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WO2016046848A2 - Nouvelle composition à base de principes actifs naturels concentrés dans une micro-émulsion huile dans eau utilisable en vue de la prévention de la chute des cheveux et du renforcement de la densité capillaire - Google Patents

Nouvelle composition à base de principes actifs naturels concentrés dans une micro-émulsion huile dans eau utilisable en vue de la prévention de la chute des cheveux et du renforcement de la densité capillaire Download PDF

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Publication number
WO2016046848A2
WO2016046848A2 PCT/IN2015/050119 IN2015050119W WO2016046848A2 WO 2016046848 A2 WO2016046848 A2 WO 2016046848A2 IN 2015050119 W IN2015050119 W IN 2015050119W WO 2016046848 A2 WO2016046848 A2 WO 2016046848A2
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Prior art keywords
extract
hair
mixture
agent
scalp
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WO2016046848A3 (fr
Inventor
Jigar Hasmukhbhai Patel
Nilay Bharatendu PANDYA
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Brillare Science Pvt Ltd
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Brillare Science Pvt Ltd
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/04—Dispersions; Emulsions
    • A61K8/06—Emulsions
    • A61K8/068—Microemulsions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34—Alcohols
    • A61K8/345—Alcohols containing more than one hydroxy group
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
    • A61K8/365—Hydroxycarboxylic acids; Ketocarboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/494—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom
    • A61K8/4953—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom containing pyrimidine ring derivatives, e.g. minoxidil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/60—Sugars; Derivatives thereof
    • A61K8/602—Glycosides, e.g. rutin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/64—Proteins; Peptides; Derivatives or degradation products thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/92—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
    • A61K8/922—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics 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
    • A61K8/9783—Angiosperms [Magnoliophyta]
    • A61K8/9789—Magnoliopsida [dicotyledons]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics 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
    • A61K8/9783—Angiosperms [Magnoliophyta]
    • A61K8/9794—Liliopsida [monocotyledons]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q5/00—Preparations for care of the hair
    • A61Q5/006—Antidandruff preparations
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q7/00—Preparations for affecting hair growth

Definitions

  • the present invention relates a novel oil in water based natural formulation for hair fall prevention prepared from plant actives in combination with other inert ingredients which also increase hair density. Further the natural formulation is stable oil in water microemulsion form with higher percentage of oils without adding any emulsifier.
  • Hair loss or hair fall results in to the baldness or alopecia in both men and women. It's a universal problem and affects social life as well as has psychological impact in life.
  • the three stages of hair growth are the anagen, catagen, and telogen phases.
  • Each strand of hair on the human body is at its own stage of development. Once the cycle is complete, it restarts and a new strand of hair begins to form.
  • the rate or speed of hair growth is about 1.25 cm or 0.5 inches per month, or about 15 cm or 6 inches per year.
  • the anagen phase is known as the growth phase. It begins in the papilla and can last from two to six years. The span at which the hair remains in this stage of growth is determined by genetics. The longer the hair stays in the anagen phase, the faster and longer it will grow. During this phase, the cells in the papilla divide to produce new hair fibers, and the follicle buries itself into the dermal layer of the skin to nourish the strand. About 85% of the hairs on one's head are in the anagen phase at any given time.
  • the catagen phase also known as the transitional phase, allows the follicle to, in a sense, renew itself. During this time, which lasts about two weeks, the hair follicle shrinks due to disintegration and the papilla detaches and "rests," cutting the hair strand off from its nourishing blood supply. Ultimately, the follicle is 1/6 its original length, causing the hair shaft to be pushed upward. While hair is not growing during this phase, the length of the terminal fibers increase when the follicle pushes them upward. Telogen phase
  • the follicle During the telogen, or resting, phase the follicle remains dormant anywhere from 1-4 months. Ten to fifteen percent of the hairs on one's head are in this phase of growth at any given time. In this phase the epidermal cells lining the follicle channel continue to grow as normal and may accumulate around the base of the hair, temporarily anchoring it in place and preserving the hair for its natural purpose without taxing the body's resources needed during the growth phase.
  • the follicle will begin to grow again, softening the anchor point of the shaft initially.
  • the hair base will break free from the root and the hair will be shed.
  • the new hair shaft will begin to emerge.
  • the anagen phase begins again once the telogen phase is complete.
  • the process results in normal hair loss known as shedding.
  • US20060029557 discloses a natural hair care composition comprising extract of flowers of plant Butea frondosa and/or stem bark of plant Butea parviflora, and/or the exudates of stem and root of plant Butea superba, and a cosmetically acceptable carrier. Also disclosed are methods for obtaining the plant extract and use thereof in regulation of hair growth and prevention of hair loss in all kinds of hair disorders.
  • US6495174 discloses a composition comprising alcoholic extracts of herbs Rhizoma Zinziberis Recens, Rhizoma pinelliae, Flos carthami, Radix rehmanniae, Radix angelicae sinensis, Radix paenoiae rubra, Cacumen biotae, Semen sesami nigruin, Radix polydoni multiflori, Fructus mori combined with Tincture Capsicum, Tincture Cantharidinate and Oleum Ricini for direct application to scalp for the treatment of all kinds of alopecia in humans.
  • US6447762 describes the preparation of a hair lotion for hair protecting action and prevention of hair loss comprising extracts of herbs Humulus lupulus, Rosmarinus officinalis and Swertia japonica and Silanodiol salicylate and other pharmaceutically acceptable carriers.
  • US6365199 discribes a hair growth formulation comprising of lemon peel extract including bioflavonoids membrane and castor oil.
  • US6451777 discloses a composition containing a compound from the group consisting of lupane triterpenes, derivatives of lupane, oleanane, ursane triterpenes and salts thereof for regulating hair growth and loss of hair.
  • US6358541 disclosed improved compositions comprising saw palmetto berry extract containing phytosterols and one or more low irritability constituents that enhance penetration of the extract into hair follicular pores, for the treatment of androgenetic alopecia.
  • US6203782 discloses methods and compositions for promoting hair growth, preventing or minimizing hair loss, enhancing or restoring hair color or remelanization and treating other hair and skin conditions.
  • the compositions include as an essential component a treatment agent in an amount effective for treating the condition, preferably selected from the class of herbs consisting of Foeniculum vulgares (fennel seed), Pimpinella anisum (anise), Carum carvi (caraway seeds) and mixtures thereof with each other and/or other herbs.
  • US5000949 discloses a hair grooming composition, which promotes scalp and hair health and growth, comprising petroleum jelly, an oil extract of cactus, glycerin and oil of clover or other odorant and method of producing the composition.
  • R.sub.2 represents a linear saturated or unsaturated hydrocarbon-based radical containing from 1 to 18 carbon atoms, or a branched or cyclic saturated or unsaturated hydrocarbon-based radical containing from 3 to 18 carbon atoms; and also an optical isomer thereof and/or a corresponding salt thereof, in a composition for caring for and/or making up keratin fibres, in particular human keratin fibres, for the purpose of inducing and/or stimulating the growth of the keratin fibres and/or of halting their loss and/or increasing their density.
  • US20120199152 discloses a composition for topical treatment of hair loss/alopecia including three natural, active ingredients, caffeine, saw palmetto berry extract, and epigallocatechin-3-gallate (EGCG).
  • the invention also provides methods for using this composition to treat hair loss.
  • US20130078301 describes method for stimulating hair growth includes providing a topical composition including a purified oil extract from Melaleuca alternifolia, also known as tea tree. The method may further include applying the topical composition to the skin surrounding the follicles of the human hair at least once a day.
  • a method for preventing the loss of human hair includes providing a topical composition including a purified oil extract from Melaleuca alternifolia, also known as tea tree. The method may further include applying the topical composition to the skin surrounding the follicles of the human hair at least once a day.
  • WO2014027363 describes an invention relates to an intra-dermally, sub-dermally or topically administrable growth factor concentrate derived from approximately 500 x 106 to 1500 [chi] 106 human platelets per ml for treating hair loss.
  • the concentrate comprises approximately 800 to 1200 pg/ml of Epidermal growth factor (EGF), 20 to 80 pg/ml of Vascular Endothelial growth factor (VEGF), 15 to 30 pg/ml of Basic fibroblast growth factor (b-FGF), 30000 to 40000 pg/ml of Transforming growth factor - [beta] (TGF- [beta]) and 100000 to 200000 pg/ml of Platelet Derived growth factor- AB (PDGF- AB).
  • EGF Epidermal growth factor
  • VEGF Vascular Endothelial growth factor
  • b-FGF Basic fibroblast growth factor
  • TGF- [beta] Transforming growth factor - [beta]
  • alopecia treatments for alopecia include hair transplantation, oral, and topical application of drugs and in some case natural solutions. Hair transplantation methods are usually painful, costly, and frequently result in an undesirable, unnatural appearance.
  • the predominant oral as well as topical preparations are chemical products such as Rogaine ® and Regaine ® , Propecia ® and Proscar ® ' Andolactone ® , Androcur ® , Eulexin ® .
  • oral contraceptives containing estrogens and/or estradiol
  • tretinoin tretinoin
  • azelaic acid drugs that have been the subject of scientific studies for their potential to enhance hair growth.
  • the inventors of the present inventions have surprisingly found that effective and stable oil in water type emulsion with high percentage of oils can be prepared from the active agents derived from natural sources and one more inert ingredient without any synthetic emulsifier.
  • One aspect of the present invention is to provide a novel oil in water based natural formulation comprising concentrated plant actives for prevention of hair fall and hair growth with increase in hair density which does not contain any emulsifier.
  • One aspect of the present invention is to provide a novel oil in water based natural formulation comprising of plant actives such as scalp purifying agent, hair nourishing complex, hair growth promoter, scalp anti-aging extract, exfoliating agent, hair growth stimulating agent, hair densifier complex, anti-dandruff agent, embedded in oil globules with neutralizer, preservatives, and optionally one or more inert ingredients, wherein the formulation is devoid of emulsifier.
  • plant actives such as scalp purifying agent, hair nourishing complex, hair growth promoter, scalp anti-aging extract, exfoliating agent, hair growth stimulating agent, hair densifier complex, anti-dandruff agent, embedded in oil globules with neutralizer, preservatives, and optionally one or more inert ingredients, wherein the formulation is devoid of emulsifier.
  • Yet another aspect of the present invention is to provide a novel oil in water based natural formulation comprising of emollient (Macadamia seed oil esters), scalp purifying agent (Mixture of caprylol glycine and xylitylglucoside), hair nourishing complex ((Mixture of Saccharum officinarum (Sugarcane) extract, citrus limon fruit (Lemon) extract, Betaine, Hexylene glycol, Pyrus malus (apple) fruit extract, Camellia sinensis leaf (Green tea leaf) extract and Hexapeptide -11) and/or (Mixture of Acetyl tetrapeptide-3 and trifolium pratense flower extract)), hair growth promoter (Pisum sativum sprout extract), scalp anti-aging extract (Pterocarpus marsupium bark extract), exfoliating agent (Glycolic acid), hair growth stimulating agent (Diaminopyrimidine oxide), hair densifier complex (Mixture of Ocimum basilicum hairy
  • One more aspect of the present invention is to provide a novel oil in water based natural formulation comprising 15 to 25 % of Emollient (Macadamia seed oil esters), 2.5 to 10% of Scalp purifying agent (Mixture of Capryloyl glycine and Xylitylglucoside), 5 to 20% of Hair nourishing complex ((Mixture of Saccharum officinarum (Sugarcane) extract, Citrus limon fruit (Lemon) extract, Betaine, Hexylene glycol, Pyrus malus (apple) fruit extract, Camellia sinensis leaf (Green tea leaf) extract and Hexapeptide -11) and/or (Mixture of Acetyl tetrapeptide-3 and Trifolium pratense flower extract)), 2 to 5% of Hair growth promoters (Pisum sativum sprout extract), 1 to 5% of Scalp anti-aging extract (Pterocarpus marsupium bark extract), 1 to 20% of Exfoliating agent (Glycolic acid), 1.00
  • Hair densifier complex Mention of Ocimum basilicum hairy root culture ethanolic extract, Helianthus annuus seed oil, Cocos nucifera oil
  • Anti-dandruff agent Pig nigrum fruit extract
  • Scalp warning agent Vanillyl butyl ether
  • Neutralizer 0.45 to 2.00% of Preservatives and optionally one or more inert ingredients, wherein the formulation is devoid of emulsifier.
  • Yet One more aspect of the present invention is to provide a novel oil in water based natural formulation comprising 15 to 25 % of Emollient (Macadamia seed oil esters), 2.5 to 10% of Scalp purifying agent (Mixture of Capryloyl glycine and Xylitylglucoside), 5 to 20% of Hair nourishing complex ((Mixture of Saccharum officinarum (Sugarcane) extract, Citrus limon fruit (Lemon) extract, Betaine, Hexylene glycol, Pyrus malus (apple) fruit extract, Camellia sinensis leaf (Green tea leaf) extract and Hexapeptide -11) and/or (Mixture of Acetyl tetrapeptide-3 and trifolium pratense flower extract)), 2 to 5% of Hair growth promoters (Pisum sativum sprout extract), 1 to 5% of Scalp anti-aging extract (Pterocarpus marsupium bark extract), 1 to 20% of Exfoliating agent (Glycolic acid), 1
  • Hair densifier complex (Ocimum basilicum hairy root culture ethanolic extract, Helianthus annuus seed oil, Cocos nucifera oil), 0.2 to 1% of Anti-dandruff agent (Piper nigrum fruit extract), 0.01 to 1.00% of Scalp warning agent (Vanillyl butyl ether), 0.2 to 1.5% of Neutralizer, 0.45 to 2.00 of Preservatives and optionally one or more inert ingredients, wherein hair densifier complex comprises 0.1 to 10% Ocimum basilicum hairy root culture ethanolic extract, 50 to 80% of Helianthus annus seed oil and 20 to 40% of Cocos nucifera oil, while scalp purifying complex comprises of mixture of 10 to 15% of Capryloyl glycine and 25 to 50% of Xylityl glucoside, while hair nourishing complex comprises mixture of 14 to 16 % of Saccharum officinarum (Sugarcane) extract, 8.4 to 9.6% of Citrus limon
  • One more aspect of the present invention is to provide a novel oil in water based natural formulation comprising about 20% of Emollient (Macadamia seed oil esters), 10% of Scalp purifying agent (Mixture of Capryloyl glycine and Xylitylglucoside), 5% of Hair nourishing complex ((Mixture of Saccharum officinarum (Sugarcane) extract, Citrus limon fruit (Lemon) extract, Betaine, Hexylene glycol, Pyrus malus (apple) fruit extract, Camellia sinensis leaf (Green tea leaf) extract and Hexapeptide -11) and/or (Mixture of Acetyl tetrapeptide-3 and Trifolium pratense flower extract)), 4% of Hair growth promoters (Pisum sativum sprout extract), 2 % of Scalp anti-aging extract (Pterocarpus marsupium bark extract), 1.5 % of alpha hydroxy acid (Glycolic acid), 1.5% of Hair growth stimulating agent (Diamin
  • hair densifier complex (Ocimum basilicum hairy root culture ethanolic extract, Helianthus annuus seed oil, Cocos nucifera oil), 1% of Anti-dandruff agent (Piper nigrum fruit extract), 0.3% of Scalp warning agent (Vanillyl butyl ether), 1% of neutralizer, 1.05% of preservatives (0.7% of Phenoxyethanol, 0.2% of Sodium benzoate, 0.15% of Potassium sorbate) and optionally one or more inert ingredients, wherein hair densifier complex comprises 0.1 to 10% Ocimum basilicum hairy root culture ethanolic extract, 50 to 80% of Helianthus annus seed oil and 20 to 40% of Cocos nucifera oil, while scalp purifying complex comprises of mixture of 10 to 15% of Capryloyl glycine and 35 to 50% of Xylityl glucoside, while hair nourishing complex comprises mixture of 14 to 16 % of Saccharum officinarum (Sugarcane)
  • Yet another aspect of the present invention is to provide a process for preparing novel oil in water based natural formulation comprising the steps of
  • step 2) Adding the mixture of step 2) to step 1) with stirring for 30 minutes till proper emulsion will form.
  • exfoliating agent Glycolic acid
  • neutralizer Triethanolamine
  • step 6 Adding scalp purifying agent (Mixture of Capryloyl glycine and Xylityl glucoside) into the mixture of step 5) with stirring for 15 minutes. 7. Add step by step, hair nourishing complex (Mixture of Saccharum officinarum extract, citrus limon extract, Betaine, Hexylene glycol, pyrus malus fruit extract, Camellia sinensis leaf extract and Hexapeptide -11) in a mixture of step 6) with stirring for 15 minutes.
  • scalp purifying agent Mention of Capryloyl glycine and Xylityl glucoside
  • step 7 Add step by step, hair nourishing complex (Mixture of Saccharum officinarum extract, citrus limon extract, Betaine, Hexylene glycol, pyrus malus fruit extract, Camellia sinensis leaf extract and Hexapeptide -11) in a mixture of step 6) with stirring for 15 minutes.
  • step by step Add step by step, hair nourishing complex (Mixture of Acetyl tetrapeptide-3 and trifolium pratense flower extract) with stirring for 15 minutes.
  • Yet one more aspect of the present invention is to provide a novel oil in water based natural formulation for the prevention of hair fall and for hair growth in human being with increase in hair density.
  • the instant invention of the present invention provides a novel oil in water based natural formulation comprising active ingredients derived from natural sources.
  • the present invention provides oil in water based natural formulation for the prevention of hair fall in human being and at the same time for growth of hair with increase in hair density.
  • natural or “herbal” as used herein refer to any phytochemical or mixture thereof that is obtained, isolated, and/or derived from one or more extracts of plant material(s) or essential oil(s) thereof.
  • plant material refers to any plant material including, but not limited to, leaves, hark, stems, flowers, fruits, seeds, roots, and combinations thereof.
  • naturally and “herbal” can be used interchangeably.
  • formulation means oil in water based formulation and can be selected from emulsion, suspension, solution. Preferred is emulsion with more preferred is microemulsion.
  • Microemulsions are clear, thermodynamically stable, isotropic liquid mixtures of oil, water with the help of emulsifier. In contrast to ordinary emulsions, microemulsions form upon simple mixing of the components and do not require the high shear conditions generally used in the formation of ordinary emulsions.
  • the three basic types of microemulsions are direct (oil dispersed in water, o/w), reversed (water dispersed in oil, w/o) and bicontinuous.
  • the present invention is oil in water based micro emulsion wherein the plant active which is in oil form is dispersed in aqueous phase and get embedded in oil globule form in aqueous phase.
  • the inventors of the present invention have surprisingly found that the microemulsion of the plant active can be prepared by specific selection of inert ingredients without adding any emulsifier.
  • the formulation of present invention can be used for treatment of prevention of hair fall and growth of hair in human beings with increase in hair density.
  • the novel oil in water based formulation as provided herein is effective combination of plant actives derived from natural sources which provide the end results without any undesirable side effects and further the provided formulation is stable.
  • Yet another advantage of the formulation of present invention is although there is higher % of oil present, the viscosity of the final formulation is lower which provides the ease in application and spreadability on scalp.
  • the present invention is in the form of oil in water formulation with higher amount of plant active which is in oil form but does not contain any emulsifier and yet stable and effective for prevention of hair fall and stimulates hair growth.
  • the novel formulation of the present invention comprises novel Emollient (Macadamia seed oil esters), Scalp purifying agent (Mixture of caprylol glycine and xylitylglucoside), Hair nourishing complex ((Mixture of Saccharum officinarum (Sugarcane) extract, citrus limon fruit (Lemon) extract, Betaine, Hexylene glycol, Pyrus malus (apple) fruit extract, Camellia sinensis leaf (Green tea leaf) extract and Hexapeptide -11) and/or (Mixture of Acetyl tetrapeptide-3 and trifolium pratense flower extract)) Hair growth promoter (Pisum sativum sprout extract), Scalp anti-aging extract (Pterocarpus marsupium bark extract), Exfoliating agent (Glycolic acid), Hair growth stimulating agent (Diaminopyrimidine oxide), Hair densifier complex (Mixture of Ocimum basilicum hairy root culture ethanolic extract, Helianthus annuus
  • Inert ingredient as used herein means any ingredients which do not have any therapeutic or biological effect and can be mixed with any other therapeutic active ingredient without causing any undesirable biological effects or interacting in a deleterious manner with any of the other ingredients of the formulation in which it is contained.
  • Inert ingredient which can be used for the natural formulation of the present invention can be selected from the group consisting of neutralizer, preservatives, fragrances, coloring agent and carrier.
  • Plant actives as used herein means the active ingredient derived from plant.
  • the plant actives are emollient, hair nourishing complex, hair growth promoter, scalp anti- aging extract, hair densifier complex, and anti-dandruff agent.
  • Macadamia ternifolia Water dispersible Macadamia oil esters (Macadamia ternifolia) is having with emollient, skin soothing, purifying and nourishing properties of macadamia oil. As per the present invention, Macadamia oil esters can be used in the range of 15 to 25%. b) Hair nourishing complex
  • Hair nourishing complexes are made up of one or more ingredients having a hair nourishing properties. There are two complexes, which can be used as hair nourishing complex.
  • Hexylene glycol, Pyrus malus (Apple) fruit extract, Camellia sinensis leaf (Green tea leaf extract) and Hexapeptide -11 It is a mixture of different plant derived extracts such as Saccharum officinarum extract, Citrus limon extract, Betaine, Hexylene glycol, Pyrus malus fruit extract, Camellia sinensis leaf extract as well as biofermented peptide. This complex mixture improves health of hair follicle, increase penetration of actives through follicle, and reduces hair loss.
  • Preferably it comprises of mixture of 14 to 16 % of Saccharum officinarum (Sugarcane) extract, 8.4 to 9.6% of Citrus limon fruit (Lemon) extract, 8 of 12% of Betaine, 8 to 12% of Hexylene glycol,
  • Fruit extracts isolated from sugar cane offer natural exfoliating action through the action of a- hydroxy acids promoting cell renewal on the scalp. This helps clear the follicles of excessive buildup of dead cells, allowing more thicker hair growth.
  • Betaine is also known to be part of the important cascades for cellular production of ATP, the energy molecule of every living cell. Betaine has been shown in vitro to stimulate the production of collagen in human dermal fibroblasts. Improving the production of collagen in the skin helps to strengthen the extracellular matrix where the hair bulb principally resides.
  • Enhancing the energy cascades of the hair bulb improves the ability of the hair to function during the anagen or growth cycle of the hair fiber.
  • Hexapeptide- 11 is a biofermented peptide which able to upregulate the Androgen Receptor gene (AR) indicating that the peptide appears capable of binding to the Androgen Receptor much the way testosterone will. This suggests that Hexapeptide- 11 may be able to influence the principal biochemical pathways responsible for converting young velus hair into mature terminal hair.
  • AR Androgen Receptor gene
  • biomimetic peptide acetyl tetrapeptide-3
  • red clover extract a red clover extract
  • a biomimetic peptide (acetyl tetrapeptide-3) combined with a red clover extract rich in Biochanin A. its efficacy is based on the association and synergistic action of its two ingredients. Mixture shows direct action on 5a-reductase enzyme which is responsible for formation of
  • DHT Dihydrotestosterone
  • Extracellular matrix proteins such as collagen type III and anchoring fibers such as laminin and collagen VII which will favor a good hair anchoring in the hair bulb surrounding tissue.
  • Mixture of acetyl tetrapeptide-3 and Trifolium pranse (clover) flower extract can be used in the range of 0.5 to 5%.
  • Hair growth promoter Pig sativum sprout extract
  • An aqueous extract based on sprouts of organic pea which reduces hair loss by inducing dermal papilla cells to reactivate hair growth especially in the anagen phase.
  • Pisum sativum sprout extract can be used in the range of 2 to 5%.
  • Scalp anti aging extract Panocarpus marsupium extract
  • Scalp anti aging extract can be used in the range of 2 to 10%.
  • Hair densifier complex ocimum basilicum hairy root culture ethanolic extract, helianthus annuus seed oil and cocos nucifera oil
  • Hair densifier complex is made up of one or more ingredients having hair densifying property.
  • Preferred are ocimum basilicum hairy root culture ethanolic extract, helianthus annuus seed oil and cocos nucifera oil.
  • the hair densifier complex comprises 0.1 to 10% of ocimum basilicum hairy root culture 20 ethanolic extract, 50 to 80% of helianthus annuus seed oil and 20 to 40% of cocos nucifera oil.
  • This complex mixture shows inhibitory effect on 5 a Reductase enzyme, which is mainly responsible for hair loss.
  • An extract from a hairy root culture from basil helps reduce hair loss by inhibiting 5 a reductase activity and by stimulating dermal papilla cells.
  • Helianthus annuus oil is extracted from the seeds of the sunflower, Helianthus annuus and used as skin conditioning agent having emollient property. Cocos nucifera oil
  • Coconut oil is extracted from the kernels of the seeds of coconot palm, Cocos nucifera.
  • Conditioning agent, Emollient, Masking Solvent Hair densifier complex can be used in the range of 0.5 to 1.5 %, preferably 1% of the total formulation f) Anti-dandruff agent (Piper Nigrum fruit (black paper) extract)
  • Extract of Piper Nigrum fruit black paper extract titrated in Piperine having anti dandruff, Anti- Inflammatory and Soothing Property.
  • piper nigrum fruit extract can be used in the range of 0.5 to 1.5%, preferably from 0.75 to 1.25% and most preferred is 1%.
  • Scalp purifying agent can be used in the range of 2.5 to 10%.
  • Glycolic Acid (hydroxyacetic acid) is the first member of the series of alpha-hydroxy carboxylic acids, which means it is one of the smallest organic molecules with both acid and alcohol functionality.
  • Glycolic Acid occurs naturally as a trace component in sugarcane, beets, grapes and fruits. It is mainly used for chemical peeling.
  • Glycolic acid can be used in the range of 1 to 20%. Preferably 1 to 10% and most preferred is 1.5%.
  • Other ingredients that can be used in place of glycolic acid are citric acid, stearic acid and palmitic acid.
  • Neutralizer can be selected from the group consisting of monoethanolamine, diethanolamine, triethanolamine, monopropanolamine, dipropanolamine, tripropanolamine, 2-amino-2-methyl-l ,3- propanediol, 2-amino-2-methyl-l -propanol, 2-amino-2-hydroxymethyl-l ,3- propanediol and mixtures thereof. Preferred one is triethanolamine. As per the present invention, Neutralizer can be used in the range of 0.2 to 1.5%, preferably 1%. d) Hair growth stimulating agent (Diaminopyrimidine oxide)
  • Hair growth stimulating agent as used herein means an agent that promotes the hair growth.
  • the hair growth stimulating agent for the purpose of present invention is Diaminopyrimidine oxide.
  • the hair growth stimulating agent promotes the proliferation of dermal papillae cells that control the hair cycle and also effectively retard hair loss and stimulate new hair growth.
  • hair growth stimulating agent can be used in the range of 0.2 to 1.5%. Preferably in the range of 1.0 to 1.5% and most prefer is 0.2%. e) Preservatives
  • Preservatives as used for the present invention is selected from the group consisting of sodium benzoate, potassium sorbate and Phenoxyethanol the other example are phenoxyethanol, methyl chloroisothiazolinone & methylisothiazolinone, gluconolactone, benzyl alcohol, DMDM Hydantoin, benzethonium chloride,sodium benzoate, dehydroacetic acid, chlorhexidine digluconate, methyl paraben, propyl paraben, butyl paraben, sodium methyl paraben, sodium propyl paraben, Diazodinyl urea.
  • Preferred is combination of sodium benzoate, potassium benzoate and phenoxyethanol.
  • the functional group of Vanillyl butyl ether is called the vanillyl group. It plays the main role in inducing the warming sensation via the nervous system, it enhances microcirculation and boosts delivery of nutrients and oxygen to the hair follicles.
  • the scalp warming agent can be used in the range of 0.01 to 1%.
  • Fragrance All types of individual & combination of following can be used fragrances. Citrus fragrances, berries fragrances, stone fruits fragrances, pip fruits fragrances, botanicals fragrances, cereals fragrances, tea fragrances, alcoholic fragrances, floral fragrances. h) Coloring agent
  • Water soluble and water insoluble grades of Colouring agent are Ponceau 4r, Brilliant blue, Indigo carmine, Carmine red colour, Sunset yellow, Quinoline yellow, Tartrazine, Erythrosine.
  • Dissolving hair growth stimulating agent (Diaminopyrimidine oxide) and hair growth promoter (Pisum sprout extract) in purified water by stirring.
  • Dissolving anti-dandruff agent (Piper nigrum fruit extract) and hair densifier complex (mixture of Ocimum basilicum hairy root cluture ethanolic extract, Helianthus annuus seed oil and Cocos nucifera oil) in to macadamia seed oil esters with stirring.
  • step 2) Adding the mixture of step 2) to step 1) with stirring for 30 minutes till proper emulsion will formed. 4. Adding gradually Scalp anti-aging extract (Pterocarpus marsupium bark extract), Preservatives
  • exfoliating agent Glycolic acid
  • Neutralizer Triethanolamine
  • step 7 Add step by step, hair nourishing complex (Mixture of Saccharum officinarum extract, citrus limon extract, Betaine, Hexylene glycol, pyrus malus fruit extract, Camellia sinensis leaf extract and Hexapeptide -11) in a mixture of step 6) with stirring for 15 minutes.
  • hair nourishing complex Menture of Saccharum officinarum extract, citrus limon extract, Betaine, Hexylene glycol, pyrus malus fruit extract, Camellia sinensis leaf extract and Hexapeptide -11
  • step by step Add step by step, hair nourishing complex (Mixture of Acetyl tetrapeptide-3 and trifolium pratense flower extract) with stirring for 15 minutes.
  • Dissolving anti-dandruff agent Pig nigrum fruit extract
  • Scalp warming agent Vanillyl butyl ether
  • hair densifier complex mixture of Ocimum basilicum hairy root cluture ethanolic extract, Helianthus annuus seed oil and Cocos nucifera oil
  • step 2) Adding the mixture of step 2) to step 1) with stirring for 30 minutes till proper emulsion will form.
  • step 6 Add step by step, hair nourishing complex (Saccharum officinarum extract, citrus limon extract, Betaine, Hexylene glycol, pyrus malus fruit extract, Camellia sinensis leaf extract and Hexapeptide -11) in a mixture of step 5) with stirring for 15 minutes.
  • hair nourishing complex sacharum officinarum extract, citrus limon extract, Betaine, Hexylene glycol, pyrus malus fruit extract, Camellia sinensis leaf extract and Hexapeptide -11
  • step by step Add step by step, hair nourishing complex (Acetyl tetrapeptide-3 and trifolium pratense flower extract) with stirring for 15 minutes.
  • hair nourishing complex Acetyl tetrapeptide-3 and trifolium pratense flower extract
  • Clarity Clear, Light to Dark yellow coloured, Transparent liquid with pleasant odor

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Abstract

La présente invention concerne une nouvelle composition naturelle de type émulsion huile dans eau utilisable en vue de la prévention de la chute des cheveux et favorisant la pousse des cheveux avec une augmentation de la densité capillaire, préparée à partir d'ingrédients d'origine naturelle, soit seuls, soit en combinaison avec d'autres ingrédients inertes. En outre, cette composition naturelle forme une microémulsion huile dans eau stable présentant un pourcentage plus élevé d'huiles, et ce, sans émulsifiant.
PCT/IN2015/050119 2014-09-26 2015-09-23 Nouvelle composition à base de principes actifs naturels concentrés dans une micro-émulsion huile dans eau utilisable en vue de la prévention de la chute des cheveux et du renforcement de la densité capillaire Ceased WO2016046848A2 (fr)

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US10493011B2 (en) 2017-08-03 2019-12-03 ALASTIN Skincare, Inc. Peptide compositions and methods for ameliorating skin laxity and body contour
CN110972954A (zh) * 2019-12-30 2020-04-10 内蒙古民族大学 一种红车轴草毛状根的诱导方法及增殖方法
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CN112107528A (zh) * 2020-09-22 2020-12-22 沧州明辰生物科技有限公司 一种改善头皮毛囊精华液及其制作方法
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US11103455B2 (en) 2018-08-02 2021-08-31 ALASTIN Skincare, Inc. Liposomal compositions and methods of use
WO2022221491A1 (fr) * 2021-04-14 2022-10-20 Virtue Labs, LLC Compositions de traitement capillaire et procédés d'utilisation
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WO2024212124A1 (fr) * 2023-04-12 2024-10-17 Henkel Ag & Co. Kgaa Composition pour améliorer la santé du cuir chevelu, et procédé pour améliorer la santé du cuir chevelu l'utilisant
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KR100992565B1 (ko) * 2005-10-17 2010-11-08 (주)아모레퍼시픽 모발 성장 촉진용 외용제 조성물
JP2011511787A (ja) * 2008-02-29 2011-04-14 ザ プロクター アンド ギャンブル カンパニー 毛髪ケア組成物及び毛髪直径を増大させかつ追加利益を送達する方法

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US10086035B2 (en) 2016-02-04 2018-10-02 ALASTIN Skincare, Inc. Compositions and methods for invasive and non-invasive procedural skincare
US11426443B2 (en) 2016-02-04 2022-08-30 ALASTIN Skincare, Inc. Compositions and methods for invasive and non-invasive procedural skincare
US10688147B2 (en) 2016-02-04 2020-06-23 ALASTIN Skincare, Inc. Compositions and methods for invasive and non-invasive procedural skincare
US11752084B2 (en) 2017-08-03 2023-09-12 ALASTIN Skincare, Inc. Methods for fat reduction or elimination of lipid droplets
US10493011B2 (en) 2017-08-03 2019-12-03 ALASTIN Skincare, Inc. Peptide compositions and methods for ameliorating skin laxity and body contour
US11052032B2 (en) 2017-08-03 2021-07-06 ALASTIN Skincare, Inc. Peptide compositions and methods for ameliorating skin laxity and body contour
CN109846765A (zh) * 2017-11-30 2019-06-07 赵茹伊 一种生发精华
US12053547B2 (en) 2018-08-02 2024-08-06 ALASTIN Skincare, Inc. Liposomal compositions and methods of use
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KR102141574B1 (ko) * 2020-03-20 2020-08-05 주식회사 세리화장품 두피케어 화장료 조성물 및 그 제조방법
CN112107528A (zh) * 2020-09-22 2020-12-22 沧州明辰生物科技有限公司 一种改善头皮毛囊精华液及其制作方法
WO2022221491A1 (fr) * 2021-04-14 2022-10-20 Virtue Labs, LLC Compositions de traitement capillaire et procédés d'utilisation
CN113318043A (zh) * 2021-05-21 2021-08-31 广州市涵美化妆品有限公司 一种具有固发、生发功效的精华液及其制备方法
CN115887319A (zh) * 2022-11-08 2023-04-04 广州市中通生化制品有限公司 一种滋养皮肤防脱固发高山植物组合物及其精华液与制备方法
WO2024212124A1 (fr) * 2023-04-12 2024-10-17 Henkel Ag & Co. Kgaa Composition pour améliorer la santé du cuir chevelu, et procédé pour améliorer la santé du cuir chevelu l'utilisant
FR3160317A1 (fr) * 2024-03-21 2025-09-26 Amélie MECHKATI Composition capillaire à base d’extraits végétaux

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