WO2001012151A1

WO2001012151A1 - Skin care product

Info

Publication number: WO2001012151A1
Application number: PCT/GB2000/003083
Authority: WO
Inventors: Paul Rodney Clayton
Original assignee: Individual
Current assignee: Individual
Priority date: 1999-08-12
Filing date: 2000-08-10
Publication date: 2001-02-22
Anticipated expiration: 2002-02-12
Also published as: GB9919079D0; GB0019702D0; EP1207847A1; AU6458700A; GB2355193A

Abstract

Skin care products are disclosed for reducing, delaying or preventing skin ageing. The products comprise oral and topical formulations and contain at least one inhibitor of catabolism of the extracellular matrix and at least one anabolic or pro-anabolic factor for the extracellular matrix.

Description

SKIN CARE PRODUCT

This invention relates to a skin care product. At least some embodiments provide skin care products for delaying or preventing skin ageing. At least some embodiments improve the physical appearance of persons afflicted with skin ageing. The invention further provides a cosmetic method of improving the appearance of a person suffering from skin ageing.

Skin, like all biological tissue, simultaneously undergoes breakdown and repair. As the body ages the regenerative powers fall off relative to the rate of catabolism.

It is believed, although we do not wish to be bound by this theory, that the reduction in the regenerative powers of skin and/or the increase in catabolism is due to depletion of one or more micronutrients.

Skin ageing appears to involve two pathways; extrinsic and intrinsic. Extrinsic factors are important. 80% or more of skin ageing may be due to extrinsic factors. A major extrinsic factor is photic ageing. Photic ageing is cumulative damage due to repeated exposure to the ionising radiation content of sunlight. Such ionising radiation is thought, but again we do not wish to be bound by this theory, to trigger the release of free radicals. The free radicals are thought to cause damage in a number of ways. Very high levels may cause acute cell death. This leads to sloughing of the skin and the loss of generative cells in the lower dermis. Lower levels of free radicals may cause DNA damage. This can lead to cellular dysfimction, loss of skin structure and, in some cases cancer. This can also damage skin cell membranes to the point where lysosomed membranes may be ruptured. This is believed to cause release of matrix metalloproteases (MMPs). MMPs are thought to cause an inflammatory reaction including lysis of the extracellular matrix. The extracellular matrix is a mesh of micro fibres that provide a soft skeleton. Degradation of the mesh results in thinning and wrinkling of the skin, loss of firmness, elasticity, strength and moisture holding capacity. These are characteristic features of the cosmetic damage caused by skin ageing.

Like all -body tissues, the extracellular matrix is subject to two competing processes; catabolism and anabolism, which may be categorised as tissue wear and renewal respectively. In general, the catabolic process is slightly greater than the anabolic process, and there is a gradual nett loss of tissue integrity, which results in the gradual appearance of ageing. In the particular case of the extracellular matrix underlying the skin, a large part of the catabolic or damaging process is caused by free radical damage caused by exposure to light. Extensive exposure to sunlight increases the rate of catabolism, resulting in accelerated ageing. It follows therefore that skin appearance can be improved by either slowing photic ageing, or increasing the rate of tissue renewal, or preferably both.

According to the invention there is provided a skin care composition for reducing the photic ageing of skin by degradation of extracellular matrix comprising: i) at least one inhibitor of catabolism of the extracellular matrix; and ii) at least one anabolic or pro-anabolic factor for the extracellular matrix.

According to the invention there is provided a cosmetic method of improving the appearance of a mammal afflicted with photic skin ageing comprising administering to the afflicted mammal the skin care composition of the invention.

Compositions of the invention can include inhibitors of catabolism. Catabolism inhibitors fall into several classes. The invention may provide one or more members of one or more classes. a) UV-blocking agent UV-blocking agents reduce the amount of high energy radiation reaching the skin. Since a reduced amount of radiation reaches the skin the potential for damage is reduced. Those skilled in the art will have little difficulty in selecting suitable UV- blocking agents. Examples include metal oxides such as titanium dioxide and zinc oxide which are opaque to a wide range of wavelengths and unsaturated compounds which have strong UV absorbency such as esters of cinnamic acid. The UV blocking agent will generally be applied topically. b) Free radical quenchers

Free radical quenchers destroy free radicals before substantial damage occurs.

The free radical quenchers fall into two sub-groups. The first such as vitamin E, and carotenoids such as β-carotene and lycopene are lypophilic and thus tend to penetrate the dermis. The second sub-group such as vitamin C are hydrophilic and tend to be most effective in extracellular fluids. The free radical quenchers can be applied topically, orally or both. c) MMP Inhibitors Free radicals may promote the release of MMPs which cause inflammation and hence damage. Some embodiments of the invention comprise MMP inhibitors. Examples include flavonoids such as those obtain from bilberry, elderberry or chokeberry. These flavonoids may also inhibit glycosylation of macromolecules which may also be implanted in degeneration of the extracellular matrix. These materials may be administered orally or topically or both. d) Anti-inflammatories

Anti-inflammatories are thought to reduce the damage caused by MMPs.

Examples include fatty acids such as omega 3 polyunsaturated fatty acids and cis- linoleic acid. Purified fatty acids may be used but relatively impure forms such as certain fish oil or preferably plant oils may be used instead. Application may be oral, topical or both. e) Protease inhibitors

In view of the large number of proteases in the body it is generally preferred to apply the inhibitor topically. However in the case of the Birket-Bowman protease inhibitor and other inhibitors which are present in foods, and which are frequently ingested, oral application may be preferable.

The above components alone or in conjunction may reduce the rate of photic ageing. At lease some embodiments of the invention seek to enhance the rate of microfibre formation. It is believed that in many people microfibre formation is reduced due to micronutrient deficiency. Consequently administration of the micronutrients may enhance formation of micro fibres in the extracellular matrix.

Collagen formation may be stimulated by oral administration of vitamin C, vitamin B6, zinc ions and/or copper ions.

Formation of the aminosugar polymer component can be facilitated by glucosamine which will generally be administered orally as a physiologically acceptable salt such as the sulphate or, more preferably the hydrochloride. As manganese is considered to be an important co-factor in glucosamine polymerisation, manganese ions will also be included in the formulation.

In some embodiments of the invention a two part composition is employed. A first part is for oral administration and a second for topical administration. Examples of suitable compositions are as follows: Oral Components

Vitamin C 0.1 -5g, preferably 0.5-2g, especially 1 g in divided doses, more preferably in sustained release form; Vitamin B6 1 - 10 x RDI (Recommended Daily Input), preferably 5x RDI ;

Zinc (in bioavailable form, e.g. as a chelate or organic or inorganic salt)

-lOOmg preferably 5-20mg, especially lOmg; Copper (in bioavailable form, e.g. as a chelate or organic or inorganic alt) 1-lOOmg preferably 1-1 Omg, especially 5mg; Glucosamine (as hydrochloride) 0.1 - 1 Og preferably 0.5-2g, especially 1 g

Manganese (in bioavailable form, e.g. is a chelate) 1-100 mg, preferably

5-40mg; Selenium (as selenium enriched yeast) 150 meg; Betaine 500 mg

Topical Components

Titanium dioxide (finely divided) or other UV filter Vitamin E - max permitted load Vitamin C (ascorbyl palmitate) - max permitted load OPC flavonoids

Omega 3 fatty acid

Stearadonic acid - 20-40% of cream or lotion by volume Protease inhibitor

Mixed carotenoids - 10~20mg - present in the oral and/or topical formulation Berry flavonoids - 200-500 mg - present in the oral and/or topical formulation The oral component may be presented in powdered, tablet, encapsulated or liquid form and may optionally include colourings, flavourings and other materials.

The topical component will generally be presented in the form of a cream or lotion and may include colourings and perfumes

Claims

CLAIMS:-

1. A skin care composition for reducing the photic ageing of skin by degradation of extracellular matrix comprising: i) at least one inhibitor of catabolism of the extracellular matrix; and ii) at least one anabolic or pro-anabolic factor for the extracellular matrix.

2. A composition as claimed in claim 1 wherein the inhibitor of catabolism is one or more of 1) a UV impermeable material;

2) a lipophilic free radial quencher;

3) a hydrophilic antioxidant;

4) anti-inflammatory fatty acids;

5) matrix metalloprotease inhibitors; and 6) Protease inhibitors, preferably Birket-Bowman protease inhibitor.

3. A composition as claimed in claim 1 or claim 2 wherein the anabolic or pro-anabolic factor is one or more of

1) vitamin C; 2) vitamin B6;

3) zinc ions;

4) copper ions;

5) glucosamine;

6) manganese; and 7) Selenium.

4. A composition as claimed in any one of the preceding claims in multi- component form comprising a first component for topical administration and a second component for oral administration.

5. A composition as claimed in claim 4 wherein the first, topical, component comprises one or more of a UV impermeable material; a lipophilic free radical quencher; an anti-inflamniatory fatty acid; an MMP inhibitor; a protease inhibitor; and a lipophillic free radical quenchers.

6. A composition as claimed in claim 4 or claim 5 wherein the second, oral, component comprises one or more of vitamin C; vitamin B6; zinc ions; copper ions; glucosamine; manganese; selenium; a protease inhibitor; and betaine

7. A cosmetic method of improving the appearance of a mammal afflicted with photic skin ageing comprising administering to the afflicted mammal a composition as claimed in any one of the preceding claims.

8. A method as claimed in claim 7 wherein the composition is in multi- component form and comprises a first component for topical application and a second component for oral administration and wherein the two components are administered simultaneously or at spaced intervals.