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CN-122005348-A - Penetration-promoting skin nano-composite globule peptide, preparation method thereof and application thereof in preparation of scalp oil control, anti-drop and anti-aging products

CN122005348ACN 122005348 ACN122005348 ACN 122005348ACN-122005348-A

Abstract

The application relates to the technical field of transdermal delivery and cosmetics, in particular to a penetration-promoting skin nano-composite globule peptide, a preparation method thereof and application thereof in preparing scalp oil control, anti-drop and anti-aging products. The preparation method comprises the steps of adding compound peptide into a first organic solvent to be heated and dissolved at a first temperature (35-45 ℃) to obtain a first solution, adding tolcoronene into a second organic solvent to be heated and dissolved at a second temperature (40-60 ℃) to obtain a second solution, adding poloxamer into water to be heated and dissolved at a third temperature (40-60 ℃) to obtain a third solution, mixing the second solution and the third solution to obtain a fourth solution, and adding the first solution into the fourth solution at a first rate (1-3 mL/min) to be dispersed at a fourth temperature (40-50 ℃). The penetration-promoting skin nano-composite globulin has high stability, excellent transdermal absorption performance and good effects of controlling oil, preventing alopecia and resisting aging on scalp.

Inventors

  • Zheng Rujing
  • JIANG JINJIE
  • GUO WENHUA
  • LI DANDAN
  • Pan Youyou

Assignees

  • 浙江浩迈科技有限公司

Dates

Publication Date
20260512
Application Date
20260414

Claims (10)

  1. 1. The preparation method of the penetration-promoting skin nano-composite globulin is characterized by comprising the following steps of: Adding a compound peptide into a first organic solvent, mixing, and carrying out ultrasonic dissolution at a first temperature to obtain a first solution, wherein the composition of the compound peptide comprises components (i) - (iii) including (i) palmitoyl tripeptide-1 or a derivative thereof, (ii) palmitoyl tripeptide-5 or a derivative thereof, and (iii) palmitoyl tetrapeptide-7 or a derivative thereof, wherein the first organic solvent is aliphatic polyol, and the first temperature is 35-45 ℃; Adding the tolocham into a second organic solvent, mixing, and heating and dissolving at a second temperature to obtain a second solution, wherein the tolocham is vitamin E polyethylene glycol succinate, the second organic solvent is aliphatic polyol, and the second temperature is 40-60 ℃; Adding poloxamer into the first water, mixing, and heating and dissolving at a third temperature to obtain a third solution, wherein the third temperature is 40-60 ℃; mixing the second solution and the third solution to prepare a fourth solution; and adding the first solution into a fourth solution at a first rate, stirring and dispersing at a fourth temperature to obtain the penetration-promoting skin nano composite globule peptide, wherein the first rate is 1-3 mL/min, and the fourth temperature is 40-50 ℃.
  2. 2. The penetration enhancing skin nanocomposite bulb peptide of claim 1, wherein the first and second organic solvents each independently comprise one or more of propylene glycol, 1, 3-propanediol, 1, 2-butanediol, 1, 3-butanediol, 1, 4-butanediol, 2, 3-butanediol, 1, 2-pentanediol, 1, 5-pentanediol, glycerol, dipropylene glycol, 1, 2-hexanediol, 1, 6-hexanediol, methylpropanediol (2-methyl-1, 3-propanediol), trimethylolpropane, and pentaerythritol.
  3. 3. The penetration enhancing skin nanocomposite globulin of claim 1, wherein the polyethylene glycol building blocks of said vitamin E succinate have a molecular weight of 500Da to 5000Da.
  4. 4. The penetration-promoting skin nanocomposite globulin according to claim 1, wherein the poloxamer comprises polyoxyethylene in an amount of from 70% to 75% by mass and has an average molecular weight of from 8000Da to 15000Da.
  5. 5. A penetration enhancing skin nanocomposite spheropeptide according to any one of claims 1 to 4, wherein at least one of the following conditions is met: (1) In the composite peptide, the mass ratio of the components (i), (ii) and (iii) is 1 (0.8-1.2): 0.8-1.2; (2) The mass ratio of the compound peptide to the tolochia is (0.0001-0.5): 1-20; (3) The mass ratio of the tolcoronene to the poloxamer is (1-1.5): 1.
  6. 6. A penetration enhancing skin nanocomposite spheropeptide according to any one of claims 1 to 4, wherein at least one of the following conditions is met: (1) The weight percentage of the composite peptide in the first solution is 0.0001-0.5%; (2) The weight percentage of the tolclomazone in the second solution is 20% -60%; (3) The weight percentage of the poloxamer in the third solution is 0.1% -5%.
  7. 7. The penetration enhancing skin nanocomposite spheropeptides according to any one of claims 1-4, wherein said first solution is added to said fourth solution at a first rate and said step of stirring and dispersing at a fourth temperature is performed at a stirring and dispersing speed of 100rpm-600rpm.
  8. 8. Use of a penetration enhancing skin nanocomposite globulin according to any one of claims 1 to 7 in the preparation of a cosmetic.
  9. 9. The use according to claim 8, wherein the cosmetic product is an antioxidant product.
  10. 10. The use according to claim 8, characterized in that the cosmetic is a product for scalp oil control, anti-hair loss and anti-aging.

Description

Penetration-promoting skin nano-composite globule peptide, preparation method thereof and application thereof in preparation of scalp oil control, anti-drop and anti-aging products Technical Field The application relates to the technical field of transdermal delivery and cosmetics, in particular to a penetration-promoting skin nano-composite globule peptide, a preparation method thereof and application thereof in preparing scalp oil control, anti-drop and anti-aging products. Background In the cosmetic and skin care fields, polypeptides have great potential in skin care and pharmacotherapy due to their high biological activity. Lipid modification such as palmitoylation is a common means for solving the problem of polypeptide transdermal in cosmetics, and the originally water-soluble polypeptide is changed into a lipid-soluble precursor by linking fatty acid chains, so that the affinity of the polypeptide with the stratum corneum is enhanced. Among them, palmitoyl tripeptide-1, palmitoyl tripeptide-5 and palmitoyl tetrapeptide-7 are representative members and have been demonstrated to be effective in promoting collagen synthesis, inhibiting inflammatory reactions and repairing damaged skin barriers. However, the polypeptide modified with lipid such as palmitoylation becomes a lipid-soluble polypeptide, and is difficult to apply to aqueous products. The prior application technology is mainly designed for water-soluble polypeptides, and when treating fat-soluble polypeptides, the prior application technology faces the bottlenecks of poor solubility, low stability (easy hydrolysis and easy precipitation) and insufficient delivery efficiency in a water-based formula system, so that the commercial development and the exertion of terminal efficacy are seriously restricted. In the technical field of active ingredient delivery, self-assembly of amphiphilic polymers to form micelles is an effective strategy for solubilizing hydrophobic drugs. At present, although poloxamer or tolocham is singly used as a polypeptide carrier to prepare polypeptide micelles, the stability of the micelles is not strong, the polypeptides can be separated out and degraded, and in addition, the transdermal effect of the micelles and the dispersion performance of the micelles in water aqua are still to be improved. Disclosure of Invention Through a large number of experiments, the penetration-promoting nano composite ball peptide which is prepared by taking the tolochen and the poloxamer as carriers and adopting a proper method has small particle size, high stability and excellent transdermal absorption performance, and has good effects of controlling oil, preventing alopecia and resisting aging on scalp. The first aspect of the application provides a penetration-promoting skin nanocomposite globulin, which comprises the following steps: Adding a compound peptide into a first organic solvent, mixing, and carrying out ultrasonic dissolution at a first temperature to obtain a first solution, wherein the composition of the compound peptide comprises components (i) - (iii) including (i) palmitoyl tripeptide-1 or a derivative thereof, (ii) palmitoyl tripeptide-5 or a derivative thereof, and (iii) palmitoyl tetrapeptide-7 or a derivative thereof, wherein the first organic solvent is aliphatic polyol, and the first temperature is 35-45 ℃; Adding the tolocham into a second organic solvent, mixing, and heating and dissolving at a second temperature to obtain a second solution, wherein the tolocham is vitamin E polyethylene glycol succinate, the second organic solvent is aliphatic polyol, and the second temperature is 40-60 ℃; Adding poloxamer into the first water, mixing, and heating and dissolving at a third temperature to obtain a third solution, wherein the third temperature is 40-60 ℃; mixing the second solution and the third solution to prepare a fourth solution; and adding the first solution into a fourth solution at a first rate, stirring and dispersing at a fourth temperature to obtain the penetration-promoting skin nano composite globule peptide, wherein the first rate is 1-3 mL/min, and the fourth temperature is 40-50 ℃. The penetration-promoting skin nano-composite globule peptide is prepared by a specific preparation method, so that a hydrophobic vitamin E group of the tolochoene and a polyoxypropylene chain of the poloxamer are synergistic to form a stable hydrophobic inner core to effectively wrap fat-soluble polypeptide, and meanwhile, a hydrophilic polyethylene glycol chain of the tolochoene and a polyoxyethylene chain of the poloxamer are mutually interwoven to form a compact hydrophilic protective layer, so that the nano-micelle has good transdermal property and stability, smaller particle size and better dispersion performance, and the problems of poor permeability, low solubility in water, poor stability and the like of the fat-soluble polypeptide are effectively solved. The penetration-promoting skin nano-composite globule pepti