WO2011158041A2 - Composition topique - Google Patents

Composition topique Download PDF

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Publication number
WO2011158041A2
WO2011158041A2 PCT/GB2011/051138 GB2011051138W WO2011158041A2 WO 2011158041 A2 WO2011158041 A2 WO 2011158041A2 GB 2011051138 W GB2011051138 W GB 2011051138W WO 2011158041 A2 WO2011158041 A2 WO 2011158041A2
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WO
WIPO (PCT)
Prior art keywords
chlorogloeopsis
skin
extract
spp
damage
Prior art date
Application number
PCT/GB2011/051138
Other languages
English (en)
Other versions
WO2011158041A3 (fr
Inventor
Clare O'connor
Stephen Charles Skill
Carole Anne Llewellyn
Original Assignee
The Boots Company Plc
Plymouth Marine Laboratory
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by The Boots Company Plc, Plymouth Marine Laboratory filed Critical The Boots Company Plc
Priority to GB1300858.6A priority Critical patent/GB2495055A/en
Publication of WO2011158041A2 publication Critical patent/WO2011158041A2/fr
Publication of WO2011158041A3 publication Critical patent/WO2011158041A3/fr

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/08Anti-ageing preparations
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9706Algae
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783Angiosperms [Magnoliophyta]
    • A61K8/9789Magnoliopsida [dicotyledons]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783Angiosperms [Magnoliophyta]
    • A61K8/9794Liliopsida [monocotyledons]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
    • A61Q17/04Topical preparations for affording protection against sunlight or other radiation; Topical sun tanning preparations
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q1/00Make-up preparations; Body powders; Preparations for removing make-up
    • A61Q1/02Preparations containing skin colorants, e.g. pigments
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q1/00Make-up preparations; Body powders; Preparations for removing make-up
    • A61Q1/02Preparations containing skin colorants, e.g. pigments
    • A61Q1/04Preparations containing skin colorants, e.g. pigments for lips
    • A61Q1/06Lipsticks
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/005Preparations for sensitive skin

Definitions

  • This invention relates to novel personal care compositions comprising a microalgae extract from Chlorogloeopsis spp. and to uses and methods for the protection of mammalian keratinous tissue against the effects of UV- radiation.
  • UV radiation causes damage to the skin and other keratinous tissue.
  • UV-A 400nm-320nm
  • UV-B 320nm-280nm
  • UV-induced skin damage may include sunburn, thickening and/or thinning of areas of the skin, accelerated skin ageing, age spots, lowered immunity against infection, destruction of beneficial vitamins in the skin (such as vitamin A) and also direct and/or indirect DNA damage.
  • UV-B radiation primarily affects the epidermis causing an erythemal response, leading to sunburn. UV-B may also cause direct damage to the DNA, including the formation of cyclopyrimidine dimers which, if not repaired, may lead to DNA-mutations which may be a factor in some cancerous conditions.
  • UV-A radiation penetrates deeper into the skin leading to effects such as collagen breakdown and premature skin ageing. UV-A radiation may also cause the formation of free radicals and reactive oxygen species in the epidermis which are detrimental to living tissue though damage to cell function and may lead to indirect damage to the DNA and, in some cases, the formation of malignant melanoma.
  • sunscreening agents are incorporated in topical compositions.
  • Sunscreens are materials which absorb or reflect UV radiation, thus protecting the skin against exposure to sunlight and other sources of UV radiation. Sunscreens may be selected from a variety of classes of organic and inorganic materials. The efficacy of each sunscreen varies due to factors including the degree of protection, the period of time after application for which the sunscreen provides effective protection, the solubility of the sunscreen in the formulation and the wavelength range over which the sunscreen absorbs UV radiation. A sunscreen is generally most effective over a particular sub-range in the UV-A or UV-B range.
  • compositions incorporate a combination of sunscreens which attempt to provide protection across the UV-A and UV-B spectrum, but these generally only provide a degree of protection due to the limited absorption ranges of the materials used, as well as the degradation of, and potential interactions between, the photo-reactive ingredients.
  • topical compositions may comprise anti-oxidants, such as Vitamin E, lipoic acid and grapeseed oil, to reduce the effects of free-radicals on the skin, moisturising agents such as glycerine and shea butter, soothing agents such as aloe vera and camomile and/or anti-inflammatory agents, for example allantoin and liquorice extract.
  • anti-oxidants such as Vitamin E, lipoic acid and grapeseed oil
  • moisturising agents such as glycerine and shea butter
  • soothing agents such as aloe vera and camomile and/or anti-inflammatory agents, for example allantoin and liquorice extract.
  • the majority of compositions which are used to protect body surfaces from UV radiation comprise at least one sunscreening agent and may comprise one or more ingredients selected from anti-oxidants, moisturising agents, soothing agents and anti-inflammatory agents in order to try to maximise protection.
  • Extracts from microalgae have a variety of interesting uses in skincare, for example microalgae have some moisturising and soothing properties and can be used in a wide variety of cosmetics.
  • some microalgae are known to have useful UV-absorbing properties.
  • the algae in response to potentially damaging UV radiation, the algae can produce mycosporine-like amino acids (MAAs) which absorb certain wavelengths in the UV spectrum (for example 310-360nm) to protect the organism from such radiation.
  • MAAs mycosporine-like amino acids
  • One illustrative microalgae is the cyanobacterium Chlorogloeopsis PCC 6912 which was found to synthesise two putative UV sunscreen compounds of the MAA type - mycosporine-glycine and shinorine (Portwich et al, Arch Microbiol (1999), 172, p187-192). Also, a UV-B specific photoreceptor has been identified in the above cyanobacterium (Portwich el al, Photochemistry and Photobiology, 71 (4): p493-498, 2000). Some references relate to the utility of certain naturally-occurring materials as sunscreening agents, namely materials which absorb or reflect UV radiation.
  • sunscreen compositions which comprise naturally occurring materials as sunscreen agents, which materials may be extracted from plants, algae, cyanobacteria, fungi and bacteria that protect against exposure to solar radiation.
  • cyanobacteria principally use a combination of carotenoids, scytonemin and mycosporine amino acids to provide sunscreen activity against UV radiation.
  • sunscreen compositions for topical application to human skin and hair may be prepared from one or more of these materials, preferably a synergistic combination of all three materials.
  • microalgae Plectonema boryanum is cultured under conditions which maximise production of myxoxanthophyll, scytonemin and mycosporine and the resulting product formulated into a sunscreen cream which is shown to provide enhanced UV protection compared to conventional UV absorbing agents.
  • WO 0239974 describes that the sunscreening properties of personal care compositions may be improved by combining conventional inorganic or organic sunscreening agents with sunscreening compounds which are mycosporine-like amino acids (MAAs), including palythine, palythine serine, palythinol, asterina, mycosporine-2-glycine, shinorine, porphyra-334, N- methyl mycosporine serine, N-methyl mycosporine threonine, mycosporine- glycine valine, palythenic acid, usijirene and palythene .
  • MAAs mycosporine-like amino acids
  • Chlorogloeopsis spp. has advantageous properties in protecting keratinous tissue against the deleterious effects of UV radiation.
  • the formulation of an extract from Chlorogloeopsis spp. in personal care compositions has not previously been proposed.
  • the present inventors have shown that an extract produced from Chlorogloeopsis spp. may be formulated as a topical composition to provide protection against exposure to UV radiation for mammalian (especially human) keratinous tissue.
  • Compositions comprising said extract possess improved protection properties against UV-radiation. It has been found that said extract has particular efficacy in inhibiting TNF-a and, in contrast to the mode of action of sunscreens, the UV protective properties of an extract produced from Chlorogloeopsis spp.
  • the extract from Chlorogloeopsis spp. is believed to possess advantageous properties in protecting the skin against free radicals and/or reactive oxygen species compared to standard UV protective agents.
  • the extract from Chlorogloeopsis spp. is derived from a naturally occurring material and thus may be considered by some consumers more suitable for application to human tissue, such as the skin, compared to synthetic materials, to provide protection from UV-radiation.
  • a personal care composition comprising a microalgae extract from Chlorogloeopsis spp. and a topically acceptable carrier therefor.
  • a method for preventing, ameliorating or treating UV-induced damage of mammalian keratinous tissue comprising the topical application of a microalgae extract from Chlorogloeopsis spp. to an area susceptible to such damage.
  • said microalgae extract protects keratinous tissue against the deleterious effects of UV radiation.
  • the extract inhibits the synthesis of TNF-a in keratinous tissue.
  • the Tumour Necrosis Factor alpha (TNF-a) mechanism may be induced when body tissues are exposed to UV radiation. It has been found that an extract derived from Chlorogloeopsis is effective in inhibiting this mechanism and thus causes a reduction in the synthesis of epidermal TNF-a. Thus, said extract is effective to inhibit the biosynthesis of TNF-a produced by exposure of keratinous tissue to UV radiation. It is believed that the reduction in cell death may be achieved through effecting a reduction in the synthesis of epidermal TNF-a. Said microalgae extract also inhibits the levels of lipo-peroxides on the skin after UV exposure. Measurement of lipo-peroxidation is an indication of free radical damage to skin lipids.
  • ROS reactive oxygen species
  • a microalgae extract from Chlorogloeopsis spp. means substantially the whole biological extract produced from the microalgae, not individual components thereof, and includes (i) water soluble extracellular or capsular material derived from the washing of Chlorogloeopsis spp.
  • the unique source of the biological extract may be
  • genomic analysis characterised by genomic analysis.
  • the whole biological extract is present.
  • substantially all of or a portion of the pigment may be removed.
  • Chlorogloeopsis is a thermophilic cyanobacterial species. It is nitrogen-fixing with heterocysts forming the sites of nitrogen fixation differentiating in response to the lack of combined nitrogen in the environment.
  • Chlorogloeopsis species also produce relatively short, motile filaments called hormogonia and this characteristic, in part, distinguishes them from members of the closely related genus Anabaena.
  • Chlorogloeopsis species differentiate spore-like structures termed akinetes in response to nutrient limitation other than nitrogen.
  • the thallus of Chlorogloeopsis is in form of a compact stratum of indefinite size, composed of irregular or irregular-rounded cell-packets and aggregates, or of uniserial up to multiserial short rows of cells (trichomes with 3-20 cells), usually without distinct mucilaginous envelopes, but sometimes single cell-packets enclosed in thin, firm sheaths. Elongated branches or typical filaments are not formed. Cells are rounded or angular, with pale blue-green, granula content. Heterocytes are terminal and intercalar, irregularly disposed, sometimes lacking.
  • Chlorogloeopsis spp. is an aquatic cyanophyceae microalgae commonly found naturally around hot springs. It may be found in saline and/or brackish lakes, but commonly is found in freshwater environments and springs.
  • Chlorogloeopsis species are distributed in illuminated portions of the biosphere, including fresh waters and tropical temperate, they are rarely found in marine habitats. Growth in both aquatic and terrestrial habitats is often as a colony of thalli within a gelatinous matrix. Growth upon soil particles is a common characteristic of these species. The size of the colonies ranges from microscopic to macroscopic dimensions. Nitrogen-fixing Chlorogloeopsis species are major contributors to the sequestration of carbon dioxide into organic compounds, especially in nutrient poor and extreme environments.
  • Characterisation of cyanobacterial strains can be achieved with extraction of genomic DNA (Singh et al, World Journal of Microbiology and Biotechnology, Vol 27, No 5, 201 1 , p1225-1230) together with a PCR based technique (Lu et al 1997, FEMS Microbiology Letters, 153 (1997) 141 -149) and compared with a reference genomic sample according to standard forensic methods.
  • genomic DNA San Diego et al, World Journal of Microbiology and Biotechnology, Vol 27, No 5, 201 1 , p1225-1230
  • PCR based technique Li et al 1997, FEMS Microbiology Letters, 153 (1997) 141 -149
  • Chlorogloeopsis fritschii [Mitra and Pandey (1966), available from Sammlung von Algenkulturen deposited as SAG 141 1 -1 a and also from the Pasteur Culture Collection as PCC6912; both cultures are derived from the same Mitra and Pandey isolates from soil in India], Chlorogloeopsis sp strain Cgs-089 and
  • Chlorogloeopsis PCC 7518 also known as Chlorogloeopsis HTF
  • Chlorogloeopsis HTF Chlorogloeopsis HTF
  • Chlorogloeopsis fritschii Chlorogloeopsis fritschii
  • the microalgae extract from Chlorogloeopsis spp. may be cultivated in media, for example aqueous media, from an isolate, for example obtained from a Culture Collection, to form a biomass according to techniques known to those skilled in the art and also using protocols described in: Algal
  • Chlorogloeopsis cells may then be harvested and then extracted according to conventional methods, for example as disclosed in Portwich et al, Arch Microbiol (1999), 172, p187-192.
  • the UV radiation against which compositions according to the present invention have been shown to provide useful protection, may be derived from an artificial source which radiates part of or the whole of the UV spectrum or it may be derived from natural sources, especially sunlight. Preferred treatments herein concern UV radiation produced in sunlight.
  • the compositions according to the invention are particularly suitable for the prevention, amelioration or treatment of UV-induced damage to mammalian keratinous tissue, including the skin, hair and nails.
  • the keratinous tissue comprises skin and hair.
  • the keratinous tissue comprises skin tissue, particularly the epidermis and the dermis, especially the epidermis.
  • the mammalian tissue may apply to any mammal for which protection from UV radiation is desired, especially human tissue which is exposed to UV radiation.
  • Damage to the keratinous tissue may include any deleterious effect that UV- radiation induces in said tissue, for example by inhibiting the healthy functioning of cells, such as by inducing mechanisms which may lead to cell death, including the formation of tissue-damaging free-radicals and/or oxygen species and/or which may be detrimental to the appearance of said tissue, especially the skin.
  • Chlorogloeopsis extract exerts a beneficial
  • the extract also promotes the functioning of healthy skin following exposure to UV radiation.
  • Chlorogloeopsis extract may exhibit protective activity for the cells of said tissue against the effects of radiation generated across part of or the whole of the UV spectrum, especially wavelengths in the UV-A and UV-B regions.
  • Chlorogloeopsis extract provides particular advantages in protecting DNA against damage arising from UV radiation, including both UV-A and UV-B radiation, which may be useful to reduce photo-ageing and associated photodamage, uneven pigmentation, wrinkles and sagging skin and/or some cancerous conditions.
  • the extract may be formulated in advantageous topical compositions which may provide valuable penetration properties in keratinous tissue, especially the skin.
  • Chlorogloeopsis extract may provide effective UV-protection in the skin below the surface of the keratinous tissue, for example, throughout the dermis and/or into the epidermis, preferably across both the dermis and the epidermis. Topical compositions comprising the extract may also provide protection deeper into the epidermis and dermis than found in conventional UV protection systems. It is also believed that Chlorogloeopsis extract may ameliorate the
  • ROS reactive oxygen species
  • Chlorogloeopsis extract may be useful in treating or preventing cell death by apoptosis which has been induced by UV radiation.
  • Cell death by apoptosis is a physiological process that enables the elimination of cells without causing an inflammatory response.
  • self-renewing tissue for example the epidermal layers of the skin, cell numbers are tightly regulated by a delicate balance between proliferation, differentiation and cell death. Cell death can be induced by exposure to UV radiation. PGE2 tests conducted with
  • Chlorogloeopsis extract indicate that no significant anti-inflammatory activity occurs. Accordingly, it is believed that the UV protection effect achieved by the Chlorogloeopsis extract does not include any significant anti-inflammatory component and in one embodiment is free of an anti-inflammatory
  • the UV protective effect of the Chlorogloeopsis extract does not include any significant UV-absorption effect and in one embodiment is free of an UV- absorption effect (for example UV-A and/or UV-B), particularly absorption of UV-B radiation.
  • the protective activity of the Chlorogloeopsis extract may include an anti-oxidant type effect by which we mean that the extract may reduce the effects of detrimental material, such as tissue- damaging free radicals and/or reactive oxygen species, generated in the keratinous tissues on exposure to UV radiation. This may include
  • neutralising the detrimental material for example by preventing said material combining with the tissue and/or stimulating the repair mechanism of the body tissues, including the production of enzymes such as superoxide dismutase, catalase, and glutathione peroxidise.
  • Chlorogloeopsis extract and compositions comprising said extract may inhibit the destruction of cells in keratinous tissue, especially skin cells, caused by UV radiation, in particular UV-B radiation.
  • Chlorogloeopsis extract and compositions comprising said extract may inhibit the destruction of cells in keratinous tissue, especially skin cells, caused by UV radiation, in particular UV-B radiation.
  • Chlorogloeopsis extract and compositions comprising said extract may inhibit the destruction of cells in keratinous tissue, especially skin cells, caused by UV radiation, in particular UV-B radiation.
  • compositions comprising said extract may inhibit the synthesis of TNF-a in keratinous tissue exposed to UV radiation.
  • Chlorogloeopsis extract and compositions comprising said extract may inhibit photoageing arising from cell death induced by TNF-a.
  • Chlorogloeopsis extract may inhibit UV-induced cell death in epidermal tissue affected by UV radiation damage.
  • Chlorogloeopsis extract and compositions comprising said extract may inhibit the formation and growth of cancerous and pre-cancerous skin cells induced by UV radiation.
  • Chlorogloeopsis extract and compositions comprising said extract may inhibit apoptotic skin cell damage.
  • Chlorogloeopsis extract and compositions comprising said extract may inhibit UV-induced non-inflammatory skin damage.
  • Chlorogloeopsis extract and compositions comprising said extract may inhibit UV-induced damage to keratinous tissue by a mechanism other than by absorption and/or reflection of UV-radiation, ie non-UV-absorptive protection against the deleterious effects of UV-radiation.
  • Chlorogloeopsis extract may inhibit lipo-peroxidation in skin tissue.
  • the Chlorogloeopsis extract and compositions containing said extract may protect DNA present in keratinous tissue against damage arising from exposure of said tissue to UV radiation.
  • the Chlorogloeopsis extract and compositions containing said extract may be combined with a sunscreen to provide enhanced protection against UV radiation.
  • the present invention provides a personal care
  • compositions for use in the prevention, amelioration or treatment of UV- induced damage of mammalian keratinous tissue comprising a microalgae extract from Chlorogloeopsis spp. and a carrier therefor.
  • Compositions according to the invention may be used to prevent the deleterious effects of UV radiation on skin, hair and nails, for example destruction of cells which can have a deleterious effect on the appearance of the body surface, such as signs of ageing of the skin, brittleness of the hair and/or nails and/or bleaching of dye coloured hair.
  • compositions according to the invention are especially useful in preventing and/or treating dermal and/or epidermal skin damage, such as one or more of the following skin conditions: photo- ageing skin damage, uneven pigmentation, wrinkles and sagging skin, preferably two or three of such conditions, most preferably all of the above conditions.
  • composition according to the invention may be applied to the keratinous tissue, before, during or after exposure to UV radiation.
  • the composition is applied before exposure to radiation, for example 1 -30 minutes before exposure, preferably 1 -15 minutes before exposure.
  • compositions according to the invention may be useful in reducing free-radical reactions in the skin and thus may still be of benefit in treating UV damaged skin.
  • Chlorogloeopsis extract is stable and is generally presented in liquid form, although it may be dried to a powder. Chlorogloeopsis extract is
  • the liquid which may be in the form of a concentrate or diluted with water and/or butylene or propylene glycols and/or glucosides, is substantially clear, although may be coloured in some cases.
  • an antimicrobial agent for example glycerine. It may be formulated as an aqueous composition or may be combined with oily materials.
  • Personal care compositions according to the present invention are generally used to benefit the area to which it is applied, for example to cleanse, moisturise, protect and/or administer beneficial ingredients to improve the condition of the area of the body to which the subject compositions are applied.
  • uncovered body surfaces are exposed to UV radiation through sunlight when outdoors and also indoors when light shines through a window onto the body or the keratinous tissue is exposed to an artificial UV source.
  • compositions of the present invention comprise a therapeutically effective amount of Chlorogloeopsis extract.
  • the personal care compositions contain said extract in an amount effective to prevent, ameliorate or treat UV-induced tissue damage.
  • compositions according to the invention may contain a total 0.05 to 20% of Chlorogloeopsis extract by weight of the total composition.
  • the total amount of Chlorogloeopsis extract that may be present is preferably in the range 0.1 to 5% w/w, more preferably 0.2 to 2% w/w and most preferably about 1 % w/w by weight of the composition.
  • a sunscreening agent may be present in the personal care compositions in an amount from 0.1 to 20% w/w, preferably 0.1 to 10% w/w, of the
  • compositions according to the invention may comprise at least one organic and/or inorganic sunscreening agent.
  • suitable inorganic sunscreening agents include: a) Microfine titanium dioxide; b) Microfine zinc oxide; and c) Boron nitride.
  • suitable organic sunscreening agents include: a) p-aminobenzoic acid sunscreens, esters and derivatives thereof, for example, 2-ethylhexyl p-dimethylaminobenzoate and the octyl ester of p- aminobenzoic acid;
  • methoxycinnamate esters sunscreens such as 2-ethylhexyl p- methoxycinnamate, 2-ethoxyethyl p-methoxycinnamate or a, -di-(p- methoxycinnamoyl)-a'-(2-ethylhexanoyl)-glycerin;
  • benzophenone sunscreens such as oxybenzone
  • benzotriazolyl sunscreens such as methylene bis-benzotriazolyl tetramethylbutylphenol
  • camphor sunscreens such as methyl benzyl idene camphor
  • organic pigment sunscreens such as methylene bis-benzotriazole
  • silicone sunscreens such as drometrizole trisiloxane and benzylidene malonate polysiloxane
  • salicylate sunscreens such as octyl salicylate.
  • a preferred group of sunscreens is microfine titanium dioxide; Microfine zinc oxide; Boron nitride; p-aminobenzoic acids, esters and derivatives thereof; methoxycinnamate esters; benzophenones; 2-phenylbenzimidazole-5- sulfonic acid; disodium phenyl dibenzimidazole tetrasulfonate;
  • terphthalylidene dicamphor sulfonic acid alkyl- , -diphenylacrylates; triazine sunscreens; benztriazolyl sunscreens; camphor sunscreens; organic pigment sunscreens; silicone sunscreens;and salicylate sunscreens.
  • Other materials useful in UV protection may be used in personal care compositions according to the presnt invention, including anti-oxidants, moisturisers, soothing agents and/or anti-inflammatory agents. Such ingredients will be used in conventional amounts known to those skilled in the art, for example 0.1 -10% w/w.
  • Topically acceptable carriers include any conventional cosmetic,
  • compositions suitable for topical administration.
  • the carrier may form the remainder of the composition, ie to form up to 100% w/w of the composition.
  • it may be present in an amount of 80-99.9% w/w, preferably 85-99.9% w/w and advantageously 90-99.9% w/w.
  • Particularly advantageous personal care compositions according to the present invention comprise 0.1 -5% w/w of a microalgae extract from
  • compositions according to the present invention comprise 0.1 -5% w/w of a microalgae extract from Chlorogloeopsis spp., 0.1 -15% sunscreens and 80-99.8% w/w of a topically acceptable carrier.
  • beneficial ingredients may be incorporated in the compositions according to the present invention.
  • Such ingredients are well known to those in the art of cosmetic formulations and may be present in conventional concentrations.
  • Suitable skin care active ingredients include anti-acne actives eg salicylic acid, vitamins eg Vitamin A or retinol, anti-wrinkle or anti-ageing actives such as peptides, flavonoids and promoters of collagen and/or elastin production, hydroxy acids, anti-oxidants, eg Vitamin E, lipoic acid and grapeseed oil, soothing agents, such as aloe vera and camomile and/or anti-inflammatory agents, for example allantoin and liquorice extract, antimicrobials eg triclosan, skin-lightening actives such as mulberry or ascorbic acid
  • Suitable hair care active ingredients include silicones, vitamins, hair conditioners, shine agents, resins, temporary, semi-permanent and oxidative dyes, sunscreens, antioxidants, proteins, amino acids, organic acids, anti- dandruff agents, lipids, moisturisers, humectants, film formers, reducing agents, oxidising agents and other suitable materials that are known to those skilled in the art.
  • each active ingredient may be used in the formulation in the range from 1 x 10 "6 % to 80% by weight of the formulation, but more usually will be in the range from 0.001 % to 20% by weight, preferably from 0.01 % to 8% by weight and most preferably 0.01 % to 5% by weight of the formulation.
  • Example formulations include sun creams or lotions, daily moisturising creams, eg for the face and eyes, shampoos containing conditioning agents and pearlescent systems, hair conditioners, serums, lipsticks and lotions.
  • Preferred compositions are in the form of a cream emulsion, an aqueous or emulsion lotion or a waxy stick, for example a lipstick.
  • the Chlorogloeopsis extract of the present invention may be incorporated into suncare products such as aqueous or oily solutions or dispersions or emulsions in the conventional way.
  • the Chlorogloeopsis extract is contained in an aqueous phase of said composition.
  • Emulsions may be in the form of an oil-in-water emulsion, a water-in-oil emulsion, an oil- in-water-in-oil emulsion or a water-in-oil-in-water emulsion.
  • Preferred compositions comprise solutions or oil-in-water emulsions.
  • the oil phase of the water-in-oil or oil-in-water emulsions of the present invention may comprise for example: a) hydrocarbon oils such as paraffin or mineral oils ; b) waxes such as beeswax or paraffin wax; c) natural oils such as sunflower oil, apricot kernel oil, shea butter or jojoba oil ; d) silicone oils such as dimethicone, cyclomethicone or cetyldimethicone ; e) fatty acid esters such as isopropyl palmitate, isopropyl myristate or dioctylmaleate ; fatty alcohols such as cetyl alcohol or stearyl alcohol ; or g) mixtures thereof, for example, the blend of waxes available commercially under the trade name Cutina (Henkel).
  • hydrocarbon oils such as paraffin or mineral oils
  • waxes such as beeswax or paraffin wax
  • natural oils such as sunflower oil, apricot kernel
  • the oil phase comprises 5 to 40%, more preferably 10 to 30% by weight of the
  • oil phase comprises 5 to 30%, more preferably 10 to 20% by weight of the composition.
  • the emulsifiers used may be any emulsifiers known in the art for use in water-in-oil or oil-in-water emulsions. It has been found that particularly effective water-in-oil and oil-in-water sunscreen compositions can be prepared by using an emulsifier or mixture of emulsifiers selected from known cosmetically acceptable emulsifiers which include : a) sesquioleates such as sorbitan sesquioleate, available commercially for example under the trade name Arlacel 83 (ICI), or polyglyceryl-2 sesquioleate ; b) ethoxylated esters of derivatives of natural oils such as the polyethoxylated ester of hydrogenated castor oil available commercially for example under the trade name Arlacel 989 (ICI) ; c) silicone emulsifiers such as silicone polyols available commercially for example under the trade name ABIL WS08 (Th. Goldschmidt AG); d) anionic emuls
  • potassium stearate and fatty acid sulphates e. g. sodium cetostearyl sulphate available commercially under the trade name Dehydag (Henkel) ; e) ethoxylated fatty alcohols, for example the emulsifiers available commercially under the trade name Brij (ICI) ; f) sorbitan esters, for example the
  • emulsifiers available commercially under the trade name Span (ICI) ;
  • ethoxylated sorbitan esters for example the emulsifiers available commercially under the trade name Tween (ICI) ; h) ethoxylated fatty acid esters such as ethoxylated stearates, for example the emulsifiers available commercially under the trade name Myrj (ICI) ; i) ethoxylated mono-, di-, and tri-glycerides, for example the emulsifiers available commercially under the trade name Labrafil (Alfa Chem.); j) non-ionic self-emulsifying waxes, for example the wax available commercially under the trade name Polawax (Croda); k) ethoxylated fatty acids, for example, the emulsifiers available commercially under the trade name Tefose (Alfa Chem. ); I) methylglucose esters such as polyglycerol-3 methyl glucose distearate available
  • Tegocare 450 (Degussa Goldschmidt) ; or m) mixtures thereof.
  • the amount of emulsifier present in the emulsion compositions of the present invention is preferably in the range 1 to 10% by weight.
  • compositions of the present invention may additionally comprise other components which will be well known to those skilled in the art.
  • emollient such as isopropyl myristate or triglycerides of fatty acids e. g. lauric triglyceride or capric/caprylic triglyceride, such as the triglyceride available commercially under the trade name Miglyol 810 (Huls UK); moisturisers such as D-panthenol ; humectants such as glycerin or 1 , 3- butylen glycol ; antioxidants such as DL-a-tocopherylacetate or butylated hydroxytoluene ; emulsion stabilising salts such as sodium chloride, sodium citrate or magnesium sulphate ; film formers to assist spreading on the surface of the skin such as alkylated polyvinylpyrrolidone, e. g. those available commercially under the trade name Antaron
  • hydroxyethylcellulose available commercially under the trade name Natrosol (Hercules) or alkylgalactomanans available under the trade name N-Hance; preservatives such as bronopol, sodium dehydroacetate,
  • polyhexamethylenebiguanide hydrochloride, isothiazolone or diazolidinylurea sequestering agents such as EDTA salts ; perfumes and colourings.
  • the Chlorogloeopsis extract may be obtained by conventional extraction techniques, including extraction with supercritical carbon dioxide or superheated water or lixiviation (separation of soluble from insoluble substances by dissolving the former in water or other solvent and recovering the soluble material by evaporation or preceipitation).
  • a preferred method comprises harvesting Chlorogloeopsis from a bioreactor, followed by freeze drying. The freeze-dried material is then resuspended into the extraction media (water and glycerin). Alternatively, harvested
  • Chlorogloeopsis may be subjected to ultrasonic extraction on a frozen algae plate at 10% w/w of dry matter diluted in the same weight of water; the concentrated extract may then be re-diluted for formal concentration of biomass to approx 2g dry/L. The resulting extract from both procedures is then preferably heated (for example to 65°C for two hours) to eliminate the pigment phycocyanin. Chlorogloeopsis extract may also be obtained by known techniques from seaweed. It will be appreciated that the method according to this aspect of the invention may be a therapeutic method, for example to treat damaged skin and to encourage it to repair so that UV-induced cancerous conditions do not develop, but will often be a primarily cosmetic method, the objective of which is to reduce the effects of photoageing which is externally visible.
  • a cosmetic method of ameliorating the effects of UV damage caused by sunlight to human keratinous tissue comprising the step of topical application of a composition comprising a microalgae extract from Chlorogloeopsis spp. and a topically acceptable carrier therefor.
  • a microalgae extract from Chlorogloeopsis spp. for use in the prevention, amelioration or treatment of damage to mammalian keratinous tissue by UV radiation and/or for the inhibition of TNF-a synthesis in human skin.
  • a method of preparing a composition for the prevention or treatment of UV-induced damage to mammalian keratinous tissue comprising combining a microalgae extract from Chlorogloeopsis spp. with a topically acceptable carrier to form a personal care composition.
  • a method of administering a composition capable of protecting mammalian keratinous tissue from the deleterious effects of UV radiation by applying a personal care composition according to the present invention to keratinous tissue in need of treatment or protection .
  • Figure 1 represents a comparison of the the effect on the monoprotection factor (MPF) of Chlorogloeopsis extract (1 % w/w) on a sun-lotion (SPF 15).
  • Figure 2 represents the monoprotection factor (MPF) value of
  • Chlorogloeopsis extract Chlorogloeopsis extract.
  • Chlorogloeopsis was harvested from a bioreactor and freeze dried. The freeze-dried material was then re-suspended into the extraction media (water and glycerin), heated to remove the coloured pigments and filtered to give aqueous Chlorogloeopsis extract.
  • extraction media water and glycerin
  • Example 1 Sunscreen composition
  • Chlorogloeopsis extract 1 .0
  • a Ingredients 2 to 1 1 are mixed and heated to 65°C to melt together.
  • B Ingredients 12 to 16 are mixed and heated to 70°C.
  • Part A is added to part B slowly with stirring.
  • Chlorogloeopsis extract 0.5
  • a Ingredients 2 to 9 are mixed and heated to 65°C to melt together.
  • Part A is added to part B slowly with stirring.
  • a Ingredients 2 to 6, and 8 and 9 are mixed and heated to 65°C to melt together.
  • Part A is added to part B slowly with stirring.
  • Part A is added to part B with stirring and homogenised for 20 minutes to give sunscreen compositions having an SPF of 8.
  • Phase B To Phase B add 15 and homogenise for 20 minutes.
  • PEG-12 isostearate 0.125
  • citric acid EDTA, sodium phosphate, disodium phosphate and lactic acid are added and dispersed. Using a homogeniser, carbomer is added and hydrated. The aqueous phase is then heated to 70°C.
  • stage 2 is added to stage 1 and this is mixed until emulsified and uniform.
  • the emulsion is then cooled to below 35°C using stirring.
  • the remaining materials, including the Chlorogloeopsis extract are then added and mixed.
  • the product is then made to weight using purified water and is stirred until uniform.
  • cetearyl isononanoate, dimethicone, silica, PVP/hexadecene copolymer, caprylic/capric triglyceride, paraffinum liquidum, petrolatum, hydrogenated coco-glycerides, cetearyl octanoate, cetearyl alcohol, octyl methoxycinnamate, talc, glyceryl stearate, PEG-100 stearate, butyl methoxydibenzoylmethane, borago officinalis, tocopheryl acetate, sodium stearoyi lactylate, isopropyl myristate, salicylate, dibenzoyi methane and lecithin oil phase are mixed and heated to 70°C to melt the waxes.
  • stage 2 is added to stage 1 and this is mixed until emulsified and uniform.
  • the emulsion is then cooled to below 35°C using stirring.
  • the remaining materials, including Chlorogloeopsis extract, are then added and mixed.
  • the product is then made to weight using purified water and is stirred until uniform.
  • Example 10 Measurement of TNF-g Inhibition
  • test compositions were administered topically to human skin and protection against UV radiation assessed by measuring the inhibition of TNF-a.
  • the compositions were as follows:
  • Test composition A As Control composition except that Test Composition A comprises Chlorogloeopsis extract (5% w/w) in replacement for a portion of the water content (5% w/w).
  • Test composition B As Control composition except that Test Composition B comprises Chlorogloeopsis extract (0.5% w/w) in replacement for a portion of the water content (0.5% w/w).
  • the explants were transferred to a well of 96 multiwells containing Agar gel (310 ⁇ ) and then irradiated with UVA (50 J/cm 3 ) and UVB (500 mJ/cm 3 ).
  • the explants were placed in a well of 6 multiwells for 24 hours. The supernatants were removed and frozen for the dosage of TNF-a.
  • the explants were cut in half and placed in a well of 24 multiwells with 1 ml of Hanks balance salt Solution (HBSS) buffer solution and incubated for 3 hours at 37°C in a humid atmosphere containing 5% v/v CO2.
  • HBSS Hanks balance salt Solution
  • the explants were then rinsed and placed in a new well of 24 multiwells with 1 ml isopropanol for 2 hours at room temperature under agitation. 200 ⁇ of each well was transferred into a well of 96 multiwells and a reading of the optical density at 540nm achieved through a conventional UVM 340 microplate reader.
  • TNF-alpha ELISA kit The dosages of TNF-a were conducted with a conventional quantification kit (TNF-alpha ELISA kit).
  • the results of assays are expressed in picograms/ml of TNF-a culture medium after a calibration curve performed with a solution of TNF-a. The results are expressed as a percentage of untreated control.
  • TNF- ⁇ measurements for the Control were made before and after UV irradiation.
  • TNF-a measurements were made for test compositions A and B and the results shown in Table I below.
  • Test Composition A was effective against UV radiation. The presence of 5% w/w Chlorogloeopsis extract was found to reduce the production of TNF-a by 43% compared to the UV-irradiated Control composition.
  • Test Composition B was effective against UV radiation. The presence of 0.5% w/w Chlorogloeopsis extract was found to reduce the production of TNF-a by 31 % compared to the UV-irradiated Control composition.
  • Chlorogloeopsis extract was produced as follows:
  • Frozen biomass was re-suspended in a litre of de-mineralized water to achieve the required final re-suspension concentration.
  • the Lipid-peroxidation test was carried out as follows:
  • a 0.1 % solution of Triton X-100 ((octylphenol ethoxylate) using distilled water was made up (This solution is used to dilute test products).
  • Stock samples of extracts 1 :1 ratio of 0.1 % Triton - X 100 solution and test sample were made up .
  • 50 ⁇ of the Test samples was added to microfuge tubes and mixed (Whirlmixer).
  • 50 ⁇ of the lipid stock was added to the microfuge tubes and mixed (Whirlmixer).
  • a 7.5 ⁇ sample from each microfuge tube was removed and placed in an appropriate well in one half of the Microtitre Plate.
  • the microtitre plate was irradiated for 1 19 seconds under the Solar Simulator. The plate was removed from under Solar Simulator and 7.5 ⁇ of Assay standard added to 3 wells in each half of the plate in triplicate. 75 ⁇ of reagent A (Enzyme reagent (Ascorbi, Oxidase, Lioprotein, Lipase, Stabiliser)) from the Lipid peroxidation kit was added into every well (being careful not to make any bubbles with the pipette) and incubated for 5 minutes exactly at 30°C. 175 ⁇ of reagent B (Chromogen Reagent) was added into each well and incubated for 10 minutes at 30°C. Finally, the microtitreplate was scanned immediately on the plate reader at 675nm.
  • reagent A Enzyme reagent (Ascorbi, Oxidase, Lioprotein, Lipase, Stabiliser)
  • the mean absorbency of each material was calculated and converted to lipid peroxide (nmol/ml) by taking the mean of each material absorbency and subtracting the mean of the blank and dividing by the calibrator mean, subtracting the blank mean and multiplying by 50.
  • the % inhibition of each material was then calculated by comparing the irradiated and non irradiated samples, by mean of the lipid peroxide (nmol/ml) and dividing by the lipid peroxide (nmol/ml) of the linoleic acid.
  • Example 12 Test to Compare SPF value of a Sunscreen composition (SPF 15) with and without Chloroqloeopsis extract 1 % w/w. Method:
  • Sunscreen product was applied to the roughened surface of the substrate (PMMA plate) at the designated application rate and was left to dry, in the dark, for 15 minutes together with a 100% transmission blank substrate which had been 'wetted' with an appropriate material (eg glycerine).
  • an appropriate material eg glycerine
  • the 100% transmission blank substrate was placed in the path of the measurement instrument's light source and signal measurements were taken in 2nm increments from 290nm to 400nm at a number (minimum 3) of different positions on the substrate surface.
  • the mean of the signal measurements at each wavelength represents the 100% transmission signal at that wavelength.
  • the sunscreen-treated substrate was then placed in the path of the measurement instrument's light source so that the light-beam fell directly onto a small area on the surface of the substrate.
  • Transmission signal measurements were then made in 2 nanometre increments from 290nm to 400nm at this first location on the substrate surface.
  • the substrate was then moved so that the light beam fell on to a different spot on the surface of the substrate and a further series of transmission signal measurements were made in 2nm increments. This procedure was repeated until a minimum of 5 measurements had been made and a minimum substrate surface area of 2.0 cm 2 had been sampled.
  • the minimum area criterion is achieved either by ensuring that each individual measurement is made through a minimum area of 0.4cm 2 or by increasing the number of individual measurements.
  • Example 13 Test to Compare the MPF absorbance value of Chlorogloeopsis extract.

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Abstract

La présente invention concerne une composition d'hygiène personnelle qui comprend un extrait de microalgue de Chlorogloeopsis spp. et un vecteur topiquement acceptable associé. Les compositions sont utiles dans des procédés de prévention, d'amélioration ou de traitement, chez les mammifères, de lésions du tissu kératinique induites par les UV, par exemple dans une ou plusieurs des conditions cutanées suivantes : lésions cutanées induites par le photo-vieillissement, une pigmentation non homogène, les rides et un relâchement cutané.
PCT/GB2011/051138 2010-06-18 2011-06-17 Composition topique WO2011158041A2 (fr)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020231426A1 (fr) * 2019-05-15 2020-11-19 Algenol Biotech LLC Production d'acides aminés de type mycosporine utilisant des souches de production améliorées et de nouvelles enzymes

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Publication number Priority date Publication date Assignee Title
WO2000024369A1 (fr) 1998-10-23 2000-05-04 Nouvab Inc Composition de protection contre le rayonnement solaire
WO2002039974A1 (fr) 2000-11-17 2002-05-23 Natural Environment Research Council Compositions de soins personnels

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WO2000024369A1 (fr) 1998-10-23 2000-05-04 Nouvab Inc Composition de protection contre le rayonnement solaire
WO2002039974A1 (fr) 2000-11-17 2002-05-23 Natural Environment Research Council Compositions de soins personnels

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PORTWICH, A., F. GARCIA-PICHEL.: "Ultraviolet and osmotic stresses induce and regulate the synthesis of mycosporines in the cyanobacterium Chlorogloeopsis PCC 6912", ARCH. MICROBIOL, vol. 172, 1999, pages 187 - 192, XP002681240, DOI: doi:10.1007/s002030050759
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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020231426A1 (fr) * 2019-05-15 2020-11-19 Algenol Biotech LLC Production d'acides aminés de type mycosporine utilisant des souches de production améliorées et de nouvelles enzymes

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