A white mulberry polypeptide compound whitening and repairing composition, and a preparation method and application thereof

Abstract

The present application relates to the field of cosmetic technology, and discloses a white muscardine polypeptide composite whitening and repairing composition, a preparation method and application thereof. The composition takes fermented white muscardine oligopeptide as a core functional ingredient, and is compounded with ethyl vitamin C and 4D hyaluronic acid. The composition realizes whole-pathway whitening through a wind-phlegm-stasis three-dimensional blocking mechanism, and has barrier repairing and anti-inflammatory soothing effects. The present application also discloses a preparation process of the composition. The white muscardine is subjected to biological fermentation and fractional purification to obtain low molecular active peptides with a molecular weight of 0.3-3 kDa. The double-bin compounding technology is used to ensure the activity of the ingredients. The prepared cosmetic is mild and non-irritating, and is suitable for sensitive skin, people with post-inflammatory hyperpigmentation, and post-medical beauty, and can realize the effects of brightening skin color, improving dullness, and lightening color spots, and has the advantages of traditional Chinese medicine beauty theory and modern biological technology.

Description

Technical Field

[0001] This invention belongs to the field of cosmetic technology, specifically relating to a whitening and repairing composition of white silkworm polypeptide, its preparation method and application. Background Technology

[0002] Skin whitening and blemish removal are popular demands in the cosmetics industry. Existing whitening products mostly use chemical whitening agents or single plant extracts, which have many technical drawbacks: chemical whitening agents such as hydroquinone are highly irritating and can easily cause skin allergies, making them unsuitable for sensitive skin; traditional Chinese medicine whitening extracts such as coarse powder / extract of silkworm pupae have problems such as low transdermal absorption of large molecules, fishy smell, and potential allergenic risks; moreover, most whitening products only act on a single link in melanin production, resulting in a single whitening pathway and limited effects.

[0003] Meanwhile, although silkworm pupae have a thousand-year history of whitening and freckle removal in traditional Chinese medicine beauty, their industrial application in cosmetics is limited by insufficient raw material modification technology, and the small-molecule transformation of active ingredients and removal of risk factors have not been achieved. Although vitamin C and its derivatives are classic whitening ingredients, the original vitamin C is highly acidic and has poor stability, resulting in poor compatibility with the formulation of Chinese medicine extracts. High-concentration use can easily cause skin redness and irritation, making it difficult to synergistically enhance the effects of Chinese medicine ingredients.

[0004] In addition, current consumer demand for whitening products has shifted from simply whitening to "whitening and repairing," especially for people with post-inflammatory hyperpigmentation or post-cosmetic procedures. They need gentle, non-irritating whitening products that combine anti-inflammatory and barrier repair properties, but existing products are unable to meet this demand.

[0005] Therefore, developing a composite composition that combines classic Chinese medicine ingredients with modern biotechnology and is suitable for sensitive skin has become an urgent need in the cosmetics industry. Summary of the Invention

[0006] The purpose of this invention is to provide a whitening and repairing composition of white silkworm polypeptide, its preparation method and application, in order to solve the problem mentioned in the background art that the whitening effect of traditional white silkworm based on traditional Chinese medicine beauty is difficult to guarantee the dual effects of whitening and repair.

[0007] To achieve the above objectives, the present invention provides the following technical solution:

[0008] A white silkworm polypeptide complex whitening and repairing composition, by weight percentage, contains the following core active ingredients: fermented white silkworm oligopeptide 3-5%, ethyl vitamin C 2-3%, and 4D hyaluronic acid 1-2%.

[0009] Preferably, the fermented silkworm oligopeptides are low-molecular-weight oligopeptides obtained from silkworm through bidirectional fermentation with probiotics, enzymatic hydrolysis, and 0.3–3kDa ultrafiltration fractionation. After desalting and de-small molecule treatment, potential risk factors such as ammonium oxalate and beautifier are removed, resulting in high transdermal absorption rate, no fishy smell, and reduced risk of allergy.

[0010] Preferably, ethyl vitamin C, as a vitamin C derivative, is stable, lipophilic and hydrophilic, and has perfect compatibility with silkworm oligopeptides at pH 5.5-6.0, thus avoiding the strong acidity irritation of the original vitamin C.

[0011] Preferably, the 4D hyaluronic acid is a compound system of hyaluronic acid with different molecular weights, including small molecule, medium molecule, large molecule and supramolecular hyaluronic acid, used to construct a three-dimensional water storage and transdermal carrier system.

[0012] The present invention also discloses a method for preparing the above composition, comprising the following steps:

[0013] To prepare fermented *Bombyx mori* oligopeptides, *Bombyx mori* raw materials conforming to the standards of the *Pharmacopoeia of the People's Republic of China* were used. After batch-by-batch traceability and testing for fungal contamination, pesticide residues, and heavy metals, probiotic activation was performed. The activated probiotics were then mixed with the *Bombyx mori* raw materials for bidirectional fermentation, controlled at a temperature of 30-37℃, pH 6.0-7.0, and a fermentation time of 48-72 hours. This process achieved the initial degradation of macromolecular proteins in *Bombyx mori*, while simultaneously deodorizing, desensitizing, and enriching active ingredients such as *Bombyx mori* extract. The fermentation product was then extracted with deionized water. A complex enzyme consisting of neutral protease and papain was added to the liquid and enzymatically hydrolyzed at 45-50℃ for 2-4 hours to completely degrade the protein into peptides. After hydrolysis, the enzyme was inactivated by high temperature. The hydrolysate was fractionated using a 0.3–3 kDa ultrafiltration membrane to screen for functional peptide windows that combine permeability and stability. The product was then desalted and de-small molecule treated with a resin column to remove potential risk factors such as ammonium oxalate and beauveria bassiana. Finally, the product was sterilized and filtered, and quality control was performed using LC-MS peptidomics to ensure batch consistency, yielding the fermented silkworm oligopeptide stock solution.

[0014] To prepare the aqueous matrix, heat deionized water to 70-80℃, add 4D hyaluronic acid, moisturizers such as glycerin and propylene glycol, and thickeners such as xanthan gum, and stir rapidly until completely dissolved to form a homogeneous aqueous matrix. Slowly cool to 35-40℃ to avoid high temperature damaging the activity of subsequent active ingredients.

[0015] Add fermented silkworm oligopeptide stock solution to the above aqueous matrix and stir at low speed for 15-20 minutes until homogeneous; then add stabilizers such as ethyl vitamin C and disodium EDTA, and soothing agents such as panthenol / ceramide, adjust the pH of the system to 5.5-6.0 using citric acid / triethanolamine, and continue stirring for 10-15 minutes until the system is homogeneous and free of particles to obtain the composition base.

[0016] The dual-compartment packaging uses the composite base material as the aqueous phase compartment and oil-soluble VC powder or VC-IP essence as the active phase compartment. It is packaged with a dual-compartment pump head, and is squeezed and mixed during use to ensure the freshness of the VC ingredients and avoid premature oxidation and failure.

[0017] The composition of the present invention can be used to prepare various whitening and repairing cosmetics, such as serums, lotions, creams, and masks. During preparation, emulsifiers, preservatives, fragrances and other excipients that comply with cosmetic regulations can be added according to the requirements of cosmetic dosage forms. The process is simple and can be mass-produced.

[0018] Preferably, the compound enzymatic hydrolysis uses a combination of neutral protease and papain, with a hydrolysis temperature of 45-50℃ and a hydrolysis time of 2-4 hours, followed by enzyme inactivation treatment.

[0019] Preferably, the pH of the system is adjusted by citric acid / triethanolamine, and the added soothing agent is one or a combination of two of panthenol and ceramide.

[0020] Compared with the prior art, the beneficial effects of the present invention are:

[0021] The composition of this invention achieves complementary mechanisms between fermented silkworm oligopeptides and ethyl vitamin C. Silkworm oligopeptides inhibit melanin synthesis and have anti-inflammatory and soothing effects, while ethyl vitamin C reduces melanin and has antioxidant effects. The two work synergistically to achieve whitening through all pathways, solving the problem of single pathway in traditional whitening products. Furthermore, the anti-inflammatory effect of silkworm alleviates the potential irritation of vitamin C and improves the gentleness of the product.

[0022] This invention involves bio-fermentation and fractional purification of *Bombyx mori* to obtain low-molecular-weight oligopeptides of 0.3–3 kDa. This solves the problems of low transdermal permeability, fishy smell, and allergenicity associated with traditional *Bombyx mori* extracts, while also removing potential risk factors. The raw materials are controllable and safe and compliant.

[0023] This invention selects ethyl vitamin C and 4D hyaluronic acid, which have good compatibility with the fermented silkworm oligopeptide formula. 4D hyaluronic acid not only moisturizes and repairs, but also acts as a transdermal carrier to promote the skin penetration of silkworm oligopeptides and vitamin C, thereby improving the utilization rate of active ingredients.

[0024] The preparation process of this invention adopts technologies such as bio-fermentation, ultrafiltration fractionation, and dual-compartment encapsulation. The process is controllable and can be mass-produced. The dual-compartment technology ensures the activity of VC components, avoids premature oxidation, and improves the product's shelf life and efficacy.

[0025] The composition of this invention has both whitening and repairing effects, and is suitable for various groups such as those with sensitive skin and those who have undergone cosmetic procedures. It also allows for the phased development of ordinary cosmetics and special cosmetics, meets national cosmetic regulatory requirements, and has broad prospects for industrial application.

[0026] This invention combines the classic TCM beauty ingredient, silkworm pupae, with modern biotechnology to create a "TCM technology" whitening and skincare system. It aligns with the consumer trend of green skincare and natural extracts, and has unique market selling points. Attached Figure Description

[0027] Figure 1 Comparison of tyrosinase inhibition rates in different samples (column chart)

[0028] Figure 2 The graph showing the changes in skin efficacy indicators in human patients over 28 days in this embodiment of the invention. Detailed Implementation

[0029] The technical solutions of the embodiments of the present invention will be clearly and completely described below with reference to the accompanying drawings. Obviously, the described embodiments are only some embodiments of the present invention, and not all embodiments. Based on the embodiments of the present invention, all other embodiments obtained by those skilled in the art without creative effort are within the scope of protection of the present invention.

[0030] Combination Figure 1 - Figure 2 As shown:

[0031] Example 1:

[0032] White Silkworm Peptide Complex Whitening and Repairing Essence

[0033] Key active ingredients (by weight): Fermented silkworm oligopeptide 3%, ethyl vitamin C 2%, 4D hyaluronic acid 1%;

[0034] Excipients (by weight): 5% glycerin, 3% propylene glycol, 0.1% xanthan gum, 1% panthenol, 0.5% ceramide, 0.05% disodium EDTA, appropriate amount of triethanolamine, appropriate amount of citric acid, deionized water to 100%;

[0035] Preparation method: (1) Prepare fermented silkworm oligopeptide stock solution according to the above process; (2) Heat deionized water to 75°C, add 4D hyaluronic acid, glycerin, propylene glycol and xanthan gum, stir until dissolved, and cool to 38°C; (3) Add fermented silkworm oligopeptide stock solution, stir for 20 min, add ethyl vitamin C, panthenol, ceramide and disodium EDTA, adjust pH to 5.8 with citric acid / triethanolamine, and stir for 15 min; (4) Dual-compartment encapsulation: the aqueous phase compartment is the above base material, and the active compartment is VC-IP essence to obtain whitening and repairing essence.

[0036] Example 2: White Silkworm Polypeptide Complex Whitening and Repairing Face Cream

[0037] Key active ingredients (by weight): Fermented silkworm oligopeptide 5%, ethyl vitamin C 3%, 4D hyaluronic acid 2%;

[0038] Excipients (by weight): Squalane 3%, Shea Butter 2%, Polyglycerol-6 Distearate 0.8%, Glycerin 6%, 1,3-Propanediol 4%, Carbomer 0.15%, Panthenol 1.5%, Disodium EDTA 0.08%, Triethanolamine (as needed), Citric Acid (as needed), Deionized Water to 100%;

[0039] Preparation method: (1) Prepare fermented silkworm oligopeptide stock solution; (2) Oil phase preparation: Heat squalane, shea butter and polyglycerol-6 distearate to 75°C and stir until dissolved; (3) Aqueous phase preparation: Heat deionized water to 75°C, add 4D hyaluronic acid, glycerin, 1,3-propanediol and carbomer, stir until dissolved, and cool to 40°C; (4) Emulsification and compounding: Slowly add the oil phase to the aqueous phase, emulsify at high speed for 10 min, add fermented silkworm oligopeptide stock solution, stir for 15 min, then add ethyl vitamin C, panthenol and disodium EDTA, adjust pH to 5.5, and stir for 10 min; (5) Dual-compartment packaging: The aqueous phase compartment is the cream base material and the active compartment is VC powder to obtain whitening and repairing face cream.

[0040] Efficacy verification

[0041] The in vitro and human efficacy verification of the essence prepared in Example 1 was conducted:

[0042] In vitro tyrosinase inhibition rate test: After fermented silkworm oligopeptide was combined with ethyl vitamin C, the tyrosinase inhibition rate reached 89.2%, which was significantly higher than that of the single component;

[0043] The results are as follows Figure 1 As shown, the tyrosinase inhibition rate of the fermented crude extract of *Bombyx mori* was 52.4% ± 3.1%, while the inhibition rate of the fermented *Bombyx mori* oligopeptide of this invention was significantly improved, exceeding that of the positive control arbutin group, and the difference was statistically significant (P < 0.01). This indicates that the composition of this invention has a significant synergistic effect in inhibiting tyrosinase activity.

[0044] Human patch test: 30 volunteers received patches continuously for 24 hours, with no redness, swelling, itching, or other irritation reactions, demonstrating 100% mildness; results are as follows. Figure 2 As shown.

[0045] 28-day human clinical trial: After use in 40 volunteers with post-inflammatory hyperpigmentation, the skin L* value increased by an average of 12.5%, the melanin index decreased by an average of 18.3%, the visibility of acne marks / sun spots was significantly reduced, and the skin barrier index (transepidermal water loss) decreased by an average of 25.6%.

[0046] Industrial applicability

[0047] The white silkworm polypeptide complex whitening and repairing composition of the present invention has a scientific formula and controllable process, and can be mass-produced into various cosmetic dosage forms such as essence, lotion, face cream, and mask. The products are gentle and non-irritating, with significant whitening and repairing effects, suitable for a wide range of people, and meet the regulatory requirements for cosmetics. It has extremely high industrial applicability and market promotion value.

[0048] In summary, the core mechanism of action of the composition of this invention is a three-dimensional blockade of wind, phlegm, and blood stasis: fermented silkworm oligopeptides inhibit tyrosinase activity from the source, blocking melanin synthesis (phlegm removal); ethyl vitamin C reduces the oxidized melanin that has been generated, promoting melanin metabolism (blood stasis removal); 4D hyaluronic acid repairs the skin barrier, promotes microcirculation, and relieves skin inflammation (wind dispelling). The three work together to achieve whitening through all pathways, while also taking into account anti-inflammatory, soothing, and barrier repair effects.

[0049] This composition is suitable for women aged 25-45, especially those who have undergone chemical peels / microneedling / phototherapy procedures, those with post-acne inflammation and pigmentation, and those with sensitive skin who want to fade marks but cannot tolerate strong whitening agents. It can effectively brighten skin tone, improve dullness, fade sun spots and acne marks, and repair post-medical pigmentation. It is gentle and non-irritating with no significant risk of allergies.

[0050] Regarding cosmetic efficacy claims and compliance, the composition of this invention adopts a phased development strategy: In the first phase, it is used as a general cosmetic, claiming to brighten skin tone, improve dullness, even out skin tone, and repair the skin barrier. It does not require special cosmetic registration, has a short development cycle, and low cost. In the second phase, after completing human efficacy tests by a cosmetic registration / filing testing agency, it is filed in accordance with the "Cosmetic Efficacy Claim Evaluation Standard" and can be used as a special cosmetic to claim to remove spots and whiten skin, which meets the national cosmetic regulatory requirements.

[0051] Furthermore, if the fermented silkworm oligopeptide prepared by this invention is structurally confirmed as a novel active ingredient, and its process and application are significantly innovative, it can be deployed in accordance with the cosmetic new raw material registration / filing system, combined with patent protection, to form a core technology barrier.

[0052] It should be understood that numerous specific implementation decisions can be made during the development of any practical implementation, such as in any engineering or design project. Such development efforts may be complex and time-consuming, but for those skilled in the art who benefit from this disclosure, the development effort will be a routine work of design, manufacturing, and production without requiring much experimentation.

[0053] It should be noted that the above embodiments are only used to illustrate the technical solutions of the present invention and are not intended to limit it. Although the present invention has been described in detail with reference to preferred embodiments, those skilled in the art should understand that modifications or equivalent substitutions can be made to the technical solutions of the present invention without departing from the spirit and scope of the technical solutions of the present invention, and all such modifications or substitutions should be covered within the scope of the claims of the present invention.

Claims

1. A whitening and repairing composition of white silkworm polypeptide complex, characterized in that, By weight percentage, it contains the following core active ingredients: 3-5% fermented silkworm oligopeptide, 2-3% ethyl vitamin C, and 1-2% 4D hyaluronic acid; the fermented silkworm oligopeptide is a 0.3-3kDa oligopeptide fraction obtained from silkworm through bio-fermentation, enzymatic hydrolysis, and ultrafiltration fractionation, and has had potential risk factors including ammonium oxalate and beauveria bassiana removed.

2. The whitening and repairing composition according to claim 1, characterized in that: The preparation process of the fermented white silkworm oligopeptides includes: using pharmacopoeia-grade white silkworm as raw material, through probiotic bidirectional fermentation, water extraction and enzymatic hydrolysis, 0.3–3kDa ultrafiltration fractionation, resin desalting and small molecule removal, and LC–MS peptidomics quality control, to obtain batch-consistent white silkworm oligopeptides, and the raw material has passed the tests for fungal contamination, pesticide residues and heavy metals.

3. The whitening and repairing composition according to claim 1, characterized in that: The 4D hyaluronic acid is a compound system of hyaluronic acid with different molecular weights, including small molecule, medium molecule, large molecule and supramolecular hyaluronic acid, which is used to construct a three-dimensional water storage and transdermal carrier system.

4. A method for preparing a whitening and repairing composition, used to prepare the white silkworm polypeptide complex whitening and repairing composition as described in any one of claims 1-3, characterized in that: Includes the following steps: S1. Preparation of fermented silkworm oligopeptides: Pharmacopoeia-grade white silkworms were used, and after activation with probiotic strains, they were subjected to two-way fermentation. The fermentation temperature was controlled at 30-37℃, pH at 6.0-7.0, and the fermentation time was 48-72 hours. The fermentation product was extracted with water, hydrolyzed with compound enzymes, and then fractionated using a 0.3-3kDa ultrafiltration membrane. After desalting and removing small molecules through a resin column, it was sterilized and filtered to obtain fermented white silkworm oligopeptide stock solution. S2. Preparation of aqueous matrix: Heat deionized water to 70-80℃, add 4D hyaluronic acid, moisturizer, and thickener, stir until completely dissolved, and cool to 35-40℃. S3, Compound Efficacy Components: Add fermented silkworm oligopeptide stock solution to the aqueous matrix of S2, stir evenly, add ethyl vitamin C, stabilizer, and soothing agent, adjust the pH of the system to 5.5-6.0, stir until homogeneous, and obtain the composition base material; S4, Dual-compartment encapsulation: The composition base material of S3 is used as the aqueous phase compartment, and oil-soluble VC powder / essence is used as the active phase compartment. The product is obtained by encapsulating with a dual-compartment pump head.

5. The preparation method according to claim 4, characterized in that: The compound enzymatic hydrolysis described in S1 uses a combination of neutral protease and papain, with a hydrolysis temperature of 45-50℃ and a hydrolysis time of 2-4 hours. After hydrolysis, the enzyme is inactivated.

6. The preparation method according to claim 4, characterized in that: The pH of the system described in S3 is adjusted by citric acid / triethanolamine, and the added soothing agent is one or a combination of two of panthenol and ceramide.

7. The application of the white silkworm polypeptide complex whitening and repairing composition as described in any one of claims 1-3 in the preparation of whitening and repairing cosmetics, characterized in that, The cosmetic product is one of the following: serum, lotion, cream, or mask. It is suitable for brightening skin tone, improving post-inflammatory hyperpigmentation, fading sun spots / acne marks, and repairing hyperpigmentation after cosmetic procedures. It is also suitable for people with sensitive skin.

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