FIELD OF THE INVENTION

[001 ] The present invention relates to a cosmetic skin anti-aging composition. The invention particularly relates to a composition combined of skin anti-aging agents.

BACKGROUND OF THE INVENTION

[002] The skin is the outer coverage of the body. As skin ages, it becomes thinner and is more easily damaged. Intensifying this effect is the decreasing ability of the skin to heal itself as a person ages. Among other things, skin aging is noted by a decrease in volume and elasticity. There are many internal and external causes to skin aging. For example, aging skin receives less blood flow and lower glandular activity. Clinical findings of skin aging are categorized as laxity (sagging), rhytids (wrinkles), and the various facets of photoaging, including erythema/telangiectasia (redness), dyspigmentation (brown discoloration), solar elastosis (yellowing), keratoses (abnormal growths) and poor texture.

[003] Cosmetics are care substances used to enhance the appearance of skin or odor of the human body. Cosmetics are generally composed of mixtures of chemical compounds, some being derived from natural sources, others being synthetic. The United States Food and Drug Administration (FDA) defines cosmetics as "intended to be applied to the human body for cleansing, beautifying, promoting attractiveness, or altering the appearance without affecting the body's structure or functions." [004] Cosmetic skin care products are used in general to improve the appearance and health of the skin, formulated for different types of skin and associated tissues. Skin care products include cleansers, facial masks, toners, moisturizers, sunscreens, and also tanning oils and lotions, skin lighteners, serums and exfoliants, including skin anti-aging agents.

[005] Skin anti-aging agents are products that typically include powdered supplements, skin creams, vitamins, and facial masks. They are designed to reduce or diminish the effects of aging. Many products seek to hide the effects of aging while others claim to alter the body's chemical balances to slow the physical effects of aging.

Niacinamide

[006] Niacinamide, also known as nicotinamide, is the amide of nicotinic acid (vitamin B ₃ or niacin). Niacinamide is a water-soluble vitamin and is part of the vitamin B group. In cells, nicotinic acid is converted to niacinamide, which is incorporated into nicotinamide adenine dinucleotide (NAD ⁺ ) and nicotinamide adenine dinucleotide phosphate (NADP ⁺ ), or their reduced forms NADH and NADPH, respectively. NADH and NADPH constitute coenzymes in a wide variety of enzymatic oxidation-reduction reactions, including enzymes involved in the production of cellular energy and lipids that are involved in cell growth. With a sufficient supply of NADH and NADPH the skin creates an effective barrier to external factors that influence the aging process. However, the levels of both NADH and NADPH decline with aging. Thus, topical application of niacinamide reduces the rate of decline of NADH and NADPH. Since topical application of niacinamide can help to preserve the level of NADH and NADPH, it contributes to the support of the skin's barrier against pollutants and other irritants. As a result, many skin conditions, such as acne, the redness associated with rosacea (adult acne), and other inflammatory conditions can be actively managed by topical application of niacinamide or its derivatives, e.g. N- nicotinoyl dopamine. Niacinamide has been also shown to be useful for encouraging production of natural emollients that can help the skin remain hydrated, and it is also reported to be an effective skin whitener in topical application. In addition, it has been shown that topical application of niacinamide provides a broad array of additional improvements in the appearance of aging facial skin, including reductions in fine lines and wrinkles, hyperpigmented spots, red blotchiness and skin shallowness. In addition, elasticity of the skin was also improved following topical application of niacinamide.

[007] Niacinamide is a substance found in cosmetics as a skin lightening and/or moisturizing agent. Cosmetic compositions with niacinamide have been reported in various publications including United States Patents 5,833,998; 5,939,082; 5,962,482; 5,968,528; 5,980,921 ; 5,997,890; 5,997,887; 6,024,942; 6,183,761 ; 6,224,888; and 6,309,657.

Coenzyme Q10

[008] Coenzyme Q10, also known as ubiquinone, is an oil-soluble substance that is present in most eukaryotic cells, primarily in the mitochondria. Coenzyme Q10 can be synthesized in all tissues but at a low level. Several functional properties have been attributed to coenzyme Q10, including function as a cofactor for different enzymes mainly in mitochondria, electron- and proton- carrier in the respiratory chain, antioxidant and radical scavenger, and having a role in the control of membrane dynamics. The production and uptake of coenzyme Q10 is sufficient under normal conditions. However, supplementation may be necessary in several conditions, including advanced age (above 40 years), high physical exercise, stress, impaired immune system and mitochondrial disease.

[009] There are several beneficial effects provided by topical application of coenzyme Q10, including but not limited to, protection against photo aging; increase of antioxidant status; reduction of wrinkles; increase of epidermal turnover; alternative to retinoic acid treatment; increase of glycosaminoglycan in fibroblasts; reduction of collagenase expression induced by ultra violet A irradiation in fibroblasts; reduction of ultra weak photon emission after ultra violet A irradiation; and reduction of wrinkle depth.

[010] Coenzyme Q10 is an orange coloured oil-soluble powder. It has been found that administration of coenzyme Q10 in powder form in capsules shows poor bioavailability. However, encapsulation of coenzyme Q10 into nanoparticles results in a water-dispersible form, when a particle size of 50 nanometers results in transparent oil/water nanoemulsions, with improved bioavailability in oral and topical applications, mainly through improved penetration of the conenzyme Q10 nanoemulsions into the skin. Thus, encapsulation of coenzyme Q10 into nanoparticles stronly increases the beneficial effects of topical application of coenzyme Q10.

[01 1 ] Coenzyme Q10 is a substance found in cosmetics as an agent for the treatment of the signs of skin aging. Cosmetic compositions with coenzyme Q10 have been reported, for example in WIPO Patent Application WO/2008/047882; United States Patent Application 2005/0271692; European Patent Application 1243252; and United States Patent 6,906,106.

Caprylic/capric triglyceride and geranylgeranylpropanol composition [012] Caprylic/capric triglyceride and geranylgeranylpropanol comprise a composition manufactured by Sederma, France, and having the trade name Juvinity™. Caprylic/capric triglyceride is a mixed ester composed of caprylic and capric fatty acids, extracted from coconut oil, and considered a good emollient and thickening agent in cosmetics. Geranylgeranylpropanol is a derivative of isoprene - a complex lipid the includes in particular a geranylgeranyl polyterpenic chain, likely to treat disorders of the outmost layer of skin, via an inhibitory activity of the formation of desmosomes (cell structures specialized for cell-to-cell adhesion) in the epidermis. According to experimental results published by Sederma, France, Juvinity™ delays both nucleus and metabolic senescence; limits oxidative stress and telomer shortening to ensure optimal replication as a young cell; rebalances mitochondrial activity; promotes adenosine triphosphate synthesis; protects the cytoskeleton; reactivates the extracellular matrix; helps reducing visible signs of aging on the face, neck and shoulders; and recharges the skin with long-life youth.

[013] A composition including caprylic/capric triglyceride and geranylgeranylpropanol can be used in cosmetics as an agent for the treatment of wrinkles, fine lines and visible discontinuities of skin, and for treating pigmentation disorders. Cosmetic compositions with a composition including caprylic/capric triglyceride and geranylgeranylpropanol have been reported, for example WIPO Patent Application WO 201 1/125039 and Japanese Patent 10167957

Lepidium sativum sprout extract

[014] Lepidium sativum (garden cress) sprout extract is manufactured by homogenization and extraction of fresh Lepidium sativum sprouts with water. The extract is then purified, concentrated and encapsulated into liposomes. The active compound of the Lepidium sativum sprout extract is sulforaphane, which activates the body's detoxification system. Lepidium sativum sprout extract has been found to stimulate the expression of antioxidants and detoxification enzymes in the skin to protect againd environmental pollutants (e.g. cigarette smoke, exhaust fumes, smog, endotoxins and heavy metals), extrinsic and intrinsic reactive oxygen species, and DNA damage, causing premature skin aging.

[015] Lepidium sativum extract is a substance found in cosmetics as an agent for skin whitening. A cosmetic composition with Lepidium sativum extract has been reported, for example in Korean Patent 201 1 1083028.

Gold particles

[016] Throughout history gold has been recognized for its luxurious and beautifying properties. In ancient Chinese medicine gold was a key to youth, as queens used a gold massage roller on their face every day. These gold facials were also used in ancient Indian culture and are said to firm the skin, give it a glow and reduce wrinkles. Under the action of gold a higher amount of blood is brought in the area, speeding up cellular processes and activating regeneration. Moreover, gold action is closely connected with the ions present in the cells that are sensitive to electric charges; these ions will become active under the influence of gold and recreate broken cellular connections. That way the appearance of fine lines and wrinkles is diminished with each treatment. In terms of benefits within the deep cellular levels, gold is well reputed for restoring the lost elasticity properties of the tissues. Gold slows down collagen depletion and the breakdown of elastin to prevent sagging skin. It stimulates cellular growth of the basal layer to regenerate healthy, firm skin cells and provides a tightening effect. Gold reduces the appearance of sun damage and age spots. Gold has also been successfully used to treat rheumatoid arthritis by reducing inflammation. Anti-inflammatory properties of gold also decrease skin inflammation, thereby slowing down melanin secretion and reducing age spots. Gold is also well known for its anti-aging qualities and thought to have numerous healing benefits that have been used for centuries by the oriental cultures. Gold can also be used as a preventive treatment in order to maintain a healthy young and radiant looking skin. In addition, gold has anti-pathogenic properties.

[017] Gold as a substance is found in cosmetics as a glittering agent and/or as an agent providing soft focus effects. Cosmetic compositions with gold have been reported in various publications including United States Patent 2,1 1 1 ,912; European Patent 2283804, German Patent 19625560; and United States Patent Application 2003/0019501 .

[018] None of the prior art teaches a synergistic cosmetic skin anti-aging composition including niacinamide or derivative thereof, coenzyme Q10 or derivative thereof, a composition of caprylic/capric triglyceride and geranylgeranylpropanol, Lepidium sativum sprout extract and gold to obtain improved anti-aging of the skin.

SUMMARY OF THE INVENTION

[019] It is an object of the present invention to provide a synergistic cosmetic skin anti-aging composition including niacinamide or derivative thereof, coenzyme Q10 or derivative thereof, a composition of caprylic/capric triglyceride and geranylgeranylpropanol, Lepidium sativum sprout extract and gold that can improve anti-aging of the skin significantly. [020] The present invention relates to a skin anti-aging composition in which several skin anti-aging agents are advantageously combined for obtaining improved skin anti-aging.

[021 ] In accordance with embodiments of the present invention there is provided a synergistic skin anti-aging composition including: i) from 0.2 to 10.0% by weight niacinamide or derivative thereof; ii) from 0.01 to 2.00% by weight coenzyme Q10 or derivative thereof; iii) from 0.2 to 5.0% by weight composition including a combination of caprylic/capric triglyceride and geranylgeranylpropanol; iv) from 0.01 to 1 .00% by weight Lepidium sativum sprout extract, and v) from 0.0001 to 1 .0000% by weight gold particles.

DESCRIPTION OF EMBODIMENTS OF THE INVENTION

[022] Illustrative embodiments of the invention are described below. In the interest of clarity, not all features/components of an actual implementation are necessarily described.

[023] A component of the skin anti-aging composition is niacinamide, also known as vitamin B ₃ . Exemplary derivatives of niacinamide compounds, as described for example in United States Patent 7,332,152, include nicotinic acid esters - including non-vasodilating esters of nicotinic acid, nicotinyl amino acids, nicotinyl alcohol esters of carboxylic acids, nicotinic acid N-oxide and niacinamide N-oxide.

[024] Niacinamide is used preferably as a solid powder and is incorporated at a ratio of 0.2 to 10.0% by weight of the skin anti-aging composition. Niacinamide is available from a variety of pharmaceutical houses, for example Royal DSM, The Netherlands. [025] Another component of the skin anti-aging composition is coenzyme Q10, also known as ubiquinone. An exemplary derivative of coenzyme Q10, or a salt thereof, is described for example in United States Patent Application 2010/0074879. The coenzyme Q10 derivative is represented

(1)

by the formula (1 ):

wherein R ¹ and R ² are jp, at least one of R ¹ and R ² is a ph je of 1 to 9.

[026] Coenzym der and is incorporated at a ratio of 0.01 to 2.00% by weight of the agent. Coenzyme Q10 is available from a variety of pharmaceutical houses, for example Mibelle Biochemistry, Switzerland.

[027] A composition of caprylic/capric triglyceride and geranylgeranylpropanol is used preferably as a liquid, and is manufactured for example by Sederma, France under the trade name Juvinity™. A detailed description of a composition of caprylic/capric triglyceride and geranylgeranylpropanol can be found for example in WIPO Patent Application WO 201 1 /125039 - between page 6, line 22 and page 12, line 17. The composition of caprylic/capric triglyceride and geranylgeranylpropanol is incorporated at a ratio of 0.2 to 5.0% by weight of the skin anti-aging composition.

[028] Lepidium sativum sprout extract is used preferably as a liquid.

This extract is manufactured for example by Mibelle Biochemistry, Switzerland, under the trade name Detoxophane, and is incorporated at a ratio of 0.01 to 1 .00% by weight of the skin anti-aging composition. [029] As described for example in WIPO Patent Application WO

201 1/018258, gold particles are available commercially in various dimensions and shapes. They may be spherical, platelet shaped, flake shaped, or irregularly formed. In the context of the present invention the flake form is most useful. Average particle size may vary from the nanometer to the millimeter range. The purity of the gold particles may be 24 karat, or it may be alloyed with other metals such as tin, copper, nickel, titanium, silver or any combinations thereof (e.g. 22 karat). The above described gold particles may also be made of compounds of gold rather than the elemental metal, for example gold chloride, gold sulphate, gold nitrate, gold phosphate, gold borate or organo gold complexes. An embodiment of the skin anti-aging composition of the present invention includes 24 karat elemental gold flakes having an upper size limit of 2.5 millimeters. Such product is available for example from J.G. Eytzinger GmbH, Germany, under the trade name GoldCosmetica Gold 999 Flake No 5, which is incorporated in the skin anti-aging composition at a ratio of 0.0001 to 1 .0000% by weight of the composition.

[030] NIAPEPTYGOLD™ is a trade name given to the synergistic skin anti-aging composition of the present invention, including: i) from 0.2 to 10.0% by weight niacinamide or derivative thereof; ii) from 0.01 to 2.00% by weight coenzyme Q10 or derivative thereof; iii) from 0.2 to 5.0% by weight composition including a combination of caprylic/capric triglyceride and geranylgeranylpropanol; iv) from 0.01 to 1 .00% by weight Lepidium sativum sprout extract, and v) from 0.0001 to 1 .0000% by weight gold particles.

[031 ] An example of a formulation of the synergistic skin anti-aging composition of the present invention is given in Table 1 . [032] NIAPEPTYGOLD ^{I M} includes totally a ratio of 6.45% by weight of the composition given in Table 1 . The components of NIAPEPTYGOLD™ are given in Table 2.

Table 1 : Formulation of a synergistic skin anti-aging composition.

Anthemis Nobilis (Chamomile) Flower Extract 0.10% skin calmer

Fragrance 0.10% perfume

Stearic Acid 0.10% fragrance; surfactant - cleansing & emulsifying agent

Simmondsia Chinensis (Jojoba) Seed Oil 0.10% skin conditioner

Triethylene Glycol 0.10% preservative

Allantoin 0.08% skin conditioner; skin protectant

Oenothera Biennis (Evening Primrose) Oil 0.08% skin conditioner

Rosa Canina Fruit Oil 0.08% skin conditioner

Algae (Dunaliella) Extract 0.06% humectant

Camellia Sinensis Leaf Extract 0.06% antioxidant; fragrance; skin conditioner; ultraviolet light absorber

Macadamia Ternifolia Oil 0.05% skin conditioner

Tocopheryl Acetate (Vitamin E) 0.04% antioxidant; skin conditioner

Hyaluronic Acid 0.03% skin conditioner; viscosity increasing agent

Table 2: Formulation of NIAPEPTYGOLD

Synergistic effect

[033] In order to evaluate the skin anti-aging effect of the skin anti-aging composition given in Table 1 , compositions were manufactured, in which each composition contained only one component (out of the five components described in Table 2) in a respective concentration, namely: 2.80% niacinamide; 1 .00% coenzyme Q10; 2.00% Juvinity™; 0.15% Lepidium sativum sprout extract; or 0.50% 24 karat gold flakes.

[034] A blind test was conducted with 30 women volunteers in the ages

30-50, which were separated to six groups of five individuals each. The volunteers of each group treated their facial skin with a different composition including either 2.80% niacinamide; 1 .00% coenzyme Q10; 2.00% Juvinity ; 0.15% Lepidium sativum sprout extract; 0.50% 24 karat gold flakes; or 6.45% NIAPEPTYGOLD™. Each volunteer was asked to rank the effect of the composition, in a range between 1 (lowest effect) and 5 (highest effect), on the following criteria of skin anti-aging: improvement of skin moisture, depth of skin wrinkles, skin tightening, skin texture uniformity and skin elasticity. Average ranks for each composition are given in Table 3.

Table 3: Average ranks of the effect of separate components of the skin anti- aging composition of the present invention on anti-aging criteria, compared to the effect of the skin anti-aging composition - NIAPEPTYGOLD™.

As can be seen in Table 3, volunteers who treated their facial skin with NIAPEPTYGOLD™ rated its effect vis-a-vis the five anti-aging criteria in substantially higher ranks than the effect of each component separately, thus emphasizing the synergistic skin anti-aging effect of the skin anti-aging composition of the present invention. [035] It should be understood that the above description is merely exemplary and that there are various embodiments of the present invention that may be devised, mutatis mutandis, and that the features described in the above- described embodiments, and those not described herein, may be used separately or in any suitable combination; and the invention can be devised in accordance with embodiments not necessarily described above.