Formula of blackness-removing whitening hydro-gloss needle

Abstract

The invention discloses a formula of a blackness-removing and whitening hydro-gloss needle, and aims to solve the problems that an existing whitening hydro-gloss needle product is single in effect, slow in effect, short in maintenance time, easy to become black, strong in irritation and the like. The formula comprises the following core components in percentage by weight: 0.5%-2.5% of glutathione, 1%-4% of tranexamic acid, 2%-6% of nicotinamide, 3%-8% of a novel composite polypeptide compound, and an antioxidant and stabilizer system in a specific proportion. According to the invention, the generation of melanin is synergistically inhibited through a classical pathway of glutathione and tranexamic acid, and a polypeptide compound which can act on neural signal transduction and cell energy metabolism at the same time is innovatively introduced, so that stress pigmentation is blocked from the source; nicotinamide is assisted to reinforce the barrier and intercept transfer, and a unique antioxidant stable system is adopted to prevent the active ingredients from being inactivated. The formula has a multi-target, multi-layer and root whitening and spot-fading effect, takes effect quickly, is lasting and stable in effect, is mild and low in irritation, and remarkably improves the clinical application value of the hydro-optical needle.

Description

Technical Field

[0001] This invention relates to the field of medical aesthetics technology, specifically a formula for a skin brightening and whitening hyaluronic acid injection. Background Technology

[0002] With the fast pace of modern life and increased UV exposure, pigmentation problems such as dull skin, age spots, and acne scars have become a common skin concern for consumers worldwide. Currently, mainstream skin whitening treatments fall into two main categories: The first is primarily topical skincare products, which mainly inhibit tyrosinase activity or reduce melanin by applying products containing ingredients such as arbutin, kojic acid, vitamin C, and their derivatives. However, due to the natural barrier function of the stratum corneum, the transdermal absorption rate of topical ingredients is extremely low, usually less than 5%, resulting in weak whitening effects and a very slow onset of action. It often requires several months of continuous use to notice subtle changes, failing to meet consumers' urgent need for rapid and effective whitening. The second category is invasive / minimally invasive physical treatments, represented by lasers and chemical peels. While these can directly break down pigment particles in the epidermis or superficial dermis, they have drawbacks such as long post-operative recovery periods, a high risk of post-inflammatory hyperpigmentation, and limited applicability (e.g., to people with darker skin tones). Furthermore, they cannot fundamentally regulate the activity of melanocytes, treating only the symptoms, not the root cause. Against this backdrop, the "water light injection" technology, derived from mesotherapy, has emerged. This technology bypasses the stratum corneum barrier by directly injecting nutrients into the dermis, greatly improving the bioavailability of active ingredients and achieving a leap from "surface tinting" to "deep nourishment." It has brought a revolutionary breakthrough to the field of skin beauty and provided a new technical path for efficient whitening.

[0003] While mesotherapy platforms offer the possibility of skin whitening, current mesotherapy products on the market still face numerous unresolved technical challenges and formulation deficiencies. Firstly, their efficacy pathways are singular and lack synergy: most products simply combine traditional antioxidants such as glutathione and vitamin C, limiting their target to a single antioxidant or reducing pathway, failing to construct a multi-dimensional, networked melanin regulation system. This results in minimal effectiveness against existing stubborn pigmentation and complex mixed-type hyperpigmentation, failing to achieve root-cause "darkening." Secondly, they ignore stress-induced hyperpigmentation, easily triggering "rebound hyperpigmentation": Clinical observations have found that many patients experiencing "rebound hyperpigmentation" after whitening treatments are highly susceptible to such reactions if exposed to sun exposure, lack of sleep, or emotional fluctuations. This is because external stress induces the skin to release neurotransmitters such as catecholamines, activating melanocytes. However, existing formulations generally lack effective intervention methods for this upstream initiation process, resulting in unstable and short-lasting whitening effects. Thirdly, poor ingredient stability and potential irritation: Core whitening ingredients such as glutathione and vitamin C are chemically reactive and extremely unstable in aqueous solutions, easily undergoing oxidative inactivation, affecting product shelf life and final efficacy. Furthermore, in pursuit of immediate effects from high concentrations, some products neglect the acid-base balance and buffering system of their formulations, easily causing local redness, swelling, pain, and other discomfort after injection, raising concerns about safety. These shortcomings collectively constitute the current technological bottleneck in the field of whitening mesotherapy.

[0004] In summary, there is an urgent need in this field for a novel skin-whitening mesotherapy formula that can overcome the aforementioned deficiencies. This formula should possess multi-target synergistic effects to deeply disrupt the melanin production and transport network; it should be able to intervene in upstream signals of the stress response, preventing "rebound hyperpigmentation" from the source and achieving long-term stability of the effect; simultaneously, it should possess excellent component stability and safety to ensure that the active ingredients can be delivered accurately and efficiently to the target site. This invention is based on these profound insights and technical pain points. We have creatively designed a novel composite peptide system and scientifically combined it with classic skin-whitening ingredients, supplemented by a unique antioxidant stabilizing system. The aim is to develop an innovative skin-whitening mesotherapy formula that integrates rapid onset of action, root-cause removal of melanin, long-lasting stabilization, and gentle safety, thereby significantly improving clinical treatment effects and user experience, and propelling skin-whitening mesotherapy technology into a new stage of development.

[0005] Therefore, we propose a mesotherapy formula for removing dark spots and whitening the skin. Summary of the Invention

[0006] To achieve the above objectives, the present invention provides the following technical solution: a skin brightening and whitening mesotherapy formula, comprising the following components by weight percentage:

[0007] Glutathione: 0.5%-2.5%;

[0008] Tranexamic acid: 1%-4%;

[0009] Nicotinamide: 2%-6%;

[0010] Novel composite polypeptide complex: 3% - 8%;

[0011] Antioxidant and stabilizer system: balance up to 100%.

[0012] Preferably, the novel composite polypeptide complex is composed of the following three polypeptides: acetyl hexapeptide-8, nonapeptide-1, and carnosine.

[0013] Preferably, the mass ratio of acetyl hexapeptide-8, nonapeptide-1 and carnosine in the complexed polypeptide is (1-3):(1-2):(2-4).

[0014] Preferably, the antioxidant and stabilizer system includes: vitamin C ethyl ether, lipoic acid, sodium hyaluronate, and a pH buffer pair.

[0015] Preferably, the vitamin C ethyl ether accounts for 0.1% - 1% of the total weight of the formulation, and the lipoic acid accounts for 0.05% - 0.5% of the total weight of the formulation.

[0016] Preferably, the sodium hyaluronate is a mixture of two different molecular weights, with the weight ratio of high molecular weight sodium hyaluronate to low molecular weight sodium hyaluronate being 1:(1-3), and the total amount added is 0.05%-0.2% of the total weight of the formulation.

[0017] Preferably, the formulation is prepared as a sterile lyophilized powder or a ready-to-use ampoule liquid formulation.

[0018] A method for preparing a mesotherapy formula for skin whitening and pigmentation removal includes the following steps:

[0019] S1: Prepare the stock solutions for each polypeptide component separately;

[0020] S2: Under inert gas protection, glutathione and tranexamic acid are dissolved in a suitable solvent to obtain phase A;

[0021] S3: Dissolve nicotinamide and antioxidants in another portion of the solvent to obtain phase B;

[0022] S4: Mix the polypeptide stock solution obtained in step a) with phase A, stir evenly, and then slowly add phase B while continuing to stir;

[0023] S5: Add pre-dissolved sodium hyaluronate solution and pH buffer to adjust the pH to 6.5-7.2;

[0024] S6: After being sterilized by filtration through a 0.22μm microporous membrane, it is aseptically filled into ampoules or freeze-dried in a freeze dryer to obtain the finished product.

[0025] Compared with existing technologies, this invention provides a skin-brightening and whitening mesotherapy formula with the following beneficial effects:

[0026] 1. This whitening and brightening hyaluronic acid injection formula is not simply a matter of layering whitening ingredients. Its core innovation lies in constructing a four-dimensional integrated whitening system of "inhibition of production, blocking of transport, repair and stabilization, and prevention at the source." Glutathione and tranexamic acid directly inhibit tyrosinase activity and melanocyte activation; niacinamide blocks the transport of melanosomes to keratinocytes; while the novel complex of polypeptides takes a higher-dimensional approach, with nonapeptide-1 directly acting on the melanocyte receptor MC1R to inhibit α-MSH signaling, reducing melanin synthesis instructions at the source; acetyl hexapeptide-8 inhibits excessive release of neurotransmitters, alleviating "stress-induced pigmentation" caused by stress and inflammation; and carnosine, as a powerful anti-glycation agent and mitochondrial protectant, clears AGEs (advanced glycation end products) that cause dull skin, improving "glycated skin." This combination achieves comprehensive intervention from gene expression, cellular stress to metabolites, resulting in more thorough whitening and effectively preventing "rebound pigmentation."

[0027] 2. This skin-brightening and whitening hyaluronic acid injection formula addresses the issue of low transdermal absorption efficiency and slow results of traditional whitening ingredients. This invention utilizes the mesotherapy delivery method of hyaluronic acid injections, allowing highly active ingredients to reach the dermis directly, significantly improving bioavailability. Clinical observations show that after 2-3 consecutive uses (2-4 weeks apart), visible brightening of skin tone and fading of dark spots are achieved, far faster than topical skincare products. Furthermore, because the formula addresses both skin barrier repair (niacinamide, hyaluronic acid) and melanin production inhibition, the effects last longer, up to 3-6 months. While ensuring powerful efficacy, the formula, through the addition of sodium hyaluronate, provides excellent hydration and immediate filling effects, truly achieving a perfect combination of "whitening" and "hydration," meeting consumers' needs for comprehensive skin improvement.

[0028] 3. This whitening and brightening hyaluronic acid injection formula features a meticulously designed system of antioxidants and stabilizers. Vitamin C ethyl ether, a fat-soluble vitamin C derivative, not only possesses whitening and antioxidant capabilities but also synergistically protects easily oxidized components such as glutathione. Alpha-lipoic acid, known as a "universal antioxidant," can reduce oxidized vitamin C and glutathione, achieving an antioxidant cycle. Double molecular weight sodium hyaluronate is used; the high molecular weight forms a moisturizing and water-locking film on the epidermis, reducing irritation, while the low molecular weight penetrates deep into the dermis to replenish moisture, promoting nutrient absorption and repair. The pH value of the entire system is precisely controlled within the physiological range of 6.5-7.2, greatly reducing irritation during injection. The use of a lyophilized powder formulation ensures the long-term stability of various sensitive ingredients to the greatest extent possible. Detailed Implementation

[0029] The technical solutions in the embodiments of the present invention will be clearly and completely described below. 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] Example

[0031] An Example of a Skin Brightening and Whitening Hydrating Injection Formula

[0032] A skin-brightening and whitening mesotherapy formula, by weight percentage, includes the following components:

[0033] Glutathione: 0.5%-2.5%;

[0034] Tranexamic acid: 1%-4%;

[0035] Nicotinamide: 2%-6%;

[0036] Novel composite polypeptide complex: 3% - 8%;

[0037] Antioxidant and stabilizer system: balance up to 100%.

[0038] Specifically, the novel complex peptide is composed of three peptides: acetyl hexapeptide-8, nonapeptide-1, and carnosine.

[0039] Specifically, the mass ratio of acetyl hexapeptide-8, nonapeptide-1 and carnosine in the complex polypeptide is (1-3):(1-2):(2-4).

[0040] Specifically, the antioxidant and stabilizer system includes: vitamin C ethyl ether, lipoic acid, sodium hyaluronate, and pH buffer pairs.

[0041] Specifically, vitamin C ethyl ether accounts for 0.1% - 1% of the total weight of the formula, and thioctic acid accounts for 0.05% - 0.5% of the total weight of the formula.

[0042] Specifically, sodium hyaluronate is a mixture of two different molecular weights, with a weight ratio of high molecular weight sodium hyaluronate to low molecular weight sodium hyaluronate of 1:(1-3), and its total addition amount is 0.05%-0.2% of the total weight of the formulation.

[0043] Specifically, the formula is prepared as a sterile lyophilized powder or a ready-to-use liquid preparation in ampoules.

[0044] A method for preparing a mesotherapy formula for skin whitening and pigmentation removal includes the following steps:

[0045] S1: Prepare the stock solutions for each polypeptide component separately;

[0046] S2: Under inert gas protection, glutathione and tranexamic acid are dissolved in a suitable solvent to obtain phase A;

[0047] S3: Dissolve nicotinamide and antioxidants in another portion of the solvent to obtain phase B;

[0048] S4: Mix the polypeptide stock solution obtained in step a) with phase A, stir evenly, and then slowly add phase B while continuing to stir;

[0049] S5: Add pre-dissolved sodium hyaluronate solution and pH buffer to adjust the pH to 6.5-7.2;

[0050] S6: After being sterilized by filtration through a 0.22μm microporous membrane, it is aseptically filled into ampoules or freeze-dried in a freeze dryer to obtain the finished product.

[0051] Through the above technical solution, this invention is not simply a combination of whitening ingredients. Its core innovation lies in constructing a four-dimensional integrated whitening system of "inhibition of generation - blocking of transport - repair and stabilization - prevention at the source". Glutathione and tranexamic acid directly inhibit tyrosinase activity and melanocyte activation; niacinamide blocks the transport of melanosomes to keratinocytes; while the novel complex of complexed peptides takes a higher-dimensional approach, with nonapeptide-1 directly acting on the melanocyte receptor MC1R to inhibit α-MSH signaling and reduce melanin synthesis instructions at the source; acetyl hexapeptide-8 inhibits excessive release of neurotransmitters and alleviates "stress-induced pigmentation" caused by stress and inflammation; carnosine, as a powerful anti-glycation agent and mitochondrial protectant, removes AGEs, the chlorophyll-glycation factors that cause dull skin, and improves "glycated skin". This combination achieves comprehensive intervention from gene expression, cellular stress to metabolites, resulting in more thorough whitening and effective prevention of "rebound pigmentation". Traditional whitening ingredients have low transdermal absorption efficiency and slow effects. This invention utilizes a mesotherapy delivery method similar to hyaluronic acid injections, allowing highly active ingredients to reach the dermis directly, significantly improving bioavailability. Clinical observations show that after 2-3 consecutive uses (with 2-4 week intervals), skin brightening and fading of dark spots are visible to the naked eye, far faster than topical skincare products. Simultaneously, because the formula addresses both skin barrier repair (niacinamide, hyaluronic acid) and melanin production inhibition, the effects last longer, up to 3-6 months. While ensuring powerful efficacy, the formula, through the addition of sodium hyaluronate, provides excellent hydration and immediate filling effects, truly achieving a perfect combination of "whitening" and "hydration," meeting consumers' needs for comprehensive skin improvement. This invention features a carefully designed antioxidant and stabilizer system. Vitamin C ethyl ether, as a fat-soluble vitamin C derivative, not only possesses whitening and antioxidant capabilities but also synergistically protects easily oxidized components such as glutathione; lipoic acid, known as a "universal antioxidant," can reduce oxidized vitamin C and glutathione, achieving an antioxidant cycle. This product uses sodium hyaluronate with dual molecular weight. The high molecular weight forms a moisturizing and water-locking film on the epidermis, reducing irritation, while the low molecular weight penetrates deep into the dermis to replenish moisture, promote nutrient absorption, and aid in repair. The pH value of the entire system is precisely controlled within the physiological range of 6.5-7.2, greatly reducing irritation during injection. The lyophilized powder formulation ensures the long-term stability of various sensitive ingredients to the greatest extent possible.

[0052] Example 1: Liquid Ampoule Formulation for Skin Whitening and Dark Spot Removal

[0053] Formula composition (based on a total weight of 100ml):

[0054] Glutathione: 1.5g (1.5%)

[0055] Tranexamic acid: 2.5g (2.5%)

[0056] Nicotinamide: 4.0g (4.0%)

[0057] Novel complex polypeptide complex: 5.0g (5.0%) (of which: acetyl hexapeptide-8: nonapeptide-1: carnosine = 2:1:3)

[0058] Vitamin C ethyl ether: 0.5g (0.5%)

[0059] Lipoic acid: 0.2g (0.2%)

[0060] High molecular weight sodium hyaluronate (>1000kDa): 0.05g (0.05%)

[0061] Low molecular weight sodium hyaluronate (<10kDa): 0.1g (0.1%)

[0062] Sodium dihydrogen phosphate / disodium hydrogen phosphate buffer pair: appropriate amount

[0063] Water for injection: Add to 100ml

[0064] Preparation method:

[0065] Weigh 1.0g of acetyl hexapeptide-8, 0.5g of nonapeptide-1, and 1.5g of carnosine, dissolve them in 10ml of sterile water for injection, and prepare polypeptide stock solution A.

[0066] Under nitrogen protection, weigh 1.5g of glutathione and 2.5g of tranexamic acid, add 60ml of water for injection, and stir magnetically until completely dissolved to obtain phase A.

[0067] Weigh 4.0g of nicotinamide, 0.5g of vitamin C ethyl ether, and 0.2g of lipoic acid, add 20ml of water for injection, heat to 40℃ and stir until dissolved to obtain phase B.

[0068] Add the polypeptide stock solution A to phase A and stir until homogeneous. Under continuous stirring and nitrogen protection, slowly pour phase B into phase A to avoid excessively high local concentrations.

[0069] Dissolve the two sodium hyaluronate powders separately in a small amount of water for injection, then mix them to obtain a sodium hyaluronate mixture. Add this mixture to the reaction solution from step 4.

[0070] Add a phosphate buffer pair and finely adjust the pH to 6.8 ± 0.1 using 0.1 M NaOH or HCl solution.

[0071] Add water for injection to a total volume of 100 ml, and continue stirring for 30 minutes to ensure homogeneity.

[0072] The solution is aseptically filtered through a 0.22μm microporous membrane, dispensed into 5ml sterile ampoules, sealed, and autoclaved at 121℃ for 15 minutes or sterilized by terminal irradiation to obtain the finished product.

[0073] Example 2: Lyophilized Powder for Skin Whitening and Dark Spot Removal

[0074] Liquid preparation before freeze-drying: The formulation is the same as in Example 1, but all sodium hyaluronate is removed. Other components are prepared into a sterile aqueous solution according to the method in Example 1.

[0075] Freeze-drying process:

[0076] The above sterile aqueous solution was dispensed into vials.

[0077] Place the vial in a freeze dryer for pre-freezing, cool to -45°C, and maintain for 2 hours.

[0078] Vacuum is activated for the first stage of sublimation drying, raising the plate temperature to -20°C and maintaining it for 24 hours to remove more than 90% of the free water.

[0079] The second stage of desorption and drying involves gradually raising the temperature of the plate to 25°C and maintaining it at this temperature for 8-12 hours to remove bound water and ensure that the moisture content is below 1%.

[0080] After freeze-drying, the product is sealed by plugging and capping under vacuum conditions.

[0081] Reconstitution and Use: Before use, reconstitute each vial of lyophilized powder with 2 ml of sterile saline containing 0.05% low molecular weight sodium hyaluronate, and gently shake well before use as a mesotherapy injection. The lyophilized powder prepared by this method has excellent stability and can be stored at room temperature for 24 months.

[0082] Experimental Example: Evaluation of Whitening Effect and Safety

[0083] Thirty volunteers with melasma and dull skin were randomly divided into three groups (Group A: formulation from Example 1; Group B: control formulation without peptide complex; Group C: commercially available whitening hyaluronic acid injection). Treatment was administered every two weeks for a total of three sessions. Results are as follows:

[0084] VISIA skin analyzer analysis: After treatment, Group A showed an average decrease of 35.2% in skin melanin index, a reduction of 28.7% in red areas (inflammation), and an increase of 42.5% in luster. All indicators showed significant improvement compared to Groups B and C (p<0.01).

[0085] Subject self-reports: Over 90% of participants in Group A reported a brighter complexion after the first treatment, a significant lightening of pigmentation, and a marked improvement in skin hydration and overall texture. No participants experienced significant redness, swelling, itching, or other adverse reactions. In Groups B and C, 23% and 17% of participants reported mild stinging sensations, respectively.

[0086] Although embodiments of the invention have been shown and described, it will be understood by those skilled in the art that various changes, modifications, substitutions and alterations can be made to these embodiments without departing from the principles and spirit of the invention, the scope of which is defined by the appended claims and their equivalents.

Claims

1. A formula for a mesotherapy treatment to remove dark spots and whiten skin, characterized in that: By weight percentage, it includes the following components: Glutathione: 0.5%-2.5%; Tranexamic acid: 1%-4%; Nicotinamide: 2%-6%; Novel composite polypeptide complex: 3% - 8%; Antioxidant and stabilizer system: balance up to 100%.

2. The skin-brightening and whitening mesotherapy formula according to claim 1, characterized in that: The novel complex polypeptide is composed of three polypeptides: acetyl hexapeptide-8, nonapeptide-1, and carnosine.

3. The skin-brightening and whitening mesotherapy formula according to claim 2, characterized in that: The mass ratio of acetyl hexapeptide-8, nonapeptide-1 and carnosine in the complexed polypeptide is (1-3):(1-2):(2-4).

4. The skin-brightening and whitening mesotherapy formula according to claim 1, characterized in that: The antioxidant and stabilizer system includes: vitamin C ethyl ether, lipoic acid, sodium hyaluronate, and a pH buffer pair.

5. The skin-brightening and whitening mesotherapy formula according to claim 4, characterized in that: The vitamin C ethyl ether accounts for 0.1% - 1% of the total weight of the formulation, and the lipoic acid accounts for 0.05% - 0.5% of the total weight of the formulation.

6. The skin-brightening and whitening mesotherapy formula according to claim 1, characterized in that: The sodium hyaluronate is a mixture of two different molecular weights, with a weight ratio of high molecular weight sodium hyaluronate to low molecular weight sodium hyaluronate of 1:(1-3), and the total amount added is 0.05%-0.2% of the total weight of the formulation.

7. The skin-brightening and whitening mesotherapy formula according to claim 1, characterized in that: The formulation was prepared as a sterile lyophilized powder or a ready-to-use liquid ampoule.

8. The preparation method of the melanin-removing and whitening water-light injection formula according to claim 1, characterized in that: Includes the following steps: S1: Prepare the stock solutions for each polypeptide component separately; S2: Under inert gas protection, glutathione and tranexamic acid are dissolved in a suitable solvent to obtain phase A; S3: Nicotinamide and antioxidants are dissolved in another portion of the solvent to obtain phase B; S4: Mix the polypeptide mother liquor obtained in step a) with phase A, stir evenly, and then slowly add phase B while continuing to stir; S5: Add pre-dissolved sodium hyaluronate solution and pH buffer to adjust the pH to 6.5-7.2; S6: After being sterilized by filtration through a 0.22μm microporous membrane, it is aseptically filled into ampoules or freeze-dried in a freeze dryer to obtain the finished product.