Small nucleic acid freckle-removing essence

Abstract

The invention discloses a small nucleic acid freckle-removing essence, which is carefully matched with active ingredients such as siRNA, NARDOSTACHYS CHINENSIS extract, nicotinamide, ascorbyl glucoside, tranexamic acid and the like, not only can block the generation of melanin from the source, but also can promote the metabolism of skin, accelerate the metabolism of generated melanin, and achieve internal and external synergism, so that the freckle-removing essence has the effects of removing freckle, removing freckle and removing freckle. A good removing effect is achieved on freckles, chloasma and other color spots.

Description

Technical Field

[0001] This invention relates to the field of cosmetics, specifically to a small nucleic acid spot-removing essence. Background Technology

[0002] Pigmentation is mainly caused by factors such as ultraviolet rays, skin care products containing metals, pregnancy, endocrine disorders, and acid-base imbalance. Pigmentation includes freckles, melasma, seborrheic keratosis (age spots), and nevus of Ota.

[0003] Generally speaking, cosmetic treatments primarily target freckles and melasma. For age spots and nevus of Ota, medication is the only option.

[0004] Therefore, traditional techniques need to be improved. Summary of the Invention

[0005] The purpose of this invention is to solve the above-mentioned technical problems. To this end, this invention provides a small nucleic acid freckle-removing essence, which designs siRNA targeting the microphthalmia-associated transcription factor (MITF) gene in the regulation of melanin formation. Through RNAi regulation, it inhibits the MITF gene and its downstream tyrosinase (TYR) gene and tyrosinase-related protein-1 (TYRP-1) gene, thereby regulating melanin production and thus having a good freckle-removing effect on freckles and melasma.

[0006] To achieve the above objectives, the first aspect of this invention provides a small nucleic acid freckle-removing essence, comprising the following components in weight percentages: trehalose 1-3%, nicotinamide mononucleotide 0.1-1%, PPG-5-cetyl ether-20 0.1-1%, 3-o-ethyl ascorbic acid 1-3%, menthol 0.01-0.1%, PEG-40 hydrogenated castor oil 0.01-0.1%, 1,2-hexanediol 0.1-0.5%, laurocapram 0.1-0.5%, carbomer 0.1-0.5%, nicotinamide 1-5%, p-hydroxyacetophenone 0.4-0.6%, butylene glycol 1-5%, hydrolyzed proanthocyanidins 0.1-0.5%, hyaluronic acid 0.01-0.05%, arginine / lysine polypeptide 0.001-0.01%, yeast polypeptides 0.1-1%, ascorbate glucoside 1-3%, tranexamic acid 1-3%, siRNA 0.001-0.01%, Nardostachyschinensis extract 1-10%, water balance.

[0007] Compared with existing technologies, this invention adds siRNA to the essence. The siRNA described in this invention is designed to target the microphthalmia-associated transcription factor (MITF) gene, which is involved in the regulation of melanin formation. By regulating and inhibiting the MITF gene and its downstream tyrosinase (TYR) gene and tyrosinase-related protein-1 (TYRP-1) gene through RNAi, melanin production is regulated.

[0008] It should be understood that siRNA, also known as small interfering RNA, is an effector molecule of RNAi, consisting of two complementary single-stranded RNA molecules. RNA interference (RNAi) involves introducing a double-stranded RNA consisting of sense and antisense RNA corresponding to the mRNA sequence into the cell, causing mRNA degradation and gene silencing.

[0009] The sequence of the siRNA is shown in Table 1 below: Table 1. siRNA single-stranded sequences (the other is the complementary strand). Furthermore, the Nardostachys Chinesesis extract is obtained by the following method: (1) Take the dried roots and rhizomes of Nardostachys jatamansi, dry them, and pulverize them; (2) Soak the spikenard powder in an ethanol aqueous solution; then transfer it to a percolation tank; then elute with an ethanol aqueous solution and collect the eluent; (3) Concentrate the eluent to remove ethanol, then add an equal volume of propylene glycol to the original eluent, and extract by ultrasonication; centrifuge and take the supernatant to obtain the product.

[0010] Furthermore, the concentration of the ethanol-water solution is 75% V / V.

[0011] Furthermore, the soaking time described in step (2) is 12-24 hours.

[0012] Furthermore, in step (2), the ratio of the nardostachys powder to the ethanol aqueous solution is 1:3-1:5.

[0013] Furthermore, the amount of eluent collected in step (2) is 2 BV.

[0014] Furthermore, the ultrasonic extraction time in step (3) is 10-30 minutes.

[0015] In summary, the technical effects achieved by this invention are as follows: (1) This invention provides a biological macromolecule siRNA and applies it to the essence. This is because its molecular weight is greater than 10,000 and it has no toxic side effects on the skin. Through the change of gene information flow, it can achieve multi-target control and achieve good spot removal effect with a very small amount at the microgram level. Moreover, this invention combines active ingredients such as siRNA, Nardostachyschinensis extract, nicotinamide, ascorbate glucoside, and tranexamic acid. It can block the production of melanin from the source and also improve skin metabolism and accelerate the metabolism of melanin that has been generated. The internal and external effects work together. Consumer trial tests have proven that it has a good removal effect on freckles and melasma. Attached Figure Description

[0016] The accompanying drawings are provided to further illustrate the invention and form part of the specification. They are used together with the following detailed description to explain the invention, but do not constitute a limitation thereof.

[0017] Figure 1 The attached figure shows a before-and-after comparison of volunteers in Example 9 using the product from Example 6 for 3 months. Detailed Implementation

[0018] The embodiments described in this specification are for illustrative purposes only and do not limit the scope of protection of this invention. The scope of protection of this invention is defined only by the claims, and any omissions, substitutions, or modifications made based on the embodiments disclosed in this invention will fall within the scope of protection of this invention.

[0019] The invention will be more readily understood by referring to the following detailed description of preferred embodiments and included examples. Unless otherwise specified, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention pertains. In case of conflict, the definitions in this specification shall prevail.

[0020] As used herein, the terms “prepared from” and “comprising” are synonymous. The terms “comprising,” “including,” “having,” “containing,” or any other variations thereof, as used herein, are intended to cover non-exclusive inclusion. For example, a composition, step, method, article, or apparatus that includes the listed elements is not necessarily limited to those elements, but may include other elements not expressly listed or elements inherent to such composition, step, method, article, or apparatus.

[0021] When a quantity, concentration, or other value or parameter is expressed as a range, a preferred range, or a range defined by a series of upper and lower preferred values, this should be understood as specifically disclosing all ranges formed by any pair of any upper or preferred value with any lower or preferred value, regardless of whether the range is disclosed individually. For example, when the range “1 to 5” is disclosed, the described range should be interpreted as including the ranges “1 to 4”, “1 to 3”, “1 to 2”, “1 to 2 and 4 to 5”, “1 to 3 and 5”, etc. When numerical ranges are described herein, unless otherwise stated, the range is intended to include its endpoints and all integers and fractions within that range.

[0022] Furthermore, the indefinite articles “a” and “an” preceding the elements or components of this invention do not impose any limitation on the quantity requirement (i.e., the number of times) of the elements or components. Therefore, “an” or “a” should be interpreted as including one or at least one, and the singular form of an element or component also includes the plural form, unless the quantity clearly refers to the singular form.

[0023] To enhance understanding of the present invention, the present invention will be further described in detail below with reference to embodiments. These embodiments are only used to explain the present invention and do not constitute a limitation on the scope of protection of the present invention.

[0024] Example 1 An extract of Nardostachys Chinesesis was prepared by the following method: (1) dried roots and rhizomes of Nardostachys Chinesesis were dried and pulverized; (2) Nardostachys Chinesesis powder was soaked in 75% V / V ethanol aqueous solution for 12 hours with a material-to-liquid ratio of 1:5; then transferred to a percolation tank; then eluted with 75% V / V ethanol aqueous solution and collected 2 BV of eluent; (3) the eluent was concentrated to remove ethanol, and then an equal volume of propylene glycol was added to the original eluent and ultrasonically extracted for 10 minutes; centrifuged and the supernatant was collected.

[0025] Example 2 An extract of Nardostachys Chinesesis was prepared by the following method: (1) dried roots and rhizomes of Nardostachys Chinesesis were dried and pulverized; (2) Nardostachys Chinesesis powder was soaked in 75% V / V ethanol aqueous solution for 24 hours with a material-to-liquid ratio of 1:3; then transferred to a percolation tank; then eluted with 75% V / V ethanol aqueous solution and collected 2 BV of eluent; (3) the eluent was concentrated to remove ethanol, and then an equal volume of propylene glycol was added to the original eluent and ultrasonically extracted for 30 minutes; centrifuged and the supernatant was collected.

[0026] Example 3 An extract of Nardostachys Chinesesis was prepared by the following method: (1) dried roots and rhizomes of Nardostachys Chinesesis were dried and pulverized; (2) Nardostachys Chinesesis powder was soaked in 75% V / V ethanol aqueous solution for 18 hours with a material-to-liquid ratio of 1:4; then transferred to a percolation tank; then eluted with 75% V / V ethanol aqueous solution and collected 2 BV of eluent; (3) the eluent was concentrated to remove ethanol, and then an equal volume of propylene glycol was added to the original eluent and ultrasonically extracted for 20 minutes; centrifuged and the supernatant was collected.

[0027] Example 4 A small nucleic acid spot-removing essence comprises the following components in weight percentage: trehalose 1%, nicotinamide mononucleotide 1%, PPG-5-cetyl ether-20 0.1%, 3-o-ethyl ascorbic acid 3%, menthol 0.01%, PEG-40 hydrogenated castor oil 0.1%, 1,2-hexanediol 0.1%, laurocapram 0.5%, carbomer 0.1%, nicotinamide 5%, p-hydroxyacetophenone 0.4%, butylene glycol 5%, hydrolyzed proanthocyanidins 0.1%, hyaluronic acid 0.05%, arginine / lysine polypeptide 0.001%, yeast polypeptide 1%, ascorbate glucoside 1%, tranexamic acid 3%, siRNA 0.001%, Nardostachys chinensis extract prepared in Example 1 10%, and water as the balance; The siRNA is selected from the sequence SEQ.NO.1 described in Table 1.

[0028] Example 5 A small nucleic acid spot-removing essence comprises the following components in weight percentage: trehalose 3%, nicotinamide mononucleotide 0.1%, PPG-5-cetyl ether-20 1%, 3-o-ethyl ascorbic acid 1%, menthol 0.1%, PEG-40 hydrogenated castor oil 0.01%, 1,2-hexanediol 0.5%, laurocapram 0.1%, carbomer 0.5%, nicotinamide 1%, p-hydroxyacetophenone 0.6%, butylene glycol 1%, hydrolyzed proanthocyanidins 0.5%, hyaluronic acid 0.01%, arginine / lysine peptide 0.01%, yeast peptides 0.1%, ascorbate glucoside 3%, tranexamic acid 1%, siRNA 0.01%, Nardostachys chinensis extract prepared in Example 2 1%, and water balance; The siRNA is selected from the sequence SEQ.NO.2 described in Table 1.

[0029] Example 6 A small nucleic acid spot-removing essence comprises the following components in weight percentage: trehalose 2%, nicotinamide mononucleotide 0.5%, PPG-5-cetyl alcohol polyether-20 0.5%, 3-o-ethyl ascorbic acid 2%, menthol 0.05%, PEG-40 hydrogenated castor oil 0.5%, 1,2-hexanediol 0.3%, laurocapram 0.3%, carbomer 0.3%, nicotinamide 3%, p-hydroxyacetophenone 0.5%, butylene glycol 3%, hydrolyzed proanthocyanidins 0.3%, hyaluronic acid 0.04%, arginine / lysine polypeptide 0.005%, yeast polypeptide 0.5%, ascorbate glucoside 2%, tranexamic acid 2%, siRNA 0.005%, Nardostachys chinensis extract prepared in Example 3 5%, and water balance; The siRNA is selected from the SEQ.NO.3 sequence shown in Table 1.

[0030] Comparative Example 1 A small nucleic acid spot-removing essence, comprising the following components in weight percentage: trehalose 2%, nicotinamide mononucleotide 0.5%, PPG-5-cetyl alcohol polyether-20 0.5%, 3-o-ethyl ascorbic acid 2%, menthol 0.05%, PEG-40 hydrogenated castor oil 0.5%, 1,2-hexanediol 0.3%, laurocapram 0.3%, carbomer 0.3%, nicotinamide 3%, p-hydroxyacetophenone 0.5%, butylene glycol 3%, hydrolyzed proanthocyanidins 0.3%, hyaluronic acid 0.04%, arginine / lysine peptide 0.005%, yeast peptides 0.5%, ascorbate glucoside 2%, tranexamic acid 2%, siRNA 0.005%, and water as the balance; The siRNA is selected from the SEQ.NO.3 sequence shown in Table 1.

[0031] Comparative Example 2 A small nucleic acid spot-removing essence comprises the following components in weight percentage: trehalose 2%, nicotinamide mononucleotide 0.5%, PPG-5-cetyl alcohol polyether-20 0.5%, 3-o-ethyl ascorbic acid 2%, menthol 0.05%, PEG-40 hydrogenated castor oil 0.5%, 1,2-hexanediol 0.3%, laurocapram 0.3%, carbomer 0.3%, nicotinamide 3%, p-hydroxyacetophenone 0.5%, butylene glycol 3%, hydrolyzed proanthocyanidins 0.3%, hyaluronic acid 0.04%, arginine / lysine polypeptide 0.005%, yeast polypeptide 0.5%, ascorbate glucoside 2%, tranexamic acid 2%, Nardostachys chinensis extract prepared in Example 3 5%, and water as the balance.

[0032] Example 7 Safety Evaluation According to the human skin patch test method specified in Chapter 7, Section 2 of the "Cosmetic Safety Technical Specifications" (2015 edition), the small nucleic acid spot-removing essences prepared in Examples 4-6 and Comparative Examples 1-2 were subjected to human skin patch tests.

[0033] In this test, 30 volunteers participated in each test sample. The skin condition of the sample area and control area was examined at 0.5 hours, 24 hours and 48 hours after the removal of the test substance plaque. The results showed that no obvious adverse skin reactions were observed in the sample areas of the small nucleic acid spot-removing essences prepared in Examples 4-6 and Comparative Examples 1-2 at 0.5 hours, 24 hours and 48 hours. Therefore, it can be determined that the small nucleic acid spot-removing essences prepared in the embodiments of the present invention are not irritating to the human body and can be further evaluated for efficacy in volunteer trials.

[0034] Example 8: Evaluation of Human Efficacy Volunteer trials were conducted on the small nucleic acid spot-removing essences prepared in Examples 4-6 and Comparative Examples 1-2 to evaluate their product efficacy.

[0035] Test basis: Method 1, Ultraviolet-induced human skin melanin-induced whitening efficacy test method, Appendix 7, "Test Methods for Whitening and Spot-removing Efficacy of Cosmetics," in the Announcement of the National Medical Products Administration on Incorporating 7 Test Methods, including the Test Method for Preservatives in Cosmetics, into the Technical Specifications for Cosmetic Safety (2015 Edition).

[0036] Volunteer Recruitment: Based on the above criteria, 30 volunteers will be recruited for each test group.

[0037] Directions for use: After cleansing your face morning and evening, volunteers should apply one drop of the test sample to each cheek (forehead, left cheek, and right cheek), and gently press until absorbed. Continue use for four weeks; do not use other products during this period.

[0038] Testing process: The MI value of the volunteers' facial skin was measured in weeks 0, 1, 2, 3 and 4. The difference in skin MI before and after each product use was calculated for each group. The results are shown in Table 1.

[0039] Table 1. Skin MI difference before and after product use

[0040] As shown in Table 1, after using the small nucleic acid spot-removing essence prepared according to the embodiments of the present invention for 4 weeks, the skin MI value decreased, showing a good spot-removing effect.

[0041] Example 9: Consumer Trial Test Thirty consumers with freckles and melasma were recruited at the factory to try the small nucleic acid freckle-removing essence prepared in Example 6. After cleansing their faces morning and evening, each participant applied one drop of the sample to their forehead, left cheek, and right cheek, then evenly spread it onto their skin with their fingertips, gently pressing until absorbed. They used the product continuously for 12 weeks, during which time no other products were used. A follow-up visit after 12 weeks revealed that 25 volunteers reported that their freckles and melasma had faded or disappeared, an effectiveness rate exceeding 80%.

[0042] The technical features of the above embodiments can be combined in any way. For the sake of brevity, not all possible combinations of the technical features in the above embodiments are described. However, as long as there is no contradiction in the combination of these technical features, they should be considered to be within the scope of this specification.

[0043] The above embodiments merely illustrate several implementation methods of the present invention, and their descriptions are relatively specific and detailed, but they should not be construed as limiting the scope of the invention patent. It should be noted that those skilled in the art can make various modifications and improvements without departing from the concept of the present invention, and these all fall within the protection scope of the present invention. Therefore, the protection scope of this invention patent should be determined by the appended claims.

Claims

1. A small nucleic acid spot-removing essence, characterized in that, The product comprises the following components by weight percentage: trehalose 1-3%, nicotinamide mononucleotide 0.1-1%, PPG-5-cetyl ether-20 0.1-1%, 3-o-ethyl ascorbic acid 1-3%, menthol 0.01-0.1%, PEG-40 hydrogenated castor oil 0.01-0.1%, 1,2-hexanediol 0.1-0.5%, laurocapram 0.1-0.5%, carbomer 0.1-0.5%, nicotinamide 1-5%, p-hydroxyacetophenone 0.4-0.6%, butylene glycol 1-5%, hydrolyzed proanthocyanidins 0.1-0.5%, hyaluronic acid 0.01-0.05%, arginine / lysine peptides 0.001-0.01%, yeast peptides 0.1-1%, ascorbate glucoside 1-3%, tranexamic acid 1-3%, siRNA. 0.001-0.01%, Nardostachyschinensis extract 1-10%, water balance; the siRNA sequence is selected from SEQ.NO.1-SEQ.NO.

3.

2. The small nucleic acid freckle-removing essence according to claim 1, characterized in that, The Nardostachyschinensis extract was obtained by the following method: (1) Take the dried roots and rhizomes of Nardostachys jatamansi, dry them, and pulverize them; (2) Soak the spikenard powder in an ethanol aqueous solution; then transfer it to a percolation tank; then elute it with an ethanol aqueous solution and collect the eluent; the concentration of the ethanol aqueous solution is 75% V / V; the soaking time is 12-24h; the ratio of spikenard powder to ethanol aqueous solution is 1:3-1:5; the collection volume of the eluent is 2 BV. (3) Concentrate the eluent to remove ethanol, then add an equal volume of propylene glycol to the original eluent and sonicate for 10-30 min. Centrifuge and collect the supernatant.

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