract thus smoothes and lifts skin microrelief immediately and visibly. The immediate tensor properties of the certified organic oat extract were investigated with instrumental and a sensorial evaluation.

Instrumental assessment
The study was conducted on 18 female volunteers (mean of age 34 ± 9) applying on the forearms the certified organic oat extract formulated at 4% in an emulsified gel and a placebo. Measurements were performed before and 2 hours after a single application of the products using a SEM 575 cutometer (Courage + Khazaka). In the course of the study, the certified organic oat extract produced a statistically significant increase in two parameters characteristic of skin tension: –Uf=+6%; P=0.0396 and –Ue=+7%; P=0.0328.

Sensorial assessment
The sensorial evaluations of the immediate tightening properties of the certified organic oat extract were conducted on a trained panel of 32 women or men (mean of age 31 ± 5). The panel was regularly trained to perceive and quantify the tensor effect of a reference molecule (BSA) formulated at 5%, 10% and 20% on a scoring scale from 0 to 10. The tensor effect was then assessed by the trained panel after a single application on the crow’s feet of the certified organic oat extract formulated in a gel at 4% vs placebo. After the application of the products, 82% of panellists trained to perceive and quantify the sensation of a tensor effect reported feeling a tightening effect (mean score = 4.2) significantly higher (P<0.0001) than the mean effect felt with the placebo (mean score = 2.2) (Fig. 2).

Certified organic white lupin extract
The skin’s outermost layer, the stratum corneum, provides mechanical protection of the body on the macro-scale and a barrier function opposing water loss and penetration by exogenous molecules.2 The stratum corneum is considered as a “brick and mortar” wall. The “bricks” are corneocytes (hard, protective skin cells), while the “mortar” is formed of lipids (a continuous layer that surrounds and protects the corneocytes). This cornified envelope is surrounded mainly by ceramides (47%), cholesterol (24%) and free fatty acids (11%), often linked covalently to precursor proteins. During severe chemical or physical attack on the skin, homeostasis of the barrier function is perturbed. The stratum corneum is no longer replaced properly, and the skin becomes dry and rough. Under these circumstances it is necessary to support and stimulate the process of renewal of the cornified layer. That is the role of the certified organic white lupin extract, a plant active ingredient obtained from the sweet white lupin produced by certified organic farming – it boosts keratinocyte differentiation (data not shown) and strengthens the epidermal reinforcement of the skin by stimulating the synthesis of epidermal lipids for a restructuring and hydrating effect.

Study of the epidermal lipid synthesis
The effect of certified organic white lupin extract on the metabolism of epidermal lipids was investigated on human skin explants using thin layer chromatography (HPTLC). Human skin explants, obtained from an abdominal plasty of a 29-year-old woman, were topically treated with 1% certified organic white lupin extract for 18 h. The neosynthesised radiolabelled lipids were extracted, separated by HPTLC and then quantified with a radioactivity analyser (Storm – Amersham). In comparison with the control, the 1% certified organic white lupin extract increased the newly synthesised epidermal lipids of different classes (Fig. 3). Polar lipids increased by 64%; ceramides by 44%; cholesterol and cholesterol sulfate by 100% and 45% respectively; and cerebrosides by 20%. The active ingredient thus favours the formation of the lipid barrier of the stratum corneum.

Assessment of the skin barrier function
The study investigated the effect vs placebo of the certified organic white lupin extract formulated at 4% in an emulsion on transepidermal water loss (TEWL). Twenty female volunteers (mean of age 39 ± 9) applied the products on the upper arms after washing the skin with sodium lauryl sulfate (SLS) at 10%. Measurements were made using a Tewameter TM 210 (Courage + Khazaka) before and after 14 days of twice-daily treatment.

Compared to the placebo, the 4% certified organic white lupin extract significantly reduced TEWL by 11% after repeated SLS aggression (P=0.0395).

Certified organic alfalfa extract

The ageing process is characterised by major changes in molecular metabolism and cell behaviour. A number of studies have shown a reduction of the proliferative capacity of keratinocytes and fibroblasts resulting from the ageing process. Skin ageing is a biological process which affects particularly the dermis. Indeed, dermal ageing is characterised by changes in the quality, quantity and organisation of the macromolecules of the extracellular matrix.

On one hand, cultured fibroblasts show a decrease in their capacity for synthesis: old fibroblasts synthesise smaller quantities of collagen I than young fibroblasts.3

On the other hand, further studies on the degradation system of collagen have shown that ageing and irradiation accelerate the degradation of the extracellular matrix, demonstrating a decrease in dermal collagen and an increase in the matrix metalloproteinase-1 (MMP-1) expression level, which cleaves interstitial collagen, associated with ageing.4,5

All these changes in the biology of the dermis result in changes detectable on the surface of the skin, affecting its appearance. The skin seems less firm and less elastic, and wrinkles appear, initially around the eyes and elsewhere on the face.

To combat skin ageing, retinol and its derivatives have become indispensable molecules.

There is now a very extensive literature on the in vitro effects of retinol and its derivatives on skin cells and an equally substantial literature on the effects of topical applications of retinoids. Extensively studied, the retinoids have rapidly become benchmark cosmetic ingredients thanks to their high repair capacity, anti-wrinkle effect, lightening effect, etc.

All-trans retinoic acid (tretinoin, vitamin A acid) is the active metabolite of retinol (natural vitamin A). The use of retinol or its analogues in a topical application improves the characteristics of ageing skin – acted on are wrinkles and the texture and colour of the skin. A significant improvement of the general appearance and a dose-dependent effect increasing with treatment duration has been observed.6 These skin surface changes are accompanied by histological changes in both the dermis and the epidermis.7

However, local application of retinoic acid can have strongly irritant side effects. For this reason it cannot be used in cosmetic compositions. Cosmetology laboratories have therefore investigated other compounds in the retinoid family: retinol, retinaldehyde and the ester forms. But the use of retinol in formulation is always compromised by its high level of sensitivity to light, oxygen and heat. Furthermore, retinol also causes irritation at concentrations above 0.1%. The esters have the advantage of being more stable, but penetrate less easily.8,9

To limit the irritation effects induced by retinoids, Silab has developed the certified organic alfalfa extract, rich in galactomannans from alfalfa produced by certified organic farming and showing similar behaviour to retinol on dermal cells. An in vivo study equally showed an anti-wrinkle cosmetic benefit.

Study of the dermal metabolism
The effect of the certified organic alfalfa extract on the synthesis of MMP-1 and collagen I was conducted on normal human fibroblasts with Elisa Assay. Tested at 0.25%, 0.50% and 1% for 48 h on normal human fibroblasts, the certified organic alfalfa extract inhibited synthesis of MMP-1 induced by UVA radiation (Biosun UV lamp, Vilber- Lourmat) by respectively 50%, 59% and 85%. A comparable effect was obtained with 10-5M Retinol (–63%). Moreover tested at 0.05%, 0.1% and 0.25% for 24 h, it also led to a significant and dose-dependent stimulation of collagen I synthesis by respectively 80%, 158% and 201% (Fig. 4). This effect was comparable to that obtained with 10-5M retinol which increased collagen I synthesis by 160%. The certified organic alfalfa extract thus protects the dermal matrix by stimulating the synthesis of one of the major components, collagen I, as well as by limiting ECM degradation by MMPs.

Assessment of the anti-wrinkle properties
The anti-wrinkle properties of the certified organic alfalfa extract formulated at 4% in an emulsion were evaluated vs placebo on the crow’s feet of 21 female volunteers (mean of age 54 ± 9) by profilometry using Quantirides 99 (Monaderm) software. Profile photos of each side of the face were also taken with Visia-CR (Canfield) equipment. After 28 days of twice-daily applications and in comparison with the placebo, the certified organic alfalfa extract significantly reduced the number of wrinkles by 19% (P=0.0023); the total wrinkled surface by 26% (P=0.0060); and the total length of wrinkles by 22% (P=0.0045). The reduction of the number of wrinkles was observed in 80% of the volunteers.

Images obtained before and after treatment (Fig. 5) illustrate the antiwrinkle efficacy of the certified organic alfalfa extract.

Conclusion

There is no formal definition of natural cosmetics or natural active ingredients and this lack of clarity on what natural/organic means may be confusing. In this article, we have presented the Silab approach to “naturals”, from the selection of the raw material to the finished product. Thanks to experience gained over more than 20 years in this field, we developed a certified ecological and organic range composed, at this moment, of three actives ingredients with the same level of efficacy as standard ingredients. Being organic does not mean to be less efficient. The new active ingredients cover major anti-ageing skin care factors: immediate tensor effect (with certified organic oat extract named OSILIFT BIO), hydrating effect (with certified organic white lupin extract named STRUCTURINE BIO) and antiwrinkle effect (with certified organic alfalfa extract VITANOL BIO).

These certified organic active ingredients are useful when the following claim is made: “The formula contains certified organic active ingredients”. This is a key point – the ingredients impact on the calculation of organic requirements. Silab is keen to demonstrate the integrity, clarity, transparency and credibility it achieves in its approach to the term “organic”. It has shown, for a long time, these qualities in its approach to the term “natural”.

References

1 Euromonitor International Cosmetics and Toiletries 2008 and Beyond – A Global Perspective. Izaskun Bengoechea, Senior FMCG Analyst – In Cosmetics 2008 – Amsterdam.

2 Rawlings A.V, Matts P.J. Stratum corneum moisturization at the molecular level: an update in relation to the dry skin cycle. J Invest Dermatol. 2005 Jun; 124 (6): 1099-110. Review.

3 Varani J., Fisher G.J., Sewon K., Voorhees J.J. Molecular mechanisms of intrinsic skin aging and retinoid-induced repair and reversal. J Investig Dermatol Symp Proc, 3, 57-60 (1998).

4 Fligiel et al., 2003. Fligiel S.E., Varani J., Datta S.C., Kang S., Fisher G.J., Voorhees J.J. Collagen degradation in aged/photodamaged skin in vivo and after exposure to matrix metalloproteinase-1 in vitro. J. Invest. Dermatol. 120 (2003), pp. 842–848.

5 Jenkins, 2002. Jenkins G. Molecular mechanisms of skin ageing, Mech. Ageing Dev. 123 (2002), pp. 801–810.

6 Yaar M., Gilchrest B.A. Skin aging: postulated mechanisms and consequent changes in structure and function. Clin Geriatr Med, 17, 4, 617-630 (2001).

7 Varani J., Mitra R.S., Gibbs D., Phan S.H., Dixit V.M., Mitra R., Wang T., Siebert K.J., Nickoloff B.J., Voorhees J.J. All-trans retinoic acid stimulates growth and extracellular matrix production in growth-inhibited cultured human skin fibroblasts. J Invest Dermatol, 94, 717- 723 (1990).

8 Kafi R., Kwak H.S., Schumacher W.E., Cho S., Hanft V.N., Hamilton T.A., King A.L., Neal J.D., Varani J., Fisher G.J., Voorhees J.J, Kang S. Improvement of naturally aged skin with vitamin A (retinol). Arch Dermatol. 2007 May; 143 (5): 606-12.

9 Chavigny C. Retinol and derivatives: irreplaceable anti-wrinkles agents. Parfums Cosmétiques Actualités, 154, 89-104 (2000).