Topical Compositions and Their Uses

Abstract

This application discloses a topical composition and its use, comprising polylysine, dihydrogen phosphate, and anionic surfactant, wherein the polylysine, dihydrogen phosphate, and anionic surfactant are present in two or more different phases. The topical composition of this application is stable and does not exhibit stratification or flocculation during preparation or storage; the topical composition of this application can be deposited on the scalp; and the topical composition has good antibacterial effects.

Description

Technical Field

[0001] This application relates to the field of hair care products technology, and more particularly to a topical composition and its use. Background Technology

[0002] Dandruff is a common scalp problem, primarily caused by the overgrowth of Malassezia. Currently, anti-dandruff shampoos effectively alleviate dandruff by depositing antibacterial ingredients on the scalp to inhibit Malassezia growth. However, commonly used antibacterial ingredients, such as zinc pyrithione (ZPT) and octopirox (OCT), pose potential risks to human health and the environment, and are therefore often restricted in some countries or regions.

[0003] Polylysine is a naturally derived macromolecule with good biocompatibility. Studies have shown that polylysine can effectively inhibit the growth of microorganisms such as Malassezia. Therefore, it has the potential to become a new generation of anti-dandruff ingredients for use in shampoos. Summary of the Invention

[0004] Although polylysine can inhibit Malassezia, its high water solubility makes it difficult to deposit on the skin during washing to exert a long-lasting antibacterial effect. To enable effective deposition of polylysine on the skin, the inventors of this application attempted to combine it with other substances; however, instability such as flocculation occurred. To achieve effective deposition of polylysine and a stable formulation, this application unexpectedly discovered that combining polylysine, dihydrogen phosphate, and anionic surfactant, wherein the polylysine, dihydrogen phosphate, and anionic surfactant are not present in the same phase, can solve the above problems, thus completing this application.

[0005] The specific technical solution of this application is as follows:

[0006] 1. A topical composition comprising polylysine, dihydrogen phosphate, and anionic surfactant, wherein the polylysine, dihydrogen phosphate, and anionic surfactant are not present in the same phase.

[0007] 2. The composition according to claim 1, wherein the dihydrogen phosphate salt comprises sodium dihydrogen phosphate and / or potassium dihydrogen phosphate.

[0008] 3. The composition according to claim 1 or 2, wherein the anionic surfactant comprises a surfactant containing an amino acid group, a sulfonic acid group or a carboxylic acid group, preferably selected from one or more of sodium lauroyl sarcosinate, disodium cocoyl glutamate, sodium cocoyl aminopropionate, sodium methyl cocoyl taurate, sodium C14-16 olefin sulfonate and sodium laureth-8 carboxylate.

[0009] 4. The composition according to any one of items 1-3, wherein the concentration of the polylysine in the phase in which it is contained is 0.1-10 wt%.

[0010] 5. The composition according to any one of items 1-4, wherein the concentration of the dihydrogen phosphate in its phase is 0.1-5 wt%.

[0011] 6. The composition according to any one of items 1-5, wherein the concentration of the active ingredient in the surfactant in its phase is 1-30 wt%.

[0012] 7. Use of the composition of any one of items 1-6 in dandruff removal.

[0013] 8. Use of the composition of any one of items 1-6 in inhibiting the growth of Malassezia.

[0014] 9. Use of the composition of any one of items 1-6 in promoting the deposition of polylysine onto the skin, preferably the scalp.

[0015] The effects of the invention

[0016] The topical composition described in this application is stable and will not exhibit unstable phenomena such as stratification or flocculation during preparation or storage.

[0017] Furthermore, the topical composition of this application can deposit polylysine on the skin, effectively inhibiting the growth of microorganisms such as Malassezia. Attached Figure Description

[0018] Figure 1 This is a schematic diagram of the infrared spectrum of the sediment from Example 1.

[0019] Figure 2 This is a schematic diagram of the infrared spectrum of the sediment from Example 2.

[0020] Figure 3 This is a schematic diagram of the infrared spectrum of the sediment from Example 3. Detailed Implementation

[0021] The embodiments described below provide a detailed description of this application. While specific embodiments of this application are shown, it should be understood that this application can be implemented in various forms and should not be limited to the embodiments set forth herein. Rather, these embodiments are provided to enable a more thorough understanding of this application and to fully convey the scope of this application to those skilled in the art.

[0022] It should be noted that certain terms are used in the specification and claims to refer to specific components. Those skilled in the art will understand that different terms may be used to refer to the same component. This specification and claims do not distinguish components based on differences in terminology, but rather on differences in function. The terms "comprising" or "including" used throughout the specification and claims are open-ended and should be interpreted as "comprising but not limited to." The following descriptions in the specification are preferred embodiments for carrying out this application; however, these descriptions are for the purpose of understanding the general principles of the specification and are not intended to limit the scope of this application. The scope of protection of this application shall be determined by the appended claims.

[0023] This application provides a topical composition comprising polylysine, dihydrogen phosphate, and anionic surfactant, wherein the polylysine, dihydrogen phosphate, and anionic surfactant are present in two or more different phases.

[0024] The statement that polylysine, dihydrogen phosphate, and anionic surfactant do not exist in the same phase means that polylysine and dihydrogen phosphate can be placed in the same phase and anionic surfactant in another phase; or polylysine and anionic surfactant can be placed in the same phase and dihydrogen phosphate in another phase; or dihydrogen phosphate and anionic surfactant can be placed in the same phase and polylysine in another phase; or polylysine, dihydrogen phosphate, and anionic surfactant can be placed in different phases.

[0025] In this application, the solvent used in each phase can be the same or different, as long as the above-mentioned substances are dissolved in two or more different phases. For example, the solvent can be water.

[0026] In some embodiments, the dihydrogen phosphate salt includes sodium dihydrogen phosphate and / or potassium dihydrogen phosphate.

[0027] In some embodiments, the anionic surfactant includes a surfactant containing an amino acid group, a sulfonic acid group, or a carboxylic acid group, preferably selected from one or more of sodium lauroyl sarcosinate, disodium cocoyl glutamate, sodium cocoyl aminopropionate, sodium methyl cocoyl taurate, sodium C14-16 olefin sulfonate, and sodium laureth-8 carboxylate.

[0028] This application obtains a stable composition by placing the above three substances in two or more different phases, and the composition can be deposited on the scalp and has a good antibacterial effect.

[0029] In some embodiments, the concentration of polylysine in the phase in which it is present is 0.1-10 wt%.

[0030] For example, the concentration of polylysine in its phase can be 0.1wt%, 0.2wt%, 0.3wt%, 0.4wt%, 0.5wt%, 0.6wt%, 0.7wt%, 0.8wt%, 0.9wt%, 1wt%, 2wt%, 3wt%, 4wt%, 5wt%, 6wt%, 7wt%, 8wt%, 9wt%, 10wt%, etc.

[0031] In some embodiments, the concentration of the dihydrogen phosphate in its phase is 0.1-5 wt%.

[0032] For example, the concentration of the dihydrogen phosphate in its phase can be 0.1wt%, 0.2wt%, 0.3wt%, 0.4wt%, 0.5wt%, 0.6wt%, 0.7wt%, 0.8wt%, 0.9wt%, 1wt%, 2wt%, 3wt%, 4wt%, 5wt%, etc.

[0033] In some embodiments, the concentration of the active ingredient in the surfactant in its phase is 1-30 wt%.

[0034] For example, the concentration of the active ingredient in the surfactant in its phase can be 1 wt%, 2 wt%, 3 wt%, 4 wt%, 5 wt%, 6 wt%, 7 wt%, 8 wt%, 9 wt%, 10 wt%, 11 wt%, 12 wt%, 13 wt%, 14 wt%, 15 wt%, 16 wt%, 17 wt%, 18 wt%, 19 wt%, 20 wt%, 21 wt%, 22 wt%, 23 wt%, 24 wt%, 25 wt%, 26 wt%, 27 wt%, 28 wt%, 29 wt%, 30 wt%, etc.

[0035] In some embodiments, the polylysine has a weight-average molecular weight of 3000-5000 Da.

[0036] For example, the weight-average molecular weight of the polylysine can be 3000 Da, 3100 Da, 3200 Da, 3300 Da, 3400 Da, 3500 Da, 3600 Da, 3700 Da, 3800 Da, 3900 Da, 4000 Da, 4100 Da, 4200 Da, 4300 Da, 4400 Da, 4400 Da, 4500 Da, 4600 Da, 4700 Da, 4800 Da, 4900 Da, 5000 Da, etc.

[0037] In some embodiments, the composition may also contain excipients. In this application, the excipients are those conventionally used in the art, and this application makes no limitation thereto.

[0038] In some embodiments, the composition may be used in dosage forms including, but not limited to, water, lotion, cream, spray, gel, etc.

[0039] In some embodiments, the topical composition comprises polylysine, a dihydrogen phosphate, and an anionic surfactant, wherein the polylysine, the dihydrogen phosphate, and the anionic surfactant are present in two or more different phases. In some embodiments, the dihydrogen phosphate comprises sodium dihydrogen phosphate and / or potassium dihydrogen phosphate. In some embodiments, the anionic surfactant comprises a surfactant containing an amino acid group, a sulfonic acid group, or a carboxylic acid group, preferably selected from one or more of sodium lauroyl sarcosinate, disodium cocoyl glutamate, sodium cocoaminopropionate, sodium methyl cocoyl taurate, sodium C14-16 olefin sulfonate, and sodium laureth-8 carboxylate. In some embodiments, the concentration of polylysine in its phase is 0.1-10 wt%. In some embodiments, the concentration of the dihydrogen phosphate in its phase is 0.1-5 wt%. In some embodiments, the concentration of the active ingredient in the surfactant in its phase is 1-30 wt%.

[0040] This application provides the use of the above-described composition in dandruff removal.

[0041] This application also provides the use of the above-described composition in inhibiting the growth of Malassezia.

[0042] This application also provides the use of the above-described composition in promoting the deposition of polylysine onto the skin, preferably the scalp.

[0043] Example

[0044] This application provides a general and / or specific description of the materials and experimental methods used in the experiments. In the following examples, unless otherwise specified, % represents wt%, i.e., weight percentage. Reagents or instruments used, unless otherwise specified, are all commercially available conventional reagent products. The experimental materials used in the examples, comparative examples, and experimental cases are shown in Table 1, and the experimental equipment is shown in Table 2.

[0045] Table 1 shows the experimental materials used in the examples, comparative examples, and experimental cases.

[0046]

[0047] Table 2. Experimental equipment used in the examples, comparative examples, and experimental cases.

[0048]

[0049] Example

[0050] Preparation of the topical compositions in Examples 1-7:

[0051] (1) Weigh 3g of ε-PL and the remainder of deionized water to form a working solution of phase A with a mass fraction of 3%.

[0052] (2) Weigh out 1g of NaH2PO4, 50g of different types of surfactant solutions, and the remainder of deionized water to form a B-phase working solution with a NaH2PO4 mass fraction of 1% and a surfactant active ingredient mass fraction of 15%, as shown in Table 3.

[0053] Preparation of the topical compositions in Examples 8-10:

[0054] (1) Weigh 3g of ε-PL and the remainder of deionized water to form a working solution of phase A with a mass fraction of 3%.

[0055] (2) Weigh out 1g of salt NaH2PO4, 16.67g, 33.34g, and 66.67g of CMT surfactant solution, respectively, with the remainder being deionized water, to form phase B working solutions with a NaH2PO4 mass fraction of 1% and CMT surfactant active ingredient mass fractions of 5%, 10%, and 20%, as shown in Table 3.

[0056] Preparation of topical compositions in Examples 11-13:

[0057] (1) Weigh 3g of ε-PL and the remainder of deionized water to form a working solution of phase A with a mass fraction of 3%.

[0058] (2) Weigh out 0.5g, 2g and 3g of salt NaH2PO4, 50g of CMT surfactant solution, and the remainder is deionized water to form phase B working solutions with NaH2PO4 mass fractions of 0.5%, 2% and 3% and CMT surfactant active ingredient mass fraction of 15%, as shown in Table 3.

[0059] Preparation of the topical compositions in Examples 14-16:

[0060] (1) Weigh 1g, 6g and 8g of ε-PL respectively, and the remainder is deionized water to form working solutions of phase A with mass fractions of 1%, 6% and 8%.

[0061] (2) Weigh out 1g of NaH2PO4 and 50g of CMT surfactant solution, with the remainder being deionized water, to form a B-phase working solution with a NaH2PO4 mass fraction of 1% and a CMT surfactant active ingredient mass fraction of 15%, as shown in Table 3.

[0062] Preparation of the topical composition in Example 17

[0063] (1) Weigh 3g of ε-PL, 50g of CMT surfactant solution, and the remainder of deionized water to form a working solution of phase A with a mass fraction of 3% ε-PL and a mass fraction of 15% CMT surfactant active ingredient.

[0064] (2) Weigh 1g of NaH2PO4 and the remainder is deionized water to form a working solution of phase B with a NaH2PO4 mass fraction of 1%, as shown in Table 3.

[0065] Preparation of the topical composition in Example 18:

[0066] (1) Weigh 3g of ε-PL, 1g of NaH2PO4, and the remainder of deionized water to form a working solution of phase A with a mass fraction of 3% ε-PL and 1% NaH2PO4.

[0067] (2) Weigh 50g of CMT surfactant solution and the remainder is deionized water to form a B-phase working solution with a CMT surfactant active ingredient mass fraction of 15%, as shown in Table 3.

[0068] Preparation of the topical composition in Example 19:

[0069] (1) Weigh 3g of ε-PL and the remainder is deionized water to form a working solution of phase A with a mass fraction of 3% ε-PL.

[0070] (2) Weigh 1g of NaH2PO4 and the remainder is deionized water to form a working solution of phase B with a NaH2PO4 mass fraction of 1%.

[0071] (3) Weigh 50g of CMT surfactant solution and the remainder is deionized water to form a C-phase working solution with a CMT surfactant active ingredient mass fraction of 15%, as shown in Table 3.

[0072] Preparation of topical compositions in Comparative Examples 1-6

[0073] Weigh out 3g of ε-PL, 1g of NaH2PO4 salt, and 50g of different types of surfactant solutions, with the remainder being deionized water, to form phase A working solution. The mass fraction of ε-PL is 3%, the mass fraction of NaH2PO4 is 1%, and the mass fraction of different surfactants is 15%, as shown in Table 3.

[0074] Preparation of the topical compositions of Comparative Examples 7-14:

[0075] (1) Weigh 3g of ε-PL and the remainder is deionized water to form a working solution of phase A with a mass fraction of 3% ε-PL;

[0076] (2) Weigh 1g of different types of salt and 50g of different types of surfactant solutions respectively, with the remainder being deionized water, to form a B-phase working solution with a salt mass fraction of 1% and a surfactant active ingredient mass fraction of 15%, as shown in Table 3.

[0077] Table 3 Concentrations of the compositions used in the examples and comparative cases

[0078]

[0079]

[0080] Experimental Example 1: Deposition Test

[0081] S1) Take a piece of imitation leather with an area of ​​6*6cm, clean it with deionized water, spray it with anhydrous ethanol for sterilization, and then place it in a ventilated place for 24 hours to air dry naturally.

[0082] S2) According to the formula design table 3, take 3ml of phase A working solution and 3ml of phase B working solution respectively and place them on the imitation leather;

[0083] S3) Using disposable powder-free silicone gloves, rub the imitation leather with your index finger in a clockwise direction 30 times to ensure the working fluid is fully in contact with the surface.

[0084] S4) Clean the artificial leather with deionized water at a flow rate of 1.5 m / s for 20 seconds.

[0085] S5) Repeat S2–S4 for 15 cycles per group, then place the synthetic leather at room temperature for 2 hours.

[0086] S6) Gently scrape the surface of the imitation leather with a silicone scraper to collect the deposits for testing. The results are shown in Table 4.

[0087] Table 4 shows the deposition effects of the examples and comparative examples.

[0088]

[0089]

[0090] As can be seen from the table above, the compositions of Comparative Examples 1-6 were unstable and flocculated before testing, and no sediment was collected in Comparative Examples 7-14; yellow sediment was collected in Examples 1-19, indicating that the topical compositions prepared in the examples are stable and have a sedimentation effect.

[0091] Experiment Example 2: Confirmation of Sediment Structure

[0092] Taking Examples 1-3 as examples, the chemical structure of the yellow sediment was confirmed, and the specific operation method is as follows:

[0093] Infrared absorption spectroscopy was performed using a pellet method. Specifically, a certain amount of the deposit was taken, ground in a mortar for 1 minute, and then placed on a Fourier transform infrared spectrometer in ATR mode for detection. The scanning range was 4000–4000 cm⁻¹. -1 Their spectra are as follows: Figures 1 to 3 As shown.

[0094] from Figures 1 to 3 The infrared spectrum of the surface, in the sediments produced in Examples 1-3, showed wavenumbers δ = 1550-1660 cm⁻¹. -1 and 3270-3285cm -1 All samples contained vibrational absorption peaks of polylysine at the -NC=O and -NH groups. This indicates that the topical compositions prepared in Examples 1-3 contained polylysine in the deposits after testing.

[0095] Experiment Example 3: Verification of the antibacterial effect of sediments

[0096] Examples 1-3 are used to verify the antibacterial effect on yellow sediments.

[0097] The antibacterial properties of the sample sediments from the examples were tested using a suspension quantitative method. The specific method is as follows:

[0098] 1) Weigh 2.5g of sediment and add water to 5mL, shake to obtain a suspension; place in a sterile test tube and incubate at 20℃ for 5 minutes;

[0099] 2) Take 0.1 mL of Malassezia furfur test bacterial solution (ATCC44344) (bacterial solution concentration 10). 5 -10 6 Add (cfu / mL) to a test tube containing 5.0 mL of sample, mix quickly, and start timing immediately. Select a reaction time of 2 hours;

[0100] 3) After the set time has elapsed, take 0.5 mL of the mixture of test bacteria and sample and add it to 4.5 mL of sterile 0.03 mol / L phosphate buffer (PBS), and mix well.

[0101] 4) After standing for 10 minutes, take 1 mL of sample solution and place it in a sterile Petri dish. Pour in sterile Malassezia furfur culture medium and mix thoroughly. After the agar solidifies, turn the Petri dish over and incubate in an incubator for 3-5 days. Then, count the viable colonies.

[0102] 5) Use sterile PBS instead of the test sample, and follow the above steps as a control sample;

[0103] 6) Inhibition rate (%) = (I-II) / I x100, where I is the colony count of the control sample and II is the colony count of the test sample. Specific test results are shown in Table 5.

[0104] Table 5 Antibacterial effect of sediments

[0105]

[0106] According to the evaluation criteria of WS / T 650—2019 "Evaluation Method for Antibacterial and Bacteriostatic Effects", a bacteriostatic rate of ≥50% to 90% is considered to have a bacteriostatic effect; a bacteriostatic rate of ≥90% is considered to have a strong bacteriostatic effect. The sediments showed an inhibition rate of more than 90% against Malassezia furfur, therefore the sediments all have a strong bacteriostatic effect.

[0107] The above description is merely a preferred embodiment of this application and is not intended to limit the application in any other way. Any person skilled in the art may make changes or modifications to the disclosed technical content to create equivalent embodiments. However, any simple modifications, equivalent changes, and modifications made to the above embodiments based on the technical essence of this application without departing from the scope of the technical solution of this application shall still fall within the protection scope of this application.

Claims

1. A topical composition comprising polylysine, dihydrogen phosphate, and an anionic surfactant, wherein, The polylysine, dihydrogen phosphate, and anionic surfactant do not exist in the same phase.

2. The composition according to claim 1, wherein, The dihydrogen phosphate includes sodium dihydrogen phosphate and / or potassium dihydrogen phosphate.

3. The composition according to claim 1 or 2, wherein, The anionic surfactants include surfactants containing amino acid groups, sulfonic acid groups, or carboxylic acid groups.

4. The composition according to claim 3, wherein, The anionic surfactant is selected from one or more of sodium lauroyl sarcosinate, disodium cocoyl glutamate, sodium cocoyl aminopropionate, sodium methyl cocoyl taurate, sodium C14-16 olefin sulfonate, and sodium lauryl ether-8 carboxylate.

5. The composition according to claim 1 or 2, wherein, The concentration of polylysine in its phase is 0.1-10 wt%.

6. The composition according to claim 1 or 2, wherein, The concentration of the dihydrogen phosphate in its phase is 0.1-5 wt%.

7. The composition according to claim 1 or 2, wherein, The concentration of the active ingredient in the surfactant in its phase is 1-30 wt%.

8. Use of the composition according to any one of claims 1-7 in the preparation of a dandruff-removing product.

9. Use of the composition of any one of claims 1-7 in the preparation of a product that inhibits the growth of Malassezia.

10. Use of the composition of any one of claims 1-7 in the preparation of a product that promotes the deposition of polylysine onto the skin.

11. The use according to claim 10, wherein, The skin in question is the scalp.

Images