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01/11/07 - USPTO Class 514 |  184 views | #20070010501 | Prev - Next | About this Page  514 rss/xml feed  monitor keywords

Skin treatments

USPTO Application #: 20070010501
Title: Skin treatments
Abstract: Compositions comprising an LXR activator and retinoic acid and/or a metabolic precursor thereto are useful in reducing the effects of chronoageing and/or photoageing of the skin. (end of abstract)



Agent: Unilever Intellectual Property Group - Englewood Cliffs, NJ, US
Inventors: Gail Jenkins, Andrew Easson Mayes
USPTO Applicaton #: 20070010501 - Class: 514171000 (USPTO)

Related Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), Cyclopentanohydrophenanthrene Ring System Doai, With Additional Active Ingredient

Skin treatments description/claims


The Patent Description & Claims data below is from USPTO Patent Application 20070010501, Skin treatments.

Brief Patent Description - Full Patent Description - Patent Application Claims
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FIELD OF THE INVENTION

[0001] The invention relates to the field of topical or systemic compositions and more particularly to compositions comprising a combination of retinoic acid and a Liver-X-receptor (LXR) agonist and their use in providing a variety of skin care benefits by slowing or inhibiting photo-induced or age-related skin damage.

BACKGROUND TO THE INVENTION

[0002] Skin is subject to deterioration through dermatological disorders, environmental abuse (wind, air conditioning, central heating) or through the normal ageing process (chronoageing) which may be accelerated by exposure of skin to sun (photoageing). In recent years the demand for cosmetic methods for improving the appearance and condition and, in particular, for reversing, reducing or preventing the visible signs of wrinkled, aged and/or photodamaged skin has grown enormously.

[0003] Consumers are increasingly seeking "anti-ageing" products that reverse, treat or delay the visible signs of chronoaging and photoaging skin such as wrinkles, lines, sagging, hyperpigmentation and age spots.

[0004] It is known in the art that retinoic acid is a potent anti-ageing active and induces dermal repair of photodamaged skin. It has been shown that wrinkle effacement and dermal repair following topical treatment of skin with retinoic acid arises through new collagen deposition and synthesis in the skin (for example, Griffiths et al. N. Eng. J. med. (1993) 329, 530-535). It is widely accepted that strengthening of the dermal matrix by boosting the level of collagen in skin using retinoic acid provides anti-ageing/dermal repair benefits.

[0005] The Liver-X-receptor (LXR) is a nuclear receptor known to be present in human keratinocytes where it plays an integral role in the regulation of cell proliferation and differentiation as well as lipid metabolism within the epidermis.

SUMMARY OF THE INVENTION

[0006] The present invention is based on a finding that LXR activators enhance the effects of retinoic acid i.e. that LXR activators and retinoic acid act synergistically.

[0007] In particular, it is shown that LXR activators and retinoic acid act synergistically to upregulate CRAB P II expression in dermal fibroblasts, a well recognised marker of retinoic acid (RA) responsiveness and a transcriptional regulator in RA signalling (Delva et al., 1999, Mol. & Cell Biol. 19, 7158-7167)

[0008] Since upregulation of CRAB P II expression is known to correlate with the ability to reverse the physiological changes induced by chronological ageing and/or photoageing, a combination of an LXR activator and retinoic acid, and/or a metabolic precursor thereto, will be effective in the treatment and prevention of normal, but cosmetically undesirable, skin conditions, due to chronoaging or photoaging, such as wrinkles, lines, and sagging may be obtained through the application of cosmetic (topical) or oral compositions to the skin which comprises an LXR activating ligand in combination with retinoic acid and/or a metabolic precursor thereto.

[0009] Any reference herein to an activator of LXR includes a reference to an activator of LXR.alpha. and/or of LXR.beta., unless specifically stated to the contrary.

[0010] Accordingly, in a first aspect of the present invention a composition is provided comprising (i) an LXR activator other than 25-hydroxycholesterol and (ii) retinoic acid and/or a metabolic precursor thereto.

[0011] A second aspect of the present invention provides a cosmetic method for reducing chronoageing and/or photoageing of the skin, the method comprising applying to the skin a topical composition comprising (i) an LXR activator other than 25-hydroxycholesterol and (ii) retinoic acid and/or a metabolic precursor thereto.

[0012] A third aspect of the present invention comprises a cosmetic method of reducing chronoageing and/or photoageing of the skin, the method comprising dosing topically and/or systemically, an LXR activator and retinoic acid and/or a metabolic precursor thereto. In a preferred embodiment the LXR activator and the retinoic acid and/or metabolic precursor thereto are in the form of a composition.

[0013] In one embodiment, the LXR activator and the retinoic acid and/or metabolic precursor thereto are administered by topical application to the skin. In another embodiment, the LXR activator and the retinoic acid and/or metabolic precursor thereto are administered systemically.

[0014] The present invention also provides use of a combination of an LXR activator and retinoic acid and/or a metabolic precursor thereto in the manufacture of a composition for topical and/or systemic application for reducing chronoageing and/or photoageing of the skin. Such a composition includes both skin creams, lotions, oils etc (including sunscreen compositions) and personal wash products such as liquid or solid soaps, and bath or shower gels, creams etc.

[0015] The present invention further provides a method of enhancing the effect of retinoic acid on skin cells which method comprises administering to the skin cells (i) an LXR activator and (ii) retinoic acid and/or a precursor thereto. Enhancing the effect of retinoic acid on skin cells, such as fibroblasts, includes enhancing expression of retinoic add responsive genes such as CRAB P II.

DETAILED DESCRIPTION OF THE INVENTION

[0016] Unless defined otherwise, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art.

LXR Activating Agents

[0017] Any reference herein to an activator of LXR includes a reference to an activator of LXR.alpha. and/or of LXR.beta., unless specifically stated to the contrary.

[0018] The LXR activating agents can be provided as pure or semi-pure compounds or as crude extracts of natural products, such as plant extracts.

[0019] A preferred class of LXR activators comprises the compounds according to the general formulae (A) or (B); wherein; R represents a hydrogen, a hydroxyl, a keto, an acetyl, a C.sub.1 to C.sub.10, substituted or unsubstituted, branched or unbranched, saturated or unsaturated alkyl group; R.sub.1 represents a lower alkyl group, a hydrogen or COR.sub.6; R.sub.2 represents a hydrogen, a halogen or a hydroxyl group; R.sub.3 represents a hydrogen, a hydroxyl, a halogen, a keto or a lower alkyl group; R.sub.4 represents a hydrogen, a hydroxyl, or a keto group; R.sub.5 represents a hydrogen, a halogen, a hydroxyl or lower alkyl group; R.sub.6 represents a lower alkyl group. X represents a hydrogen, a methyl or a halogen; Y represents a hydrogen, a hydroxyl, a acetyl or a keto group.

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