Patent Application
20210212913
The present application claims the priority based on Korean Patent Application No. 10-2017-0165268 filed on Dec. 4, 2017, and the entire contents disclosed in the description and drawings of the corresponding application are incorporated in the present application.
The present disclosure relates to a cosmetic composition for promoting skin exfoliation.
In general, skin is divided into an epidermal layer and a dermal layer, of which epidermal layer is divided into a stratum corneum layer, a granular layer, a stratum spinosum layer and a basal layer. Skin cells produced through the basal layer take a form of thin and wide cells due to the denuclearization process of cells and changes in the lipid bilayer to the stratum corneum layer, and when they reach the stratum corneum, they become to have a form of dead cells filled with hydrophobic keratin proteins inside. In addition, between keratinocytes of the stratum corneum, a lamella layer composed of ceramides as a main component is formed, and a structure bound to the corneodesmosome between keratinocytes is taken. The stratum corneum composed of keratinocytes and ceramides shows a protective effect from foreign substances, and at the same time, it functions as a protective film that can prevent moisture from escaping, and the like. A normal stratum corneum has a thickness of about 15-20 layers, and the action of serine protease activated outside the stratum corneum causes the decomposition of corneodesmosome and eventually undergoes a process of complete detachment from the skin. This process takes about 15-20 days for normal cells. (Britsh J. of Dermatology, 86, 14-19, 1974; K. M. Halprin and Cosmetical Bulletin, 12(4), 265-271, 1988; M. Takahash) Even if it is not a genetic disease such as ichthyosis, aging, dryness, and acne skin have a longer period of the above exfoliation process than normal, and therefore the stratum corneum stratification which thickens the stratum corneum layer appears.
It is known that the stratum corneum stratification is generally caused by factors such as decreased skin moisturizing ability, reduced expression of serine protease or decreased activity, ultraviolet and decreased cellular activity, and the like. In order to eliminate the stratum corneum stratification produced in this way, generally, methods such as exfoliation by a physical scrub preparation, exfoliation by a chemical preparation, and physiological cell activity increase are used. These types of exfoliation methods are intended to solve external problems such as roughness or dullness of skin by artificially removing external keratinocytes and through replacement of the outermost stratum corneum layer with new keratinocytes from inside, resolving the stratum corneum stratification.
Among methods for resolving the stratum corneum stratification, in particular, the method using AHA (Alpha hydroxy acid) of chemical exfoliation methods is representative, and in addition, BHA (beta hydroxy acid) and PHA (poly hydroxy acid) are also representative methods. The chemical exfoliation method has additional effects such as removing fine wrinkles, removing blemishes, improving rough skin, and the like, through exfoliation. AHA used for chemical exfoliation may have an effect by treating skin at a high concentration (30-70%) for a short time (1-15 minutes) (Clinical, Cosmetic and Investigational Dermatology, 6, 281-288, 2013; J. Sharad), but it also shows effects such as slowly exfoliating the stratum corneum when used at a concentration of 10% or less (J. AM. Acad. Dermatol., 11, 867-879, 1984; Van Scott), enhancing skin moisturizing (happi, jully, 66-68, 1994), alleviating fine wrinkles (Cutis, 43, 222-228, 1989; Van Scott), and the like, and therefore it is used for cosmetics, and the like. The action mode of AHA is inserted into the stratum corneum and releases hydrogen ions to weaken corneodesmosome binding and lead to exfoliation, and when applied at a low pH, the insertion of the stratum corneum is smooth and the delivery of hydrogen ions is high, so inevitably low pH is required. Therefore, as low pH causes side effects such as skin stinging, itching, erythema, and the like, research to overcome these side effects has been conducted. However, when pH is adjusted or chemical modification is performed to reduce side effects, the efficacy is offset, and thus a need for a new exfoliation material that can exhibit exfoliation efficacy such as AHA even in weak acidity or neutrality has emerged.
As conventional efforts to achieve this efficacy, attempts have been made to reduce irritation and maintain or increase the exfoliation efficacy by slowing the skin permeation rate due to large molecular weight using PHA (Polyhydroxy acid) having a hydroxyl group and a carboxyl group (Korean Registered Patent No. 10-1388052). However, even in this case, when the pH is raised, its efficacy is rapidly lost, and therefore it should be used in an acidic condition, and thus there is still a potential for irritate the skin.
Conventional chemical exfoliating agents such as AHA or PHA exhibit their effects based on weakening of binding protein between keratinocytes due to delivery of hydrogen ions through low pH. Accordingly, when the pH is adjusted to a weakly acidic-neutral pH in order to alleviate side effects caused by skin irritation, they have a problem that their activities are reduced by 80% or more, so it is difficult to provide an advantage of substantially exfoliation.
The present disclosure is to solve the aforementioned problems, and is to provide a cosmetic composition with an excellent exfoliation effect than the efficacy of the conventional effective raw material even at a weakly acidic-neutral pH and low skin irritation.
To achieve the aforementioned objects, the present disclosure provides a use of a cosmetic composition for promoting skin exfoliation comprising a calcium-binding substance and a substance that changes protein structure.
According to one aspect of the present disclosure, the calcium-binding substance of the cosmetic composition for promoting skin exfoliation of the present disclosure is characterized by at least one selected from the group consisting of gluconolactone, serine, carnitine, carnosine, lactobionic acid, citric acid, hydrocaprylic acid, lactic acid and azelaic acid.
According to one aspect of the present disclosure, the calcium-binding substance of the cosmetic composition for promoting skin exfoliation of the present disclosure is characterized by at least one selected from the group consisting of gluconolactone, serine, carnitine and carnosine.
According to one aspect of the present disclosure, the substance that changes protein structure of the cosmetic composition for promoting skin exfoliation of the present disclosure is characterized by at least one selected from allantoin and creatine.
According to one aspect of the present disclosure, the substance that changes protein structure of the cosmetic composition for promoting skin exfoliation of the present disclosure is characterized by further comprising at least one selected from urea and hydroxyethyl urea.
According to one aspect of the present disclosure, the cosmetic composition for promoting skin exfoliation of the present disclosure is characterized by further comprising a polymer material.
According to one aspect of the present disclosure, the polymer material of the cosmetic composition for promoting skin exfoliation of the present disclosure is characterized by at least one selected from the group consisting of cellulose nanofiber, carboxymethyl cellulose (CMC), hyaluronic acid and carbomer.
According to one aspect of the present disclosure, the cosmetic composition for promoting skin exfoliation of the present disclosure is characterized by pH 5 to 7.5.
According to one aspect of the present disclosure, the content of the calcium-binding substance in the composition of the present disclosure is characterized by 0.001 to 20% by weight based on the total composition weight.
According to one aspect of the present disclosure, the content of the substance that changes protein structure in the composition of the present disclosure is characterized by 0.001 to 10% by weight based on the total composition weight.
According to one aspect of the present disclosure, the content of the polymer material in the composition of the present disclosure is characterized by 0.0001 to 5% by weight based on the total composition weight.
The cosmetic composition according to the present disclosure may have an excellent exfoliation effect compared to the conventional effective raw material even at a weakly acidic-neutral pH and also exhibit low skin irritation.
In particular, the present disclosure maximizes exfoliating ability through a combination of raw materials having a synergistic effect, thereby exhibiting an effect of increasing efficacy and reducing side effects which are unique side effects of a raw material that may be caused when using one kind of raw material at a high concentration.
The present disclosure to achieve the aforementioned objects is characterized by a cosmetic composition for skin exfoliation comprising a calcium-binding substance and a substance that changes protein structure. Hereinafter, with reference to drawings, the present disclosure will be described in detail.
The cosmetic composition for skin exfoliation according to the present disclosure comprises a calcium-binding substance and a substance that changes protein structure.
The term, “exfoliation” used herein means that the stratum corneum accumulated in the stratum corneum layer of skin is eliminated or removed from the stratum corneum layer. It is a concept that includes not only the case where it is removed by applying a physical force, but also the case where it is separated from the stratum corneum layer only by treating a cosmetic composition without applying a separate force.
The calcium-binding substance of the present disclosure means a substance which alleviates protein binding between keratinocytes through binding to calcium in skin.
According to one aspect of the present disclosure, the calcium-binding substance may be at least one selected from the group consisting of gluconolactone, serine, carnitine, carnosine, lactobionic acid, citric acid, hydrocaprylic acid, lactic acid and azelaic acid. Preferably, the calcium-binding substance may be at least one selected from the group consisting of gluconolactone, serine, carnitine and carnosine, and much more preferably, it may be carnitine.
The substance that changes protein structure of the present disclosure is a substance which affects the structure of the binding protein, and weakening of binding between keratinocytes may be induced through this.
According to one aspect of the present disclosure, the substance that changes protein structure may be preferably allantoin and/or creatine, and much more preferably, it may be allantoin.
According to one aspect of the present disclosure, a component for a protein structural change may be further comprised, and for example, it may be at least one selected from urea and hydroxyethyl urea.
The aforementioned substances that change protein structure have the following chemical formula in their structures in common.
According to one aspect of the present disclosure, the cosmetic composition for skin exfoliation of the present disclosure may further comprise a polymer material which can weaken binding between keratinocytes physicochemically.
According to one aspect of the present disclosure, the polymer substance may be at least one selected from the group consisting of cellulose nanofiber, carboxymethyl cellulose (CMC), hyaluronic acid and carbomer. Preferably, it may be cellulose nanofiber.
As confirmed in the present disclosure, the calcium-binding substances were classified into the above group by confirming that the activity was decreased when a calcium ion was present by an exfoliation evaluation experiment and finding that calcium binding in the stratum corneum layer was the main mechanism of exfoliation, and it was confirmed that the other two classes, the substance that changes protein structure and polymer material were not affected by calcium. In addition, polymers have a unique bed structure in which the minor axis has a nanometer size and the long axis has a micrometer size, and they are mentioned in the invention of Korean Patent Publication No. 10-2017-0103698. It is expected that this unique structure may cause cracking between keratinocytes.
In other words, in order to solve the problems of skin irritation and reduced effects from increasing pH of the conventional chemical exfoliating agents showing their effects by calcium binding, the present disclosure uses materials acting in other ways, specifically, substances which weaken the binding ability between keratinocytes through protein structural changes or through physiocochemical actions together, thereby achieving a synergistic effect of exfoliation.
According to one aspect of the present disclosure, the cosmetic composition for skin exfoliation of the present disclosure may be pH 5 to 7.5, preferably, 5.5 to 7.
According to one aspect of the present disclosure, the content of the calcium-binding substance in the composition of the present disclosure may be 0.001 to 20% by weight, preferably 0.01 to 17% by weight, more preferably 0.05 to 15% by weight, based on the total composition weight. When the content is less than 0.001% by weight, it is difficult to obtain a desired effect, and when it is over 20% by weight, the effect according to the increase of the content may be insignificant.
According to one aspect of the present disclosure, the content of the substance that changes protein structure in the composition of the present disclosure may be 0.001 to 10% by weight, preferably 0.01 to 5% by weight, more preferably 0.05 to 1% by weight, based on the total composition weight. When the content is less than 0.001% by weight, it is difficult to obtain a desired effect, and when it is over 10% by weight, the effect according to the increase of the content may be insignificant.
According to one aspect of the present disclosure, the content of the polymer material in the composition of the present disclosure may be 0.0001 to 5% by weight, preferably 0.001 to 1% by weight, more preferably 0.01 to 0.1% by weight, based on the total composition weight. When the content is less than 0.0001% by weight, it is difficult to obtain a desired effect, and when it is over 5% by weight, the effect according to the increase of the content may be insignificant.
Much more specific one example of combinations exhibiting an excellent exfoliation effect even in weakly acidity and neutrality in the composition according to the present disclosure is as (A) to (H) below.
In particular, although the above combinations are applied by relatively low concentration and high pH, each relatively low exfoliation effect exhibits a synergistic effect, and they have an excellent effect in exfoliation compared to 10% gluconolactone of pH 4-6, and at the same time, exhibit low irritation and high efficiency.
According to one aspect of the present disclosure, the composition of the present disclosure may be applied for any kind of cosmetics, quasi drugs, and skin external application products requiring exfoliation efficacy.
Hereinafter, the present disclosure will be described in more detail by examples. However, these are intended to illustrate the present disclosure in more detail, but the scope of the present disclosure is not limited thereto.
[Experimental Method]
For the porcine skin stratum corneum evaluation of the present disclosure, the exfoliation evaluation method mentioned in Journal of the European Academy of Dermatology and Venereology, 2014, 28, 415-423 was modified and used. Specifically, a sample of 6 mm diameter from 1 mm thick skin of a pig, and the like, was taken with a biopsy tool, and it was placed in a 96-well plate, and after washing it with phosphate buffered saline (PBS) once, 100 ul of the sample to be tested was added. The present sample was stored under the conditions of 37° C. and 50% humidity for a day, and then the number of exfoliated stratum corneum was measured with a cell counter and a sample containing only water was plotted as a negative control group and 10% gluconolactone pH 4 was plotted as a positive control group. The result was shown in the fold increase compared to the value of the result of gluconolactone 10% pH 6 for relative comparison.
The exfoliation ability by concentration and pH of gluconolactone was confirmed by the aforementioned porcine skin stratum corneum evaluation. The substances and composition used in the present experiment were as the following table.
The exfoliation ability by concentration of allantoin and polymer material alone was confirmed by the aforementioned porcine skin stratum corneum evaluation. The substances and composition used in the present experiment were as the following table.
The experimental result was shown in
In order to find an optimal combination of gluconolactone, allantoin and cellulose nanofiber, the exfoliation ability of combinations by concentration of them was compared through the aforementioned porcine skin exfoliation evaluation. The combination ratio used in the present experiment was as the following table.
The experimental result was shown in
The exfoliation ability by concentration of carnitine, creatine and carnosine alone was confirmed by the aforementioned porcine skin stratum corneum evaluation. The combination ratio used in the present experiment was as the following table.
In order to find an optimal combination of carnitine, creatine and carnosine, the exfoliation ability of combinations by concentration of them was compared through the aforementioned porcine skin exfoliation evaluation. The combination ratio used in the present experiment was as the following table.
The experimental result was shown in
The exfoliation ability by concentration of serine was confirmed by the aforementioned porcine skin stratum corneum evaluation. The combination ratio used in the present experiment was as the following table.
The exfoliation ability of combinations by concentration of serine. creatine and allantoin was confirmed by the aforementioned porcine skin stratum corneum evaluation. The combination ratio used in the present experiment was as the following table.
The experimental result was shown in
Based on the aforementioned experimental results, various combinations as the following table were prepared, and the exfoliation ability for time was directly compared through the aforementioned porcine skin exfoliation evaluation.
The experimental result was shown in
Subjects were 14 healthy males and females between ages of 20 to 40, and were under stratum corneum turnover enhancement evaluation by DNA staining.
Before applying a sample, the color inside the lower arm and upper arm of subjects was measured with a chroma meter, and then about 0.4 ml of dihydroxy acetone (DHA) at a concentration of 10% was attached to the inner upper and lower arm for 6 hours. After 24 hours, the color of the brown-colored area by DHA was measured to compare the color difference from before the sample was applied. Thereafter, while applying the sample twice a day, the degree of discoloration was measured with a chroma meter every day to measure the time taken to return to the original skin color. 50% TT (Turnover Time) means the time taken for replacing 50% of the existing stratum corneum layer with a new stratum corneum layer, and in the present experiment, the time taken for skin colored by DHA to return to the original to 50% is shown by relative comparison analysis by regression analysis. The result of the negative control group was estimated as 10 days, and the hypothetical positive control group (a sample that returns to 50% in one day) was estimated as 1 day, to calculate them and compare relative values.
When the result of the non-treated group was estimated as 10 days, the result of the experiment for the following experimental groups was as the table below.
As the experimental result, in case of Experimental group 91, 50% TT was 8.7 days, and the stratum corneum turnover date was advanced by about 1.3 days, and in case of Experimental group 92, it was 8.3 days, and it was advanced by 1.7 days, and in case of Experimental group 93, it was 6.8 days and it was advanced by 3.2 days. In addition, among combinations, when applied in an essence formulation, in case of Experimental group 94 and Experimental group 95, it was 7.9 days both, and it was advanced by 2.1 days equally. All the combinations did not cause side effects such as erythema, itching, burning feeling, and the like, during and after the experimental period.
Through this, it was confirmed that the combination of which efficacy was found by the porcine skin exfoliation evaluation could be used as a stratum corneum turnover enhancement material in clinical trials, and it was confirmed that its efficacy was exhibited when applied to formulations.
In the above, the applicant has described preferable examples of the present disclosure, but these examples are only examples that implement the technical spirit of the present disclosure, and it should be interpreted that any modification or alteration belongs to the scope of the present disclosure as long as the technical spirit of the present disclosure is implemented.
| Number | Date | Country | Kind |
|---|---|---|---|
| 10-2017-0165268 | Dec 2017 | KR | national |
| Filing Document | Filing Date | Country | Kind |
|---|---|---|---|
| PCT/KR2018/007659 | 7/5/2018 | WO | 00 |
