KR100521787B1 - Composition for enhancing skin or hair - Google Patents

Abstract

The present invention relates to (A) skin-treating compounds or hair-treating compounds; (B) an improving agent having the following formula

Wherein X and Y are oxygen, sulfur or Y is an imino group, X is an imino group when Y is sulfur and X is sulfur or an imino group when Y is sulfur; A is a structure in which X and Y are defined A group having; m and n are integers having a value of 1-20 and the sum of m + n is not greater than 25; p is 0 or an integer having a value of 1; q is an integer having a value of 0 or 1; r is an integer having a value of 0 or 1; R is hydrogen or an alkyl group having 1 to 6 carbon atoms and is straight or branched chain; m + n is at least 11 when p, q and r are values of 0 and Y is oxygen; (C) a carrier; And optionally (D) a cosmetic additive and a use thereof for improving the properties of the skin or hair.

Description

Composition for improving skin or hair {COMPOSITION FOR ENHANCING SKIN OR HAIR}

The present invention relates to a method for improving the physiological state of the body. More specifically, the present invention relates to compositions that are effective for improving the properties (nature) of skin or hair.

Various forms of materials are known that are effective in improving various properties of the skin, such as the softness of the skin and the texture of the skin. Examples of such substances are vitamins, antioxidant growth factors and steroids. Similarly, various types of materials are known that are effective in improving the various properties of hair, including, for example, materials that act as hair conditioners and materials that work to improve hair organization.

The present invention relates to the preparation of improved compositions for improving the properties of skin or hair.

Summary of the Invention

According to the invention, it is effective for improving the properties of the skin or hair and comprises (A) a skin-treating or hair-treating compound; (B) enhancers as described below; (C) a carrier; And optionally (D) a cosmetic additive.

Another feature of the invention is the preparation of a method for improving one or more skin or hair properties comprising applying the composition of the invention to skin or hair. In a preferred form, the composition is applied to the body part in the form of a cream or lotion.

Various advantages provided by the present invention will become apparent from the examples presented below.

As set forth above, the compositions of the present invention comprise skin- or hair-treating compounds, enhancers, carriers and optionally cosmetic additives.

The term "skin-treatment compound" refers to the quality and property of untreated skin at 95% confidence using the standard evaluation methods known to those of ordinary skill in the art and to the properties of skin treated with the material. By a statistically significant difference between is meant a substance effective to improve one or more skin properties. Examples of skin properties (qualities) that can be improved by skin-treating compounds include (A) the softness of the skin; (B) the epidermal layer thickness of the skin; (C) increased cell density of the skin; (D) decreased interossei depth; (E) elasticity of the skin; And (F) skin texture. Methods for evaluating the skin properties of the aforementioned forms by objective methods are well known to those of ordinary skill in the art. They include, for example, clinical evaluation, photographic evaluation, plastic casting, ultrasound evaluation, tissue experiments, punch biopsies and the use of tape peeling.

Examples of the class of substances for use as skin-treating compounds in the practice of the present invention include nutrients, denaturing agents, rejuvenating agents, hormones, modulators, immunomodulators, humectants and stimulants. Examples of skin-treatment materials for use in the practice of the present invention include nutrients-vitamins, amino acids and carbohydrates; Denaturant-melanin and antioxidant; Rejuvenating agent-growth factor and human growth hormone; Hormone-estrogens, progesterone and other steroids and growth hormones; Modulator-peptide, protein and anti-sense changes; Immunomodulatory-beta 1,3-glucans and farnezole; Humectants-vegetable oils, beeswax and other waxes, lanolin, fatty acid esters, mineral oils and other hydrophobic substances; And stimulants-tocopheryl nicotinate, retinoids and alpha-hydroxy acids. Many skin-treating compounds can be used in the composition.

As mentioned above, the minimum percentage improvement that is delivered to the skin by the skin-treating compound and constitutes a statistically significant difference will vary depending on the sample size and distribution as well as the skin properties being evaluated. For example, in evaluating epidermal thickness, at least 10% improvement is considered by those of ordinary skill in the art as a statistically significant difference. On the other hand, at least about 30% improvement in assessing skin elasticity constitutes a statistically significant difference to those of ordinary skill in the art.

Skin-treating compounds are used in combination with enhancers that are compounds within the range of formula I below.

Wherein: X and Y are oxygen, sulfur or conditionally an imino group of structure = NR where X is an imino group when Y is an imino group and X is sulfur or an imino group when Y is sulfur; A is a structure in which X and Y are defined A group having; m and n are integers having a value of 1-20 and the sum of m + n is not greater than 25; p is 0 or an integer having a value of 1; q is an integer having a value of 0 or 1; r is an integer having a value of 0 or 1; R is hydrogen or an alkyl group having 1 to 6 carbon atoms and is straight or branched chain; m + n is at least 11 when p, q and r are zero and Y is oxygen. When R is alkyl it may be for example methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec -butyl, amyl, hexyl and the like. Many enhancers can be used. Enhancers for use in the practice of the present invention are nontoxic and compatible with skin / hair treatment compounds comprising the compositions of the present invention. Further improvement in the properties of the skin is achieved by the use of an enhancer in combination with the skin-treating compound. This improvement is demonstrated and evaluated by the use of the same type of methodology mentioned above in combination with the skin-treating compound.

Preferably, the enhancer is a cyclic lactone compound wherein both X and Y are oxygen, q is 1 and r is 0, cyclic diesters (compounds where both X and Y are oxygen and both q and r are 1) and cyclic Ketones (compounds where both q and r are 0 and Y is oxygen). M + n is preferably at least 3 when the enhancer is a cyclic diester. When the enhancer is a cyclic ketone, m + n is preferably 11 to 15 and p is preferably 0. Particularly preferred enhancers for use in the practice of the present invention include the macrocyclic ketones and lactones of formula I above. Very preferred enhancer is cyclopentadecanoid.

Skin-treating compounds or mixtures of skin-treating compounds should be used in an amount effective to improve the properties of the skin. The minimum amount required to achieve the improvement will in particular vary depending on the skin-treating compound or mixture of skin-treating compounds used. Generally speaking, it is believed that the skin-treating compound comprises at least about 0.01 wt% of the composition. Typically the skin-treating compound comprises about 0.1-10 wt% of the composition. Preferably, the skin-treating compound comprises about 0.5 to 3 wt% of the composition.

Enhancers or mixtures of enhancers may be used in an amount that is at least effective to deliver further improvements to the skin, ie, improvements beyond those provided by the skin-treating compound. In most applications, it is believed that the enhancer comprises about 0.1-30 wt% of the composition, preferably in the range of about 0.5-10 wt%, particularly preferably in the range of about 2-5 wt%.

Skin-improvement compositions of the invention generally also include a carrier in which other components comprising the composition are dissolved or dispersed in the form of droplets of solid particles or liquid. Any suitable material may be used as the carrier, eg, a material suitable for use in pharmaceutical and cosmetic compositions. Examples of such carriers are water, alcohols, glycerin, sorbitol, propylene glycol, plant- and animal-derived oils, waxes, acids, alcohols, esters, ethers, amides, ethoxylates and propoxylates, ethylene and propylene glycol ethers, Mineral oils and waxes, silicone oils and waxes and surfactants. The carrier may also include one or more compounds. Generally speaking, the carrier comprises about 10-95 wt% of the composition.

Optionally, however, typically the composition also includes one or more compounds that impart other desired properties to the composition. Such compounds typically include substances in the form used as additives in cosmetic compositions. Examples of such materials are fragrances, colorants including pigments and dyes, preservatives, thickeners, pH adjusters, stabilizers, surfactants and emulsifiers.

The form of the composition may be liquid, semi-solid or solid. The composition can be formulated to be dispersed from an air container. Compositions in the form of creams or lotions are recommended for convenience and ease of application.

Skin-improvement compositions can be applied to the skin as often as needed to achieve the desired improvement. The frequency of application varies depending on the nature of the composition and the condition of the surrounding skin. In general, application of the composition twice a day (eg, morning and evening) may continue for a period of time, for example weeks or months or indefinitely, for a period of time suitable for handling many conditions and required to achieve a desired result. Can be. In some situations, the composition may be applied every two or three days. When treating the skin of the hands it is desirable to apply the composition every time after washing.

Compositions for treating hair are also within the scope of the present invention. Such compositions can include hair-treating compounds, such as materials that act as hair conditioners and compounds that improve the hair's grooming. Such compositions may comprise the hair-treating compound and the enhancer of formula I as well as other ingredients in amounts as described above associated with the skin-improvement composition.

Enhancers of the present invention may be used to benefit any form of skin-improving composition comprising one or more skin-treating compounds that do not readily or easily penetrate the skin epidermal barrier. Such compositions are well known to those of ordinary skill in the art. An exemplary class of such compositions are antioxidant compositions. Such compositions typically include various natural nutrients, including, for example, vitamins that act to rejuvenate the skin, retard skin aging signs, and maintain the vitality of skin cells. In vivo comparative studies involving the use of an antioxidant composition within the scope of the present invention and the use of Retin A, a substance well described for its anti-wrinkle properties, showed that the activity of the composition of the present invention was characterized by epidermal thickness without the side effects experienced with Retin A. It was measured to be consistent with Retin A in that it affected the increase.

Examples 1 to 3 below are examples of antioxidant compositions that delay skin aging by promoting natural repair processes and providing beneficial natural nutrients to skin cells. The enhancer used in the composition is cyclopentadedecanoid. Enhancers are believed to act to help the delivery of nutrients to skin cells effectively for nutrition of skin cells. This results in skin rejuvenation that gives the skin a dazzling and young appearance. Significant changes in the composition are related to the difference in viscosity and concentration of the components. This difference can be matched with the ease and effectiveness of the application so that the composition is applied repeatedly, for example, throughout the day, especially every time the body part, such as the body or hand, is washed or wiped or before bedtime.

Example 1-Hand and Body Lotion

Vitamin A Palmitate 0.38% w / w

Magnesium Ascorbyl Phosphate 0.75

Vitamin E Acetate 0.38

Alpha-bis-Avolol 0.38

Panthenol (pantothenyl alcohol) 0.25

Edetate disodium 0.10

Sodium citrate 0.60

Trollamine (triethanolamine) 1.70

Diethanolamine methoxycinnamate

       (DEA methoxycinnamate) 2.00

Aloe Vera Gel Concentrate 1.00

Beeswax, 0.50 White

Mineral oil, diesel 4.00

Cetyl Palmitate 1.00

Soya Sterol 1.00

Cetyl Alcohol 2.00

Stearic Acid 3.00

Carbomer 934 0.10

Poly (vinylpyrrolidone) / 1-eicosene copolymer 1.00

Methylparaben 0.20

Propylparaben 0.10

Imidazolidinyl urea (imideurea) 0.30

Butylated Hydroxytoluene (BHT) 0.20

Cyclopentadecanolide 4.00

Fragrance QS

water QS

100.00% w / w total

Example 2-Hand and Body Lotion

Vitamin A Palmitate 0.50% w / w

Magnesium Ascorbyl Phosphate 0.75

Vitamin E Acetate 1.50

Alpha-bis-Abolol 1.00

Panthenol (Pantothenyl Alcohol) 1.00

Edetate disodium 0.10

Sodium citrate 0.60

Trollamine (triethanolamine) 0.50

Diethanolamine methoxycinnamate

       (DEA methoxycinnamate) 2.00

Aloe Vera Gel Concentrate 1.00

Squalane 3.00

Cetyl ester 2.00

Stearyl Alcohol 4.00

PEG-40 Stearate 4.00

Glyceryl Monostearate 3.00

Methylparaben 0.20

Propylparaben 0.10

Imidazolidinyl urea (imideurea) 0.30

Butylated Hydroxytoluene (BHT) 0.20

Silicone oil 5.50

Cyclopentadecanolide 4.00

Fragrance QS

water QS

100.00% w / w total

Example 3-Night Cream

Vitamin A Palmitate 0.375% w / w

Magnesium Ascorbyl Phosphate 3.000

Vitamin E Acetate 1.500

Alpha-bis-Abolol 1.000

Panthenol (pantothenyl alcohol) 1.000

Edetate Disodium 0.100

Sodium citrate 0.600

Trollamine (triethanolamine) 0.500

Diethanolamine methoxycinnamate

       (DEA methoxycinnamate) 2.000

Aloe Vera Gel Concentrate 1.000

Squalene 3.000

Cetyl ester 2.000

Mineral Oil, Diesel 4.000

Stearyl Alcohol 4.000

PEG-40 Stearate 2.500

Glyceryl Monostearate 4.500

Methylparaben 0.200

Propylparaben 0.100

Imidazolidinyl urea (imideurea) 0.300

Butylated Hydroxytoluene (BHT) 0.200

Silicone oil 5.000

Cyclopentadecanoid 4.000

Fragrance QS

water QS

100.00% w / w total

Stationary or other shearing devices as well as standard mixing, stirring or high shear, for example at room temperature-90 ° C., to form cream emulsions or lotions with a soft feel of the components of the compositions of Examples 1-3. Formulated with substantially the same composition with a mixer. The resulting composition may be suitably packaged in plastic or aluminum tubes, glass or plastic jars, glass or plastic bottles. The composition even demonstrates gross physical stability for 3 months at violent conditions, for example at 60 ° C.

The hands and body creams of Example 2 were evaluated as effective in tests involving humans (15 Caucasians over 50 years of age). The test subjects used the composition of Example 2 or the placebo cream with blind cord for the first two months and then all the subjects used the composition of Example 2. The test composition was rubbed into the hands every night before the test subject went to bed. The following technique was used to evaluate the performance of the composition on the back of the hand: (A) photo; (B) plastic casting; (C) ultrasound B-mode scan; (D) biopsy for tissue experiments; And (E) ballistometry. Example 2 The overall effect observed as a result of use in the evaluation of the composition is summarized below.

Comparison of the subjects based on the photographic evaluation (A) showed a gradual improvement in the appearance of the back of the hand as a result of the use of the composition of Example 2. Photographic studies indicate a decrease in the number of wrinkles, a decrease in interosseous muscle depth and a general improvement in skin softness. The use of the composition of Example 2 has been shown to improve both the properties of the stratum corneum and the hydration of the epidermis and the dermis. As shown by the decrease in depth, the improvement of the interosseous muscle depth indicates improvement of the dermis.

The plastic casting of (B) above was evaluated and compared by two independent scores. Changes in local anatomy of the skin were evaluated according to the following grades: positive response; No response or no change; And negative response or worsening. These results were averaged. There was no significant difference in topical anatomy of skin on day 30. On the 90th day, the plastic casting showed that 60% of the subjects tested positive in the local anatomy of the skin and 73% of the subjects tested positive on the 180th day.

Based on the ultrasound evaluation of (C) above, the overall effect produced by the use of the composition of Example 2 can be summarized by three observations: (1) Most epidermis of the subject became thicker and more hydrated ; (2) the papillary dermis is denser; (3) Reticulated dermis increases in density. Gradually increase in thickness and density up to 3 or 4 months during the progress of the test. After this period, the increase reaches a steady state or decreases slightly. This finding suggests that the initial proliferative effect of the product in the epidermis leads to dermal reconstitution.

Fragments soiled from the tissue experiment of (D) were tested and evaluated with the following factors: (1) epidermal thickness; (2) the size of the granule layer; (3) the appearance of the stratum corneum; And (4) appearance of the dermis. Epidermal thickness increased by 19% during the study and a 50% increase in epidermal thickness of some subjects. The granule layer increased at least twice the thickness in all subjects. This increase was assessed by the number of granule cells. The stratum corneum appearance was significantly different in most subjects. From the compact initial appearance, the stratum corneum is assumed in the form of a basket net associated with the younger epidermis. Dermal evaluation is difficult to assess in that no special pigment is used. Most of the subjects showed an increase in the cytoplasm of the dermis. This finding is consistent with the process of reconstitution of the dermis.

Based on the trajectory measurement of (E) above, 10 subjects had a positive reaction and 4 subjects did not have any significant change. One subject had a negative response. This test measures dermal changes (not epidermal changes) and suggests that some reconstruction of the dermis occurs.

Based on the data obtained from the composition use evaluation of Example 2, the results were obtained regarding the use of the composition of Example 2: (1) the product is effective to increase the epidermal thickness; (2) the product is effective in producing a smooth and well-made stratum corneum; (3) the product increases epidermal proliferation; (4) the product increases skin elasticity; (5) the product helps to restore dermal structure; (6) The product is effective in restoring aged hands to a younger appearance.

The following two examples are examples of the use of the enhancers of the invention in sunscreen compositions. Such compositions typically contain a number of sunscreens, compounds that act to protect the skin by their ability to absorb various wavelengths of potentially harmful ultraviolet radiation. Sunscreen compositions include, for example, (A) the basic ability to absorb the radiation involved; (B) the ability to persist to absorb radiation for extended periods of time; (C) have a combination of properties including the ability to be unaffected by exposure to water and / or sweat. Several sunscreens are known to penetrate the skin relatively quickly, eventually leading to systematic circulation with continuous consumption of the lower skin layers (dermis). In the development of the present invention, sunscreen agents in the compositions of the present invention have been observed to remain at higher concentrations for longer periods in the epidermis. It is believed that the concentration of sunscreen in the epidermis helps to provide natural resistance to physical contact and its removal resulting from exposure to water, including sweat. The extent of this "maintenance" effect depends on the specific sunscreen, carrier used and enhancer concentration. The enhancer used in each of the compositions of Examples 4 and 5 is cyclopentadecanolide.

Example 4 Sunscreen Lotion

Benzophenone-3 (oxybenzone) 3.0% w / w

Diethanolamine methoxycinnamate

       (DEA methoxycinnamate) 3.0

Cyclopentadecanoid 4.0

Silicone oil 5.0

Glyceryl Monostearate 5.0

PEG-40 Stearate 1.0

Sodium Lauryl Sulfate 0.5

Stearyl Alcohol 7.1

Cetyl ester 5.0

Propylparaben 0.2

Butylated Hydroxytoluene (BHT) 0.2

Diethylene glycol monomethyl ether 30.0

water QS

100.0% w / w total

Example 5 Sunscreen Lotion

Benzophenone-3 (oxybenzone) 3.00% w / w

Diethanolamine methoxycinnamate

       (DEA methoxycinnamate) 3.00

Cyclopentadecanolide 4.00

Silicone oil 1.00

Glycerin (Glycerol) 5.00

Propylene Glycol 5.00

Carbomer 941 0.25

Squalane 3.00

Stearic Acid 1.50

Cetyl ester0.50

Cetyl alcohol0.50

Glyceryl Monostearate 3.00

PEG-40 Stearate 1.50

Trollamine (triethanolamine) 0.50

Methylparaben 0.20

Propylparaben 0.10

Imidazolidinyl urea (imideurea) 0.30

Fragrance QS

water QS

100.00% w / w total

The present invention provides an effective way to improve the delivery of various types of substances to the body that have a beneficial effect on our body.

Claims (19)

(A) a skin-treating compound or a hair-treating compound; And (B) an enhancer having the following formula I; And (C) a composition effective to improve the properties of the skin or hair, comprising a carrier: Wherein X and Y are oxygen, sulfur or Y is an imino group, X is an imino group when Y is sulfur and X is sulfur or an imino group when Y is sulfur; A is a structure in which X and Y are defined A group having; m and n are integers having a value from 1 to 20 and the sum of m + n is not greater than 25; p is 0 or an integer having a value of 1; q is an integer having a value of 0 or 1; r is an integer having a value of 0 or 1; R is hydrogen or an alkyl group having 1 to 6 carbon atoms and is straight or branched chain; When p, q and r have a value of 0 and Y is oxygen, m + n is 11 or more. The composition of claim 1 wherein the amount of said compound in said composition is at least 0.01 wt%. The composition of claim 1 comprising 0.1-10 wt% of said compound and 0.1-30 wt% of said enhancer. The composition of claim 3 comprising 0.5 to 3 wt% of the compound and 0.5 to 10 wt% of the enhancer. The composition of claim 3 comprising from 2 to 5 wt% of said enhancer. The composition of claim 2 wherein the composition is an antioxidant composition and the compound comprises an antioxidant material. The composition of claim 1, wherein said enhancer consists essentially of cyclopentadedecanoid. 3. The composition of claim 2, wherein said enhancer consists essentially of cyclopentadedecanoid. 4. The composition of claim 3, wherein said enhancer consists essentially of cyclopentadecanolide. 5. The composition of claim 4, wherein said enhancer consists essentially of cyclopentadecanolide. 6. The composition of claim 5, wherein said enhancer consists essentially of cyclopentadecanolide. 7. The composition of claim 6, wherein said enhancer consists essentially of cyclopentadecanolide. The composition of claim 1 comprising the skin-treating compound. 8. The composition of claim 7 comprising said skin-treating compound. The composition of claim 13, wherein the skin-treating compound comprises a sunscreen agent. The composition of claim 1 for improving the properties of the skin or hair, including applying to the skin or hair. The composition of claim 16 comprising the skin-treating compound and applying to the skin to improve the properties of the skin or hair. 17. The composition of claim 16 comprising a hair-treating compound and applying to the hair to improve the properties of the skin or hair. The composition of claim 1 further comprising a cosmetic additive.