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CN-122005346-A - Whitening composition, modified glutathione and preparation method thereof

CN122005346ACN 122005346 ACN122005346 ACN 122005346ACN-122005346-A

Abstract

The invention relates to a whitening composition, modified glutathione and a preparation method thereof. The preparation method of the modified glutathione specifically comprises the following steps of 1) obtaining liposome suspension, mixing the liposome suspension with hyaluronidase and a cross-linking agent after ultrasonic dispersion, stirring to obtain HAase-Lip suspension, and 2) mixing glutathione with the HAase-Lip suspension, stirring for reaction, and carrying out ultrasonic treatment. The phospholipid bilayer vesicle structure of Lip can form a physical barrier, and the efficacy attenuation of the phospholipid bilayer vesicle structure is greatly delayed. Meanwhile, the Lip skin-like lipid structure can be fused with a stratum corneum lipid bilayer, the nanoscale particle size can be adapted to the gap size of the stratum corneum and penetrate through the stratum corneum by means of a penetration mechanism, and on the other hand, HAase has the capability of degrading hyaluronic acid on the skin surface layer, assists in deep penetration of Lip and internal GSH into the epidermis and reduces damage of transdermal penetration to a skin barrier.

Inventors

  • ZHI QIN
  • ZHANG LIXIANG
  • LI XINYU
  • WU LIFEN
  • CHEN YUANKUI
  • GUO GUIQUAN

Assignees

  • 深圳市健翔生物制药有限公司

Dates

Publication Date
20260512
Application Date
20251231

Claims (10)

  1. 1. A method for preparing modified glutathione, comprising the steps of: 1) Obtaining liposome suspension, mixing the liposome suspension with hyaluronidase and a cross-linking agent after ultrasonic dispersion, and stirring to obtain HAase-Lip suspension; 2) And mixing glutathione with the HAase-Lip suspension, stirring for reaction, and carrying out ultrasonic treatment to obtain the glutathione-Lip suspension.
  2. 2. The preparation method according to claim 1, wherein the liposome suspension comprises hydrogenated lecithin, cholesterol and dipalmitoyl phosphatidylethanolamine-polyethylene glycol, preferably 5-7 parts by mass of hydrogenated lecithin, 2-3 parts by mass of cholesterol and 1-2 parts by mass of dipalmitoyl phosphatidylethanolamine-polyethylene glycol.
  3. 3. The method of claim 2, wherein the solvent of the liposome suspension is chloroform.
  4. 4. The preparation method according to claim 1, wherein the power of the ultrasonic dispersion in the step 1) is 250-300W for 2-5 minutes, and the power of the ultrasonic treatment in the step 2) is 150-200W for 10-15 minutes.
  5. 5. The preparation method according to claim 2, wherein the concentration of the hyaluronidase is 1-5 mg/mL, and the mass ratio of the dipalmitoyl phosphatidylethanolamine-polyethylene glycol to the hyaluronidase is (10-20): 1.
  6. 6. The preparation method of claim 1, wherein the cross-linking agent is polyethylene glycol diacrylate, and the mass ratio of the cross-linking agent is 0.5-1% of the HAase-Lip suspension.
  7. 7. The preparation method of claim 1, wherein in the step 1), hyaluronidase is added and trehalose is added, and the mass ratio of the trehalose is 1-2% of that of the HAase-Lip suspension.
  8. 8. A modified glutathione produced by the production process of any one of claims 1 to 7.
  9. 9. A whitening composition characterized in that the raw materials comprise carbomer, trehalose, betaine, allantoin, glycereth-26, EDTA-2 sodium, butylene glycol, triethanolamine, 1,2 hexanediol, phenoxyethanol, glycerol, carnosine, and glutathione, said glutathione being the modified glutathione of claim 8.
  10. 10. The whitening composition according to claim 9, wherein the raw materials further comprise a perfume and/or a compatibilizer.

Description

Whitening composition, modified glutathione and preparation method thereof Technical Field The invention relates to the technical field of cosmetic preparations, in particular to a whitening composition, modified glutathione and a preparation method thereof. Background Along with the continuous upgrading of the skin whitening demands of consumers and the improvement of the efficacy and safety cognition of skin care products, the development of efficient, stable and mild whitening active ingredients becomes an important research point in the field of cosmetics. Melanin excessive deposition is a core cause of skin darkness and color spot formation, the generation process of the melanin excessive deposition is to catalyze tyrosine to be converted into dopa and dopaquinone through tyrosinase, and finally the melanin is polymerized, and Reactive Oxygen Species (ROS) accumulation caused by oxidative stress can further accelerate the process, simultaneously destroy skin barrier and aggravate pigmentation. Glutathione (GSH) is taken as an endogenous tripeptide compound, is an ideal active ingredient with oxidation resistance and whitening effects, and has definite action mechanism, on one hand, sulfhydryl (-SH) in glutathione molecules can directly remove ROS in skin, inhibit the stimulation of oxidative stress reaction to melanocytes and reduce upstream inducement of melanin synthesis, and on the other hand, glutathione can be combined with copper ions of tyrosinase active centers to competitively block the catalytic path of tyrosine, accelerate the reduction and decomposition of generated melanin, and realize the full-link whitening effect from source inhibition to later desalination. In addition, glutathione is an endogenous component, has excellent biocompatibility, has lower irritation compared with traditional whitening components such as hydroquinone, tretinoin and the like, and is suitable for special skin types such as sensitive muscles and the like, so that the glutathione has extremely high application potential in the field of whitening skin care products. However, the practical application of glutathione in whitening compositions is limited by two major core technical bottlenecks for a long time, severely restricting the efficacy of glutathione to be exerted: 1) The glutathione has extremely poor stability, the efficacy core of easy oxidation and deactivation of glutathione depends on free sulfhydryl groups in molecules, and the chemical property of the group is extremely active, and the group is easy to react with oxygen in the environment, metal ions and other components in the composition to be oxidized and deactivated. In a conventional whitening composition system, on one hand, oxygen contacted with the composition during production, storage and use can oxidize sulfhydryl into disulfide bond to form inactive oxidized glutathione (GSSG) which has a half-life of usually less than 7 days at normal temperature, and the product has serious effect attenuation in shelf life, on the other hand, metal ions such as inevitable trace iron, copper and the like in the composition can catalyze the oxidization reaction of the sulfhydryl to accelerate the degradation of the glutathione, and in addition, if components such as preservative, essence and the like are compounded in the composition, the oxidization of partial components can further aggravate the inactivation of the glutathione, so that the actual effect of the final product is far lower than a theoretical value. In the prior art, although an attempt is made to delay the oxidation of the glutathione by adding an antioxidant such as sulfite, the sulfite component is easy to trigger skin sensitization, and the oxidation can be delayed only briefly, so that the problem of stability of the glutathione cannot be fundamentally solved. 2) The transdermal absorption efficiency is extremely low, the skin stratum corneum, which is difficult to penetrate through the skin barrier, is the main barrier for the transdermal penetration of the active ingredient, and the permeability of the dense lipid bilayer structure to water-soluble ingredients is extremely low. Glutathione is a strong water-soluble polar molecule with a molecular mass of about 307 Da and no fat-soluble group, in the conventional whitening composition, more than 90% of glutathione can only stay on the skin surface layer and cannot penetrate through the stratum corneum to reach melanocytes of the epidermis basal layer and oxidative stress sites of the dermis layer. In the prior art, some schemes improve the permeability by adding transdermal promoters such as ethanol, permeation promoting peptide and the like, but the ethanol is easy to damage skin barrier to cause the problems of dryness, redness and the like, the permeation promoting peptide has high cost and poor compatibility with glutathione, and other schemes adopt liposome wrapping technology to improve the transdermal property, but common lipos