A whitening composition, a preparation method thereof, and application in solid-state flash-release soluble microneedles
Solid-state flash-release soluble microneedles are prepared by combining a combination of tetrahydromagnanol and nonapeptide-1 with a microneedle skeleton of sodium hyaluronate, low-substituted hydroxypropyl cellulose and mannitol, which solves the problems of insignificant effects and low transdermal absorption rates of existing whitening products, and achieves rapid whitening effects and efficient transdermal delivery.
Patent Information
- Application Number
- CN202511053063.8
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- Filing Date
- 2025-07-30
- Publication Date
- 2025-09-30
- Estimated Expiration
- 2045-07-30
AI Technical Summary
Existing whitening products are not effective, have low transdermal absorption rates and may cause skin irritation. The traditional microneedle preparation process is complex and it is difficult to quickly deliver whitening components.
A combination of tetrahydromagnanol and nonapeptide-1 is used as a whitening ingredient, combined with a microneedle skeleton of sodium hyaluronate, low-substituted hydroxypropyl cellulose and mannitol, and solid-state flash-release soluble microneedles are prepared by freeze-drying to achieve rapid transdermal delivery and stable release.
Significantly improve whitening effect, enhance transdermal absorption rate, reduce the risk of skin irritation, shorten usage time, and improve ease of use.
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Figure CN120549805B_ABST
Abstract
Description
Technical Field
[0001] The present invention relates to the technical field of cosmetics, in particular to a whitening composition, a preparation method thereof, and application thereof in solid-state flash-release soluble microneedles. Background Art
[0002] Skin whitening has long been a research hotspot in the cosmetics field. Existing whitening products often achieve their whitening effects by inhibiting tyrosinase activity and blocking melanin transport. However, these products suffer from limited effectiveness and a single mechanism of action. Some whitening ingredients may irritate the skin, leading to adverse reactions such as allergies. Furthermore, traditional whitening products have limited transdermal absorption, making it difficult to fully utilize the active ingredients.
[0003] Prior art CN118948650A discloses a soluble microneedle patch, comprising a needle tip and a base. The needle tip is made of hydrogel microspheres and microneedle excipients. Components such as isonephrin, oligodeoxyribonucleotides, L-cysteine, and cyclic (proline-tyrosine) synergistically have a significant whitening effect. The microneedles are soluble, and the effective whitening components they contain can only be slowly released into the skin. The microneedles need to be applied to the skin for a long time, which can easily cause the skin to be punctured for a long time, reducing the protective effect and causing inconvenience in use.
[0004] Prior art CN109674737A discloses a rapidly dissolving microneedle based on water-soluble small molecules. The small molecule material is cyclodextrin and its derivatives. These microneedles can dissolve in an aqueous solution in less than ten minutes. However, since human skin is different from aqueous solution, the microneedles still need a long time to dissolve and release the effective components.
[0005] Prior art CN113727751A discloses a microneedle device and a method for manufacturing the same. The device is prepared by injecting two different microneedle components into a mold in sequence to form a microneedle body having a two-layer structure. However, the microneedle preparation process of this method is relatively complex. Since the microneedle model is small and different components are injected in batches to form the microneedle, it is difficult to control the product quality.
[0006] It can be seen that there are still some unresolved technical problems in the existing technology, such as: how to quickly deliver whitening components into the skin, how to improve the whitening effect, etc., so there is an urgent need to develop new whitening cosmetics. Summary of the Invention
[0007] To overcome the shortcomings of the aforementioned prior art, the present invention aims to provide a whitening composition, a preparation method thereof, and its use in solid-state flash-release soluble microneedles. The whitening composition can achieve significant whitening, brightening, and skin tone evenness through the synergistic effect of its components. Furthermore, a preparation method of the composition and its use in solid-state flash-release soluble microneedles are provided. The microneedles can significantly improve the transdermal absorption rate and stability of the whitening composition. The solid-state flash-release properties of the microneedles can save time required for whitening and skin care, thereby enhancing the whitening effect and ease of use of the product.
[0008] In a first aspect, the present invention is achieved through the following technical solutions: providing a whitening composition comprising the following components in parts by weight:
[0009] 0.2-0.4 parts of tetrahydromagnanol,
[0010] Nonapeptide-1 1-2 parts.
[0011] Furthermore, the composition may further comprise at least one of the following components:
[0012] 5-20 parts of moisturizer,
[0013] Thickener 0.1-5 parts,
[0014] Solubilizer 0.1-3 parts,
[0015] 0.1-4 parts of antioxidant,
[0016] 0.01-2 parts of preservatives,
[0017] 0.01-1 part of flavor.
[0018] The moisturizing agent is selected from at least one of glycerin, propylene glycol, butylene glycol and sorbitol.
[0019] The thickener is selected from at least one of carboxyethyl cellulose, carbomer, polyethylene glycol, coconut diethanolamide, xanthan gum, and carrageenan.
[0020] The antioxidant is selected from at least one of gallic acid, vitamin E, vitamin C, and glutathione.
[0021] The solubilizing agent is selected from at least one of Tween, phospholipids, PEG-400, and coconut glucoside.
[0022] The preservative is selected from at least one of methylparaben, ethylparaben, potassium sorbate, sodium benzoate, sodium dehydroacetate, or a composite solution of phenoxyethanol and ethylhexylglycerin.
[0023] Furthermore, the composition also includes water, and the water is deionized water.
[0024] In a second aspect, the present invention provides a method for preparing a whitening composition, comprising weighing each component according to amount and uniformly mixing the components.
[0025] In a third aspect, the present invention further provides a use of a whitening composition in the preparation of solid-state flash-release microneedles.
[0026] The whitening composition is the whitening composition described in the first aspect. The solid-state flash-release microneedles, in addition to the whitening composition, further comprise a microneedle skeleton component, comprising sodium hyaluronate, low-substituted hydroxypropyl cellulose, and mannitol. The weight ratio of sodium hyaluronate, low-substituted hydroxypropyl cellulose, and mannitol is 100:(2-3):(0.5-1).
[0027] The microneedle body has a length of 200-800 μm, preferably 400-600 μm.
[0028] Beneficial effects
[0029] The present invention provides a whitening composition, a preparation method thereof, and its use in solid-state flash-release soluble microneedles. The whitening composition and solid-state flash-release soluble microneedles of the present invention have the following advantages:
[0030] 1) Blocking melanin production throughout the entire process
[0031] Tetrahydromagnanol: It achieves the triple mechanism of "inhibition-blocking-clearance" by inhibiting tyrosinase activity, blocking melanosome transport, and activating autophagy to clear melanin.
[0032] Nonapeptide-1: As a competitive antagonist of α-MSH, it binds to the MC1-R receptor on the surface of melanocytes, inhibits melanin-stimulating signaling, and reduces melanin synthesis.
[0033] Synergistic effect: The two ingredients act on the upstream signaling pathway (nonapeptide-1) and downstream metabolic process (tetrahydromagnanol) of melanin production respectively, forming a complementary inhibitory network. Compared with a single ingredient, the whitening efficiency is significantly improved, and the "whitening + brightening" effect can be further enhanced with the action of a solubilizer (such as coconut glucoside). Compared with a single ingredient or other combination, it can better and more comprehensively solve skin color problems.
[0034] 2) The microneedles effectively improve the transdermal delivery of the whitening components. The solid-state flash-release soluble microneedles described in the present invention use the soluble component sodium hyaluronate as the main skeleton component, and the porosity of the microneedle body is increased by freeze-drying, which is conducive to the absorption of water through capillary action; secondly, low-substituted hydroxypropyl cellulose is an excellent disintegrant. It is mixed with sodium hyaluronate to prepare microneedles. The network structure formed by hydrogen bond cross-linking is beneficial to enhance the strength of the microneedles, and it can swell and disintegrate after absorbing water, promoting the rapid release of the whitening components; at the same time, mannitol has an excellent effect of increasing osmotic pressure and thus enhancing water absorption. Its combination with low-substituted hydroxypropyl cellulose can further enhance the solid-state flash-release function of the microneedles. Obviously, sodium hyaluronate, low-substituted hydroxypropyl cellulose, and mannitol can effectively and synergistically deliver whitening components through the skin quickly. BRIEF DESCRIPTION OF THE DRAWINGS
[0035] Figure 1 This is the HPLC spectrum of the first peak of tetrahydromagnanol in application example 1-3, which is a standard product of tetrahydromagnanol. DETAILED DESCRIPTION
[0036] The following will be combined with the embodiments of the present invention to clearly and completely describe the technical solutions in the embodiments of the present invention. The described embodiments are only some preferred embodiments of the present invention, not all embodiments. Based on the embodiments of the present invention, all other embodiments obtained by ordinary technicians in this field without making creative efforts are within the scope of protection of the present invention.
[0037] In the examples, the experimental methods used are conventional or common methods in the art unless otherwise specified, and the materials, reagents, etc. used are all commercially available unless otherwise specified.
[0038] The raw materials used in the embodiments and comparative examples are now described as follows:
[0039] Sodium hyaluronate: purchased from Bloomage Biotechnology;
[0040] Nonapeptide-1: purchased from Guangzhou Peitao Company;
[0041] Mannitol: purchased from North China Pharmaceutical Co., Ltd. (for injection);
[0042] Sorbitol: purchased from Shaanxi Chenming Biotechnology Co., Ltd.;
[0043] Low-substituted hydroxypropyl cellulose: purchased from Shanghai MacLean Biochemical Technology Co., Ltd.
[0044] Hydroxypropyl cellulose: purchased from Shanghai MacLean Biochemical Technology Co., Ltd.
[0045] Example 1
[0046] A whitening composition, the preparation method of which is as follows:
[0047] Mix 0.3 parts of tetrahydromagnanol, 1.5 parts of nonapeptide-1, and 0.2 parts of coconut glucoside (solubilizer), add deionized water to make up to 100 parts, and mix well.
[0048] The preparation methods of Examples 2-3 and Comparative Examples 1-8 are different from those of Example 1 only in that the components or the amounts of the components are adjusted, and the remaining steps are the same.
[0049] Table 1 Components and weight percentages of the whitening compositions of Examples 1-3 and Comparative Examples 1-8
[0050] Group Tetrahydromagnanol Nonapeptide-1 Coco-Glucoside Tetrapeptide-1 4-Butylresorcinol Resveratrol Tranexamic acid Niacinamide Deionized water Example 1 0.3 1.5 0.2 / / / / / margin Example 2 0.2 2 0.2 / / / / / margin Example 3 0.4 1 0.2 / / / / / margin Comparative Example 1 / 1.5 0.2 / / / / / margin Comparative Example 2 0.3 / 0.2 / / / / / margin Comparative Example 3 0.3 1.5 / / / / / / margin Comparative Example 4 0.3 / 0.2 1.5 / / / / margin Comparative Example 5 / 1.5 0.2 / 0.3 / / / margin Comparative Example 6 / 1.5 0.2 / / 0.3 / / margin Comparative Example 7 / 1.5 0.2 / / / 0.3 / margin Comparative Example 8 / 1.5 0.2 / / / / 0.3 margin
[0051] Note: In the table, “ / ” represents that the corresponding component is not added, and the total amount of all embodiments and comparative examples is the same (100 parts).
[0052] Application Examples 1-3 and Comparative Application Examples 1-12
[0053] Application Example 1
[0054] Sodium hyaluronate, low-substituted hydroxypropyl cellulose and mannitol were mixed in a weight ratio of 100:2.5:0.8, and deionized water was added (the amount of water added was such that the concentration of sodium hyaluronate was 0.5wt%). After sufficient swelling, the mixture was stirred to prepare a microneedle excipient (microneedle skeleton) solution.
[0055] 5 mL of the whitening composition described in Example 1 was selected and mixed evenly with 15 mL of the above-mentioned microneedle excipient solution to obtain a microneedle preparation solution.
[0056] Under vacuum conditions, the microneedle preparation liquid was injected into the microneedle mold, allowed to stand at room temperature until it dried into an elastic gel, freeze-dried, slowly cooled to -25°C, and dried for 1 hour to obtain solid-state flash-release soluble microneedles with a microneedle length of 400 μm.
[0057] Application Examples 2-3, Comparative Application Examples 1-8
[0058] The preparation method is different from that of Application Example 1, except that the whitening composition described in Example 1 is replaced by the whitening compositions described in Examples 2-3 and Comparative Examples 1-8 (Application Examples 2-3 and Comparative Application Examples 1-8 correspond to Examples 2-3 and Comparative Examples 1-8, respectively), and the remaining steps are the same.
[0059] Comparative Application Example 9
[0060] The preparation method is compared with Application Example 1, except that low-substituted hydroxypropyl cellulose is replaced by hydroxypropyl cellulose, and the remaining steps are the same.
[0061] Comparative Application Example 10
[0062] The preparation method is compared with Application Example 1, except that mannitol is replaced by sorbitol, and the remaining steps are the same.
[0063] Comparative Application Example 11
[0064] The preparation method is the same as that of Application Example 1, except that the microneedle preparation solution does not contain low-substituted hydroxypropyl cellulose, and the remaining steps are the same.
[0065] Comparative Application Example 12
[0066] The preparation method is the same as that of Application Example 1, except that the microneedle preparation solution does not contain mannitol, and the remaining steps are the same.
[0067] Table 2 Microneedle components described in Application Examples 1-3 and Comparative Application Examples 1-12
[0068]
[0069] Application Examples 1-3 and Comparative Application Examples 1-12 Performance Verification
[0070] (1) Skin irritation test:
[0071] Safety evaluation of human trial test: The human skin trial test is used for testing. The specific test methods refer to the "Technical Specifications for Safety of Cosmetics" (2015 edition), see the table below for details.
[0072] Grading Skin reactions 0 No response 1 Faint erythema 2 Erythema, infiltration, and papules 3 Erythema, infiltration, edema, papules, blisters 4 Erythema, edema, bullae
[0073] A total of 450 subjects, aged 21-51 years with an average age of 29 years, were randomly divided into 15 groups. The microneedle sample 1 prepared in the application example and the comparative application example was applied to the outer side of the forearm for 0.5 hours, once in the morning and once in the evening. The subjects were followed up for four weeks (28) days. The experimental results are recorded in Table 3.
[0074] Table 3 Test results
[0075] Group Level 0 Level 1 Level 2 Level 3 Level 4 Application Example 1 30 0 0 0 0 Application Example 2 30 0 0 0 0 Application Example 3 30 0 0 0 0 Comparative Application Example 1 30 0 0 0 0 Comparative Application Example 2 30 0 0 0 0 Comparative Application Example 3 30 0 0 0 0 Comparative Application Example 4 30 0 0 0 0 Comparative Application Example 5 30 0 0 0 0 Comparative Application Example 6 30 0 0 0 0 Comparative Application Example 7 30 0 0 0 0 Comparative Application Example 8 30 0 0 0 0 Comparative Application Example 9 30 0 0 0 0 Comparative Application Example 10 30 0 0 0 0 Comparative Application Example 11 30 0 0 0 0 Comparative Application Example 12 30 0 0 0 0
[0076] The data in Table 3 demonstrate that the microneedles prepared in Application Examples 1-3 of the present invention exhibit good biosafety and are non-irritating to the skin. This also demonstrates that the whitening compositions of Examples 1-3 contained within the microneedles exhibit good biosafety. Both Examples 1-3 and Application Examples 1-3 utilize raw materials with excellent biocompatibility, which is key to ensuring the biosafety of the prepared whitening compositions and microneedles.
[0077] (2) Microneedle mechanical strength test
[0078] A Shimadzu AG-X series universal materials testing machine was used, equipped with a 10N load cell and a non-contact laser displacement meter. The testing platform featured a horizontal base and a P / 6 flat-tip stainless steel cylindrical probe (Ø1.5mm diameter, surface roughness Ra <0.1μm). A microscopic vision system (500x magnification) assisted positioning, ensuring that the probe's initial contact point was within a 0.5μm error range of the microneedle tip.
[0079] Mechanical loading mode settings: loading rate: 0.1 mm / s (constant displacement control), initial preload: 0.01 N (contact confirmation threshold), termination condition: reaching 400 μm displacement (corresponding to the full length of the microneedle), data acquisition frequency: 2000 Hz.
[0080] The entire mechanical response from the moment the probe contacts the needle tip until it reaches the predetermined end height was recorded in detail (measured at 37°C, with three parallel measurements) to evaluate the mechanical properties, deformation characteristics, and product stability of the microneedle.
[0081] Table 4 Strength of microneedles at 37°C (N)
[0082] Group average value SD value Application Example 1 16.49 0.16 Application Example 2 16.66 0.12 Application Example 3 16.42 0.13 Comparative Application Example 1 16.48 0.12 Comparative Application Example 2 16.59 0.14 Comparative Application Example 3 16.64 0.11 Comparative Application Example 4 16.48 0.13 Comparative Application Example 5 16.47 0.17 Comparative Application Example 6 16.51 0.27 Comparative Application Example 7 16.64 0.11 Comparative Application Example 8 16.58 0.19 Comparative Application Example 9 12.45 0.24 Comparative Application Example 10 16.41 0.10 Comparative Application Example 11 9.71 0.15 Comparative Application Example 12 16.63 0.17
[0083] The data in Table 4 show that: 1) The microneedle strengths of Application Examples 1-3 ranged from 16.29 to 16.75 N, indicating that at 37°C, the microneedles prepared in Application Examples 1-3 possessed suitable strength to penetrate human skin. 2) Compared with Comparative Application Examples 1-8, the microneedle strength performance of Application Example 1 was consistent, indicating that the microneedle strength was primarily influenced by the microneedle excipients (sodium hyaluronate, low-substituted hydroxypropyl cellulose, and mannitol). 3) Compared with Comparative Application Examples 9 and 11, Application Example 1 showed that low-substituted hydroxypropyl cellulose significantly enhanced the strength of sodium hyaluronate-based microneedles compared to hydroxypropyl cellulose. This is because low-substituted hydroxypropyl cellulose has more hydroxyl groups than hydroxypropyl cellulose. Low-substituted hydroxypropyl cellulose can better form hydrogen bonds with sodium hyaluronate through the hydroxyl groups, forming a cross-linked three-dimensional network and significantly improving the strength of microneedles with sodium hyaluronate as the framework. 4) Comparison of Application Example 1 with Comparative Application Examples 10 and 12 shows that mannitol has little effect on the mechanical strength of the microneedles.
[0084] (3) Microneedle solubility test
[0085] A constant temperature of 37°C water bath was used to simulate the dissolution of microneedles in the human body. 50 ml of deionized water was placed in a 200 ml beaker and the water bath was heated to 37°C. The microneedle patch was immersed in the deionized water in the beaker and the time (s) taken for the microneedle body to completely dissolve was recorded.
[0086] 1 mL (i.e., sample) was sampled at 5s, 10s, 15s, 20s, 25s, and 30s for HPLC detection of tetrahydromagnanol. The sampling time corresponding to the first peak was used to evaluate the release rate of the microneedle. Sample processing (removal of water-soluble substances such as nonapeptide-1 to prevent clogging of the chromatographic column) was performed by adding 0.5 mL of sample to 0.5 mL of DMSO, centrifuging at 10,000 g, aspirating 0.5 mL of supernatant, adding 0.5 mL of methanol, refrigerating at 4°C for 15 minutes, centrifuging at 10,000 g, and taking the supernatant to obtain the sample to be tested. Among them, the HPLC spectra of the first peak of tetrahydromagnanol in Application Example 1-3 are shown in FIG. Figure 1 .
[0087] HPLC detection conditions: HPLC (Agilent 1200, equipped with diode array detector (DAD); chromatographic column TC-C18 (4.6*250 mm, 5 μm, 400 bar); mobile phase: methanol: 0.02 mol / L potassium dihydrogen phosphate solution (3:7); flow rate 1 mL / min, injection volume 10 μL, detection wavelength 210-260 nm.
[0088] Table 5 Microneedle body dissolution time and first peak time
[0089] Group Complete dissolution time 5s sample 10s sample 15s sample 20s sample 25s sample 30s sample Application Example 1 35s Peak Application Example 2 32s Peak Application Example 3 33s Peak Comparative Application Example 1 36s Peak Comparative Application Example 2 35s Peak Comparative Application Example 3 34s Peak Comparative Application Example 4 36s Peak Comparative Application Example 5 32s Peak Comparative Application Example 6 33s Peak Comparative Application Example 7 36s Peak Comparative Application Example 8 35s Peak Comparative Application Example 9 84s / / Peak Comparative Application Example 10 56s / Peak Comparative Application Example 11 220s / / / Peak Comparative Application Example 12 53s / Peak
[0090] Note: In the table, “ / ” means that tetrahydromagnanol was not detected in the corresponding sample, and blank means that the corresponding sample was not detected.
[0091] According to the data in Table 5, the following can be seen: 1) The time for complete dissolution of the microneedle bodies in Application Examples 1-3 is between 32-36 seconds, and the 5-second sample contains tetrahydromagnanol detected by high-performance liquid chromatography (i.e., tetrahydromagnanol first peaks in the 5-second sample). This shows that the microneedle bodies prepared in Application Examples 1-3 can be effectively and quickly released (5 seconds) and completely released in a short time, with a flash release effect; the time for complete dissolution of the microneedle bodies in Comparative Application Example 1-8 is similar to that in Application Example 1-3, which is because the skeleton composition of the two is the same. 2) However, when the auxiliary material skeleton component of the microneedle body is replaced by hydroxypropyl cellulose from low-substituted hydroxypropyl cellulose in Application Example 1 compared with Comparative Application Example 9, the complete dissolution time of the microneedle body is extended from 35 seconds to 84 seconds, indicating that the disintegration-promoting release effect of low-substituted hydroxypropyl cellulose is more significant; compared with Comparative Application Example 11, Application Example 1 shows that low-substituted hydroxypropyl cellulose can promote solid-state flash release of microneedles. 3) Comparing Application Example 1 with Comparative Application Examples 10 and 12, it is clear that mannitol also promotes rapid release of microneedles, whereas its analog sorbitol does not. This is related to mannitol's ability to promote penetration and increase osmotic pressure. 4) In summary, the microneedle skeleton components of sodium hyaluronate, low-substituted hydroxypropyl cellulose, and mannitol synergistically promote rapid release of microneedles, achieving a significant flash-release effect.
[0092] (4) Whitening performance test
[0093] 150 volunteers aged 30-50 were recruited as testers and randomly divided into 15 groups with 10 people in each group. Each group used the microneedles prepared in Application Examples 1-3 and Comparative Application Examples 1-12 respectively. The subjects took the microneedles and applied them to the left outer corner of the eye once a day for 5 minutes each time for 4 weeks (28 days). A skin red-melanin tester (model HexameterMX18) was used to evaluate the changes in the melanin content of the subjects' skin before and after using the microneedles. The average melanin content before use was recorded as N1, and the average melanin content after 4 weeks of use was recorded as N2. Melanin inhibition rate T = (N 1- N2) / N1×100%.
[0094] Table 6 Melanin inhibition rate results
[0095] Group Melanin inhibition rate T (%) Application Example 1 38.46 Application Example 2 34.11 Application Example 3 35.73 Comparative Application Example 1 9.76 Comparative Application Example 2 16.31 Comparative Application Example 3 25.21 Comparative Application Example 4 16.88 Comparative Application Example 5 27.35 Comparative Application Example 6 14.12 Comparative Application Example 7 18.46 Comparative Application Example 8 16.74 Comparative Application Example 9 23.45 Comparative Application Example 10 29.33 Comparative Application Example 11 18.65 Comparative Application Example 12 30.43
[0096] According to the melanin inhibition results in Table 6, the following can be seen: 1) The microneedles described in Application Examples 1-3 can significantly improve the inhibition rate of melanin compared to the microneedles described in Comparative Application Examples 1-12, which shows that the whitening efficacy of the microneedles prepared in Application Examples 1-3 of the present invention is significant. Comparative Application Examples 1-12 show that different whitening components or combinations commonly used in the field, such as 4-butylresorcinol, tranexamic acid, niacinamide, resveratrol, and nonapeptide-1, do not achieve the whitening effect of Application Examples 1-3. 2) Compared with Application Example 1 and Comparative Application Example 3, in the absence of the solubilizer coconut oil glucoside, the whitening effect of Comparative Application Example 3 is significantly reduced. This is because coconut oil glucoside can effectively increase the solubility of tetrahydromagnanol in water, which is beneficial to the dissolution of tetrahydromagnanol after release. Secondly, the solubilizer can also effectively promote the transport of tetrahydromagnanol released by the microneedles into the cells, thereby improving the whitening effect. 3) Comparing Application Example 1 with Comparative Application Example 9 shows that hydroxypropyl cellulose has a slower release rate than low-substituted hydroxypropyl cellulose. After the microneedles penetrate the skin, the whitening components in the needles cannot be fully released within 5 minutes, resulting in a reduced whitening effect in Comparative Application Example 9. This also shows that the microneedles in Application Examples 1-3 meet the market demand for rapid release and improved ease of use, effectively reducing the time required for consumers to whiten their skin. 4) Comparing Application Example 1 with Comparative Application Examples 10 and 12, it can be seen that mannitol can regulate the release rate of microneedles and significantly enhance whitening efficacy. This is related to mannitol's ability to increase osmotic pressure and promote penetration.
[0097] The preferred embodiments of the present invention disclosed above are intended only to help illustrate the present invention. These preferred embodiments do not exhaustively describe all details, nor do they limit the present invention to the specific embodiments described. Obviously, many modifications and variations are possible based on the content of this specification. These embodiments are selected and described in detail in this specification to better explain the principles and practical applications of the present invention, thereby enabling those skilled in the art to better understand and utilize the present invention. The present invention is limited only by the claims and their full scope and equivalents.
Claims
1. A whitening composition, characterized in that The invention comprises the following components by weight: 0.2-0.4 parts of tetrahydromagnanol, 1-2 parts of nonapeptide-1, and 0.1-3 parts of a solubilizer; the solubilizer is selected from at least one of Tween, phospholipid, PEG-400, and coconut glucoside.
2. The whitening composition according to claim 1, characterized in that The invention also includes the following components: at least one of 5-20 parts of a moisturizing agent, 0.1-5 parts of a thickener, 0.1-4 parts of an antioxidant, 0.01-2 parts of a preservative, and 0.01-1 part of a flavor.
3. The whitening composition according to claim 2, characterized in that The thickener is selected from at least one of carboxyethyl cellulose, carbomer, polyethylene glycol, coconut diethanolamide, xanthan gum, and carrageenan.
4. The whitening composition according to claim 2, characterized in that The antioxidant is selected from at least one of gallic acid, vitamin E, vitamin C, and glutathione.
5. The whitening composition according to claim 2, characterized in that The preservative is selected from at least one of methylparaben, ethylparaben, potassium sorbate, sodium benzoate, sodium dehydroacetate, or a composite solution of phenoxyethanol and ethylhexylglycerin.
6. The method for preparing the whitening composition according to any one of claims 1 to 5, characterized in that: Weigh each component according to the amount and mix them evenly.
7. Use of the whitening composition according to any one of claims 1 to 5 in the preparation of solid-state flash-release soluble microneedles.
8. The use according to claim 7, characterized in that In addition to the whitening composition, the solid-state flash-release microneedle also contains a microneedle skeleton component, and the microneedle skeleton component is sodium hyaluronate, low-substituted hydroxypropyl cellulose and mannitol.
9. The use according to claim 8, characterized in that: The weight ratio of the sodium hyaluronate, low-substituted hydroxypropyl cellulose and mannitol is 100: (2-3): (0.5-1).
Citation Information
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