Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K38/00—Medicinal preparations containing peptides
  • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
  • A61K38/43—Enzymes; Proenzymes; Derivatives thereof
  • A61K38/46—Hydrolases (3)
  • A61K38/48—Hydrolases (3) acting on peptide bonds (3.4)
  • A61K38/4886—Metalloendopeptidases (3.4.24), e.g. collagenase
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
  • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
  • A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/02—Algae
  • A61K36/03—Phaeophycota or phaeophyta (brown algae), e.g. Fucus
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/18—Magnoliophyta (angiosperms)
  • A61K36/185—Magnoliopsida (dicotyledons)
  • A61K36/25—Araliaceae (Ginseng family), e.g. ivy, aralia, schefflera or tetrapanax
  • A61K36/258—Panax (ginseng)
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/18—Magnoliophyta (angiosperms)
  • A61K36/185—Magnoliopsida (dicotyledons)
  • A61K36/48—Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
  • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
• • 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
  • A61K8/66—Enzymes
• • 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
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/0012—Galenical forms characterised by the site of application
  • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P17/00—Drugs for dermatological disorders
  • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• • 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
• • B—PERFORMING OPERATIONS; TRANSPORTING
  • B05—SPRAYING OR ATOMISING IN GENERAL; APPLYING FLUENT MATERIALS TO SURFACES, IN GENERAL
  • B05B—SPRAYING APPARATUS; ATOMISING APPARATUS; NOZZLES
  • B05B11/00—Single-unit hand-held apparatus in which flow of contents is produced by the muscular force of the operator at the moment of use
  • B05B11/01—Single-unit hand-held apparatus in which flow of contents is produced by the muscular force of the operator at the moment of use characterised by the means producing the flow
  • B05B11/10—Pump arrangements for transferring the contents from the container to a pump chamber by a sucking effect and forcing the contents out through the dispensing nozzle
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
  • A61K2800/74—Biological properties of particular ingredients
  • A61K2800/78—Enzyme modulators, e.g. Enzyme agonists
  • A61K2800/782—Enzyme inhibitors; Enzyme antagonists
• • C—CHEMISTRY; METALLURGY
  • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
  • C12Y—ENZYMES
  • C12Y304/00—Hydrolases acting on peptide bonds, i.e. peptidases (3.4)
  • C12Y304/24—Metalloendopeptidases (3.4.24)
  • C12Y304/24066—Choriolysin L (3.4.24.66)

Definitions

• the present invention in general relates to a formulation for promoting hair retention, and in particular to a formulation and process for the use thereof to provide a more efficient usage of follicle health-promoting agents.
• the anatomy of the hair follicle includes the outermost layer of corneum stratum that has dead and dying dermal cells that form a constriction around the protruding hair shaft. Sebaceous secretions also coat the hair shaft and render the path a topical hair retention agent must take to reach the follicle physically blocked and hydrophobic.
• Prior art attempts to administer active agents to the follicle basal cells using emulsions have met with limited success owing to the user displeasure with the application of this type of vehicle to the scalp.
• emulsions are known to change topical delivery kinetics of active agents (S.Y. E. Hou et al. "Phase volume and partitioning effects on drug delivery from topical emulsions"; International Journal of Pharmaceutics, 66 (1990) 79-85).
• a formulation includes a hair retention-promoting substance and an enzyme that is a peptidase or lipase, where the enzyme is active in exfoliating a human scalp.
• the substance and the enzyme are present in an aqueous carrier having a pH that maintains activity of the enzyme.
• a process is provided for enzymatically exfoliating the scalp of a subject for the purpose of promoting hair retention on the subject's scalp.
• a hair retention-promoting substance is topically administered to the scalp of the subject after, or in concert with, the exfoliation of the scalp.
• a kit is also provided for performing the process with a first exfoliating phase and a second hair retention-promoting phase, where the two formulations are packaged separately; or alternatively the kit may contain a combined formulation containing both the exfoliating enzyme and the hair retention-promoting substance.
• the kit also contains instructions for using the components to achieve the desired hair retention.
• the present invention has utility in promoting hair retention. Whether scalp exfoliation precedes administration of a hair retention-promoting substance, or the two steps are carried out together, e.g., by administration in a formulation containing both the exfoliating agent and the hair retention-promoting substance, enhanced hair retention promotion is accomplished, as compared to administration of the hair retention-promoting substance without exfoliation.
• exfoliation associated with mechanical abrasion or chemical peeling causes inflammation to the scalp that appears to counteract many of the benefits associated with inventive exfoliation.
• Chemical peel exfoliation is most often associated with the usage of compounds illustratively including glycolic acid and retinoic acid.
• the present invention relies on an enzymatic scalp exfoliant that allows hair retention promoting substance to penetrate around the hair fiber to the papilla. Limiting of inflammation associated with exfoliation appears to promote hair retention promoting substance efficacy.
• range is intended to encompass not only the end point values of the range, but also individual intermediate values and intermediate ranges within the range
• a recited range of from 1 to 4 is intended to include not only 1-4, but also 1, 2, 3, 4, 1-2, 1-3, 2-4, and 3-4.
• an active enzyme that has an exfoliating effect on human corneum stratum.
• the active enzyme is in an aqueous carrier that maintains activity of the enzyme during storage.
• Peptidase enzymes, lipase enzymes and combinations thereof are active enzymes in an inventive formulation and illustratively include trypsin, bromelain, papain, proteins active in natural degrading of egg zona (synonymously referred to herein as egg hatching active proteins), and combinations thereof.
• Specific egg hatching active proteins operative herein include fish spawn proteins such as zonase (a serine protease) and choriolysin (a zinc protease). It is appreciated that the quantity of active protein present depends on factors illustratively including aqueous carrier pH, enzyme specificity, enzyme activity, carrier viscosity, and enzyme half- life.
• a peptidase is defined as an enzyme that catalyzes hydrolysis of a peptide bond that links two amino acids together in a polypeptide chain.
• the term "peptidase” is used herein synonymously with “protease” and "proteinase”.
• a fish spawn protein isolate for example, includes a zonase, a leukolectin, a choriolysin, or a combination thereof, and has the properties detailed in U.S. 6,346,245, col. 4, line 15-col. 5, line 8; U.S. 2009/0274770 Al [0321]-[0326] and U.S. 2011/0280882 [0157]- [0194]; crude extracts containing such proteins; and combinations thereof.
• Exemplary sources of fish spawn for protein isolation include roes from sturgeon, salmon, whitefish, vendace, cod, capelin, and burbot.
• an egg- or, with particularity, fish spawn protein- isolate containing at least one of the above recited proteins constitutes from 0.1 to 10% total weight of an inventive formulation, with 0.00001 to 10 percent of the extract being active protein.
• a given active protein may constitute 1 x 10 "8 to 1 x 10 "5 total weight percent of the formulation (i.e., 0.00001 to 10 percent of the extract is the protein, and the extract is 0.1% total weight of the formulation).
• the amount of protein present in an inventive cosmetic depends on factors illustratively including miscibility with other components.
• the active enzyme in the aqueous carrier is readily applied to the scalp in certain inventive embodiments as a first treatment step.
• the enzyme produces a non-inflammatory exfoliation in and around the hair follicle.
• the active enzyme is part of a single formulation that also contains the hair retention-promoting substance.
• Typical loadings of active enzyme range from 0.000001 to 1,000 enzyme units (U) per liter, where an enzyme unit corresponds to one micromole of substrate converted per minute.
• U enzyme units
• an in vitro assay can be carried out using an oligopeptide substrate that represents the target protein(s) of corneum stratum.
• the oligopeptide is chromogenic, and cleavage thereof by the enzyme produces a detectable color change.
• aqueous carrier pH is readily tailored to modify peptidase enzymatic activity
• typical aqueous carrier pH values range from 6 to 8 for many peptidase enzymes operative herein.
• Exemplary of peptidases active in this pH range are zonase and trypsin.
• an inventive formulation includes the peptidase enzyme and a hair retention-promoting substance combined in an aqueous carrier. It is appreciated that an inventive formulation containing both the active enzyme and the hair retention-promoting substance facilitates user compliance, as only a single formulation need be applied. In some embodiments, the formulation (or both formulations, when separate formulations are used) may conveniently be applied as a leave-in spray solution, which also facilitates user compliance.
• the present invention is practiced as an exfoliating enzymatic step and a separate hair retention-promoting substance step, or if these two steps are combined into one by using a single formulation containing both active ingredients
• application to the scalp typically occurs on a regime of once a week, 2-6 days per week, once daily, or even two or three times daily.
• the timing and frequency of the first can vary from the timing and frequency of the second.
• multiple doses of hair retention-promoting substance may be applied (e.g., once per day for multiple days) before the exfoliation step is repeated. It may be sufficient to do only occasional maintenance application of the enzymatic exfoliant.
• a hair retention-promoting substance is defined as a substance that promotes hair retention and is a purified organic compound, a natural product extract containing one or more such compounds, or a synthetic compound.
• the substance may be, for example, an inhibitor of prostaglandin-D2 or an inhibitor of dihydro -testosterone. It is appreciated that many natural product extracts, including some that contain polyphenols, have been shown to be effective in promoting hair retention.
• Specific hair retention-promoting substances operative herein illustratively include minoxidil, red ginseng extract, hesperidin extract, green pea shoot extracts, synthetic oligopeptides sold under the tradename SymPeptideTM, and combinations thereof.
• hair retention-promoting substances are typically used in an inventive formulation from 0.001 to 1 total weight percent, but can be up to 10 total weight percent, e.g., where the extract contains a relatively low concentration of active agent.
• An inventive formulation is readily formulated as a water based solution or as an emulsion containing an aqueous carrier phase for the enzymes. It is appreciated that some hair retention- promoting substances are lipophilic, while others are hydrophilic. Lipophilic hair retention- promoting substances are readily formulated as a two-phase formulation with a solvent appropriate for dissolution or suspension of the hair retention-promoting substance.
• the solvents illustratively include skin-compatible alcohols, ketones, esters, aldehydes, ethers, alkanes, alkenes, alkylated sulfoxides; cyclics of any of the aforementioned; fluorinated analogs of any of the aforementioned; and combinations thereof.
• Specific solvents for certain hair retention- promoting substances illustratively include water, ethanol, isopropanol, acetone, glycols, alkoxylated glycols, diethyl ether, pentane, hexane, dimethyl sulfoxide, and combinations thereof.
• lipophilic hair retention-promoting substances are present in an oil phase of an oil- in- water or water-in-oil emulsion.
• an anti-inflammatory agent is included in an enzyme and hair retention-promoting substance combined formulation, or in one or both parts of a two-formulation embodiment (one formulation containing the active enzyme and the other formulation containing the hair retention-promoting substance.
• Anti-inflammatory agents operative herein illustratively include steroidal anti- inflammatory agents; non-steroidal antiinflammatory agents; extracts of plants such as turmeric, oregano, garlic, green tea, blueberries, neem, holy basil oil, licorice, ashwaganda, raspberry leaf, St. John's Wort, chamomile, and ginger; omega fatty acids; alpha-linolenic acid; and combinations thereof.
• an antioxidant may be included in a mixed enzyme and hair retention-promoting formulation, or in one or both parts of a two-formulation embodiment.
• Antioxidants operative herein illustratively include alpha lipoic acid, beta-glucan, coenzyme Q10, grape seed extract, oat extract, chamolime, green tea, soybean sterols, superoxide dismutase, vitamin C (e.g., in the form of ascorbyl palmitate, magnesium ascorbyl palmitate, or ascorbic acid 2-gluconate), and vitamin E (e.g., alpha tocopherol or a tocotrienol), and combinations thereof. It is appreciated that a number of anti-inflammatory agents possess antioxidant properties.
• the formulations of the invention that include such an anti-inflammatory agent may also include a separate antioxidant compound.
• a formulation or a single component thereof is provided that is essentially free of synthetic compounds.
• a formulation or a single part thereof is provided that is certified organic.
• a single, mixed formulation containing both the peptidase enzyme and the hair retention-promoting substance in an aqueous solution that is suited for use as leave-in scalp spray or wash.
• aqueous carrier evaporates, it leaves the active enzyme and substance in contact with the scalp.
• a process of formulation includes the buffering of any constituent phase containing the enzyme(s) to a pH of between 5 and 8 prior to introduction of enzyme to that phase.
• Buffering is commonly practiced in the field and includes the addition of an acid, a base, a salt of an acid, or a combination thereof to equilibrate an aqueous solution or aqueous phase of an emulsion to a desired pH. It is appreciated that pH measurement is routine. pH may be measured quantitatively via volumetric titration or with potentiometric electrodes such as those commercially available from Thermo Fisher Scientific (Waltham MA, USA), or qualitatively with litmus paper kits.
• Biocides are present in some inventive embodiments.
• a biocide helps maintain product quality by inhibiting growth of microorganisms introduced during formulation of the product or during use thereof, particularly when the product is packaged in multiple-use packaging, so is exposed to continual microbial seeding from the environment or the user.
• An inventive formulation may optionally include a broad spectrum biocide and/or a combination of biocides.
• a broad spectrum biocide is defined herein as having activity against Gram positive bacteria, Gram negative bacteria, and fungi associated with a healthy human subject.
• Biocides operative herein illustratively include benzoic acid, parabens, salicylic acid, carbolic acid, sorbic acid, alkyl p-hydroxybenzoates, p-chlorometacresol, hexachlorophene, benzalkonium chloride, chlorohexidine chloride, trichlorocarbanilide, phenoxyethanol, acylsarcosines, glutathione, malic acid, tartaric acid, ascorbic acid, ascorbic acid glucoside, ascorbates, essential plant oils, mutacin proteins, and combinations thereof.
• Naturally derived biocides i.e., biocides found in nature or extracted from a natural source— are present.
• Naturally derived biocides illustratively include fermentation filtrates such as those of Lactobacillus, Streptococcus mutans, and Leuconostoc; bisabolol; eucalyptol; thymol; inositol; saponins; and natural extract of plants, such as Japanese honeysuckle (Lonicera japonica), yangti (Rumex japonicus), kushen (Sophora flavescens), candock, wild oregano, orange, sage, manifoil, common mallow, chuanxiong (Cnidii officinale Makino), Japanese green gentian (Swertia japonica Makino), bisabolol, thyme, danguii (Angelica sinensis), orange peel, bir
• a biocide may be present in the formulation(s) from 0.1 to 5 total weight percent. It is appreciated that quantities of biocides beyond 5 total weight percent may be included as desired. It is further appreciated that in some instances the inclusion of transition metal ions is used to reduce enzymatic activity of microbes.
• the formulation containing the exfoliative enzyme may be provided in a sterile form. Sterilization may be accomplished by any standard means that does not denature or degrade the enzyme. While heat or radiation may be possible, more typically size exclusion sterilization (i.e., filtration) will be used to remove contaminating bacteria and in some cases viruses from a solution containing the enzyme, or from the final formulation itself. It is appreciated that single-use packages are best suited for maintaining sterility of the sterilized formulation, as airborne microbes or microbes associated with the subject tend to infiltrate an opened package.
• the formulation(s) are packaged in a container having a pump atomizer.
• the container is a pressurized spray can, a squeeze bottle or squeeze tube, a bottle with an applicator (separate or attached), a single-use vial, or any other appropriately configured container.
• the container may be formed of plastic, glass, or metal.
• Table 1 Typical ranges of ingredients in a one-part formulation, where the percentages are total weight percent.
• Anti-inflammatory agent 0 to 5%
• Citric acid O to 1% [0030] Table 2. Typical ranges of ingredients in each of the two parts of a dual-formulation embodiment, where the specified percentages denote total weight percent.
• Anti-inflammatory agent 0 to 5%
• Vitamin(s) O to 1%
• Anti- inflammatory agent 0 to 5%
• Vitamin(s) 0 to l%
• the manner in which the formulation containing the enzyme is prepared is important to maintaining enzymatic activity. For example, one can add the enzyme late in the formulation process, or one can minimize these sources of energy when the enzyme is present, or both.
• the inventive formulation is in the form of an emulsion.
• an emulsion is well suited to wet the hair cortex, which tends to be lipophilic owing to secretion from sebaceous glands surrounding the hair follicle.
• the minority phase components of an oil-in-water emulsion illustratively include oils, waxes, esters, ethers, butters, glycerides, or combinations thereof.
• the majority phase components of an oil-in-water emulsion may include, besides water: aqueous salts, humectants, and various water soluble materials as detailed above.
• An emulsifier for such a system may be selected from ionic surfactants, non-ionic surfactants and also including lecithin, liposomes, and oleosomes.
• Other non-essential additives are readily provided that include viscosity modifiers, emulsion stabilizers, fragrances, and the like.
• the oil-in-water emulsion has a pH value of 5 to 8. If certain embodiments, the oil-in-water emulsion has a pH value of 6 to 7, e.g., 6.5 to 6.8. It is appreciated that including an enzyme in an aqueous segment of a water-in- oil emulsion serves to stabilize the enzyme against storage degradation.
• the water-in-oil emulsion or a water-in-silicone emulsion varies the relative quantities of minority and majority phase components and preferably relies on non- ionic surfactants and silicone derivatives as emulsifiers.
• Viscosity modifiers and/or emulsion stabilizers illustratively include water soluble salts, gums, waxes, and combinations thereof.
• the inner phase has a pH of 4 to 8.
• vitamin B complexes vitamin E, vitamin K, ascorbic acid derivatives such as ascorbic acid glucosides, E-O-alkyl ascorbic acid, and ascorbate phosphates are readily provided in one or both of the aforementioned emulsion phases or provided as a separate third phase.
• the vitamin(s) may be in addition to the anti-oxidant and/or anti-inflammatory ingredients described above.
• An inventive emulsion formulation is readily formed by combining premixed phases as detailed above or alternatively all such components are intermixed in sequence conventional to the art as a unified mixture— provided that, in a formulation containing active enzyme, care is taken not to subject the enzyme to excess heat or shear during the mixing process (if the enzyme is sensitive to same).
• a process of stimulating hair retention on a scalp includes enzymatically exfoliating the scalp of a subject.
• the liquid formulation solution, emulsion, or suspension
• the subject's scalp and hair roots This can be done by squirting or dabbing the formulation onto the target area, or by forming a mist with a propellant-based pressurized aerosol spray can or a manual spray pump equipped with a conventional atomizer nozzle, and directing the mist at the target area.
• the amount needed to achieve the hair retention effect will depend on factors that include the concentration of the enzyme, the concentration of the hair retention-promoting active agent, and the viscosity of the formulation.
• the application of the exfoliative enzyme and the application of the hair retention-promoting substance are readily performed as separate steps. Alternatively, one can apply them simultaneously, e.g., using a single formulation that includes both the peptidase enzyme and the hair retention-promoting substance. In instances where the two active agents are applied using separate formulations, it is appreciated that the two formulations can be similar or can be very different.
• the enzyme will generally be formulated in an aqueous solution or an emulsion with an aqueous phase containing the enzyme.
• the hair retention-promoting substance may be either hydrophilic or lipophilic and so may require a type of formulation different from that used for the enzyme.
• the first formulation (containing the active enzyme) is used routinely (e.g., daily) for the first several weeks along with regular application (e.g., daily or twice daily) of the second (hair retention-promoting) formulation; after a degree of exfoliation has been achieved, the first formulation is applied less frequently, for example, only every two or three days, while the frequency of applying the second formulation is maintained. Hair retention improvement is typically noted in two to three months.
• a process for forming a revitalizing scalp treatment in five steps in an aqueous solution of deionized water is provided.
• step A citric acid, sodium citrate, and a glucoside of ascorbic acid are added in that order to the deionized water in a main vessel, with each ingredient mixed with the water until blended prior to adding the next ingredient.
• step B sodium hydroxide (NaOH) (20%) is added to adjust the pH of the first mixture in the main vessel to between 6.5 to 6.8.
• step C glucosyl hesperidin and red ginseng extract (40% water, 60% butylene glycol and 0.2 % Panax Ginseng Root Extract by weight), are added to the main vessel and mixed in until all solids dissolve and are uniformly blended.
• step D 1,2-hexanediol, pentylene glycol, and a brown algae extract in caprilic/capric triglyceride solvent (the extract containing, in milligrams per 100 grams of solvated extract: palmitic acid 28.2, palmitoleic acid 12.4, stearic acid 6.8, oleic acid 14.7, linoleic acid - (Omega 6) 7.2, a linolenic acid 9.7, omega 3 fatty acids 26.3, cholesterol 47.2, campesterol 45.9, stigmasterol 57.5, and sitosterol 142.8) are premixed in a separate vessel, and then added to the main vessel and mixed until blended.
• caprilic/capric triglyceride solvent the extract containing, in milligrams per 100 grams of solvated extract: palmitic acid 28.2, palmitoleic acid 12.4, stearic acid 6.8, oleic acid 14.7, linoleic acid - (Omega
• step E a salmon egg hatching enzyme solution containing leukolectin(s) or other lectins, choriolysin(s), and zonase (leukolectin content of 0.00068 wt. %, zonase content of
• 0.00034 wt. %, choriolysin content of 0.0000136 wt. %) is added to the main vessel and mixed until blended, forming the final formulation.
• Table 3 lists the aforementioned ingredients, where percentages are total weight percent.
• Table 3 Exemplary inventive hair retention formulation. Deionized water Remainder
• Example 1 The process of Example 1 is repeated with the addition of a vitamin complex containing in solution vitamins B3, B5, B6, C and E.
• the amount of the vitamin complex solution added is 2 percent of the final total weight, with a corresponding reduction in the amount of deionized water.
• the vitamins are present in the vitamin complex solution in amounts varying from 10 to 200 milligrams per 100 grams of vitamin complex solution.
• a female subject suffering a daily hair loss of on average 52 hairs per day as measured by drain trap collection commenced usage of the formulation of Example 1 on a daily basis with aerosol misting of the head with 1 milliliter of solution after routine shampoo and conditioner usage, followed by 5 minutes of dwell time prior to blow drying. After 8 weeks of daily use, daily hair loss was reduced to on average 4.6 hairs per day.
• Example 3 The method of Example 3 is repeated with the formulation of Example 2, resulting in a daily hair loss of on average 3.4 hairs per day.
• EXAMPLE 5
• Example 1 The method of Example 1 is repeated, but with the omission of glucosyl hesperidin from the formulation. A reduction in daily hair loss is noted consistent with that of Example 3.
• Example 1 A clinical trial was conducted with the formulation of Example 1. Subjects were recruited with enrollment criteria that included: subject is female between the ages of 25 and 55 years; subject normally uses shampoo and conditioner; subject has hair length that is sufficient for evaluation, as determined by the cosmetologist; has Skin Type I-IV ( ranging from white to moderately brown with skin reaction to sun within the range of "always burns" to "tans with ease”; subject sheds at least 20 hairs at the baseline evaluation; subject agrees to replace their usual hair shampoo and conditioner with the provided materials during the conditioning phase and for the duration of the study; subject agrees to apply the assigned scalp treatment once every other day for the duration of the study; subject agrees to protect the scalp from sun exposure; subject is in generally good health; and subject is dependable and able to follow directions as outlined in the protocol.
• Subjects were recruited with enrollment criteria that included: subject is female between the ages of 25 and 55 years; subject normally uses shampoo and conditioner; subject has hair length that is sufficient for evaluation, as determined by the cosmetologist; has Skin Type I-IV (
• Enrolled subjects were instructed to apply the test material to the scalp every other day during the 24 week use period. Subjects were instructed to refrain from test material use and washing/conditioning the hair the morning of each visit. Subjects were also instructed to refrain from using any shampoos, conditioners, and scalp treatments (other than the materials provided), but were told they may continue styling their hair in the usual manner (i.e. blow dry, flat iron, curling iron) and may use their usual styling products.
• MEDISCOPE® combines the high resolution of digital photography with the direct capture features of a software archiving system and, in doing so, simplifies the photo- documentation process.
• Mediscope utilizes a Canon Powershot G10 (14.7 Mega Pixel). This camera takes photos in outstanding quality that can be seen immediately on-screen. The whole imaging process is completely controlled by the software.
• An overlay feature allows the baseline images to be overlaid onto the live preview images, thus ensuring almost exact repositioning at every visit.
• One digital image of the scalp (crown of the head) was collected at each visit. The hair of each subject was assessed by a cosmetologist using a modified Visual Analog Scale (VAS) at each visit.
• VAS Visual Analog Scale
• the cosmetologist selected a location on the 100mm VAS scale that corresponds with the assessment of hair thickness/volume, in relation to the labeled vertical positions on the scale. The distance between the mark recorded and the left origin of the line was subsequently measured in millimeters, to allow for assignment of a numerical score for the extent of the evaluated parameter.
• the hair was shampooed/conditioned by the cosmetologist at the laboratory using Free & ClearTM Shampoo and Conditioner. Subjects wore a drape (white for dark-haired subjects and black for light-haired subjects). The hair was detangled with a comb or pick, if necessary. The hair was divided into five sections. Each section was combed from root to end for five strokes, using a wide tooth comb. Any hair shed onto the drape or in the sink was collected and counted. The hair was then finger-blown dry. Once the hair was dry, the hair was divided into five sections. Each section was combed from root to end for five strokes, using a wide tooth comb. Any hair shed onto the drape was collected and counted.

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• 2014
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