Active peptide composition and application thereof in preparation of anti-aging and wrinkle-removing products

Abstract

The invention relates to the technical field of active peptides, in particular to an active peptide composition and application thereof in preparation of anti-aging and wrinkle-removing products. The composition provided by the invention comprises the neurotransmitter regulating peptide and the signal peptide, and the components are properly selected, so that the composition can play a better role in anti-aging and anti-wrinkle aspects. In addition, the oil-soluble wrapped anti-aging and anti-wrinkle composition prepared by the invention aims to be quickly absorbed through skin, and the utilization rate of the active polypeptide is effectively improved.

Description

Technical Field

[0001] The present invention relates to the technical field of active peptides, and particularly to an active peptide composition and its application in the preparation of anti-aging and anti-wrinkle products. Background Art

[0002] With the continuous development of social economy and the continuous improvement of the public's living standards, skin anti-aging has become an important research direction in the cosmetics field that has attracted much attention. As the main barrier between the human body and the external environment, the aging process of the skin is accompanied by a series of physiological changes such as deepening wrinkles, decreasing elasticity, and pigmentation, which not only affect the appearance beauty but also reflect the aging process of the body. To meet the urgent market demand for highly efficient skin anti-aging products, the cosmetics industry is committed to developing new products with functions such as anti-wrinkle, whitening, and moisturizing. Among them, finding safe and highly efficient active ingredients is the key to research and development.

[0003] Active polypeptides are a class of small molecule compounds formed by amino acids connected through peptide bonds. Existing research shows that some active polypeptides can activate key signal pathways in skin cells and promote the synthesis of extracellular matrix components such as collagen and elastic fibers, thereby enhancing skin elasticity and reducing wrinkles; some other active polypeptides can inhibit melanin production by regulating the physiological functions of melanocytes to achieve a whitening effect. For example, signal peptide-like polypeptides can target and bind to cell surface receptors, accelerate the penetration of active ingredients, and have anti-aging and moisturizing effects; neurotransmitter regulatory peptide-like polypeptides can produce multiple anti-wrinkle effects through different combinations. However, in the actual application process, the use of active polypeptides still faces many technical problems.

[0004] First of all, the stability problem of active polypeptides needs to be solved urgently. Most water-based active polypeptide products are extremely sensitive to environmental factors such as temperature, pH, and oxidation during storage and use, and are prone to structural damage and loss of activity, resulting in a significant reduction in product efficacy. Secondly, the barrier effect of the skin cutin layer makes it difficult for ordinary forms of active polypeptides to effectively penetrate the skin, and a large amount of active ingredients cannot reach the skin action target, causing waste of resources. In addition, although the combination of different types of active polypeptides can achieve efficacy superposition to a certain extent, due to the lack of a precise regulation mechanism, it is difficult to achieve high-efficiency synergistic enhancement at the level of multi-signal pathway cross-regulation and functional complementarity, and the combined effect of multiple active polypeptides cannot be fully exerted.

[0005] The water-in-oil microemulsion technology provides a new solution for the delivery of active peptides due to its unique oil-phase encapsulated water-phase structure. By embedding active peptides in the microemulsion system, this technology can significantly improve the oil solubility and fat solubility of the peptides, enhance their compatibility with skin lipids, and thus improve their ability to penetrate the skin barrier and bioavailability; on the other hand, the microemulsion structure can provide a stable physicochemical environment for the active peptides, effectively reduce the impact of external factors on the peptides, and reduce their degradation. Although the water-in-oil microemulsion technology has significant advantages in the delivery of active peptides, there are still technical bottlenecks in practical applications. For example, due to the large differences in the physicochemical properties of different active peptides, how to optimize the microemulsion system formula for specific peptides, while ensuring the stability of the system while retaining the activity of the peptides to the maximum extent; and how to accurately control the proportion of each component of the microemulsion system to achieve synergistic enhancement between multiple active peptides, are still technical problems that need to be solved in this field. Summary of the invention

[0006] In view of this, the technical problem to be solved by the present invention is to provide an active peptide composition and its application in the preparation of anti-aging and anti-wrinkle products.

[0007] The active peptide composition provided by the invention comprises a signal peptide and a neurotransmitter regulating peptide.

[0008] In the present invention, the signal peptide includes at least one of blue copper peptide, acetyl tetrapeptide-5, acetyl tetrapeptide-9, palmitoyl pentapeptide-4, palmitoyl tripeptide-1, palmitoyl tripeptide-5, palmitoyl tetrapeptide-2, tripeptide-1, tripeptide-9, and nonapeptide-1.

[0009] The present invention provides a composition of a signal peptide and a neurotransmitter regulating peptide, wherein the number of the signal peptides is 1 to 10, for example, 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10.

[0010] As a feasibility case, the types of signal peptides are two, which are: GHK-Cu and Acetyl Tetrapeptide-5, or GHK-Cu and Acetyl Tetrapeptide-9, or GHK-Cu and Palmitoyl Pentapeptide-4, or GHK-Cu and Palmitoyl Tripeptide-1, or GHK-Cu and Palmitoyl Tripeptide-5, or GHK-Cu and Palmitoyl Tetrapeptide-2, or GHK-Cu and Tripeptide-1, or GHK-Cu and Tripeptide-9, or GHK-Cu and Nonapeptide-1, or Acetyl Tetrapeptide-5 and Acetyl Tetrapeptide-9, or Acetyl Tetrapeptide-5 and Palmitoyl Pentapeptide-4, or Acetyl Tetrapeptide-5 and Palmitoyl Tripeptide-1, or Acetyl Tetrapeptide-5 and Palmitoyl Tripeptide-5, or Acetyl Tetrapeptide-5 and Palmitoyl Tetrapeptide-2, or Acetyl Tetrapeptide-5 and Tripeptide-1, or Acetyl Tetrapeptide-5 and Tripeptide-9, or Acetyl Tetrapeptide-5 and Nonapeptide-1, or Acetyl Tetrapeptide-9 and Palmitoyl Pentapeptide-4, or Acetyl Tetrapeptide-9 and Palmitoyl Tripeptide-1, or Acetyl Tetrapeptide-9 and Palmitoyl Tripeptide-5, or Acetyl Tetrapeptide-9 and Palmitoyl Tetrapeptide-2, or Acetyl Tetrapeptide-9 and Tripeptide-1, or Acetyl Tetrapeptide-9 and Tripeptide-9, or Acetyl Tetrapeptide-9 and Nonapeptide-1, or Palmitoyl Pentapeptide-4 and Palmitoyl Tripeptide-1, or Palmitoyl Pentapeptide-4 and Palmitoyl Tripeptide-5, or Palmitoyl Pentapeptide-4 and Palmitoyl Tetrapeptide-2, or Palmitoyl Pentapeptide-4 and Tripeptide-1, or Palmitoyl Pentapeptide-4 and Tripeptide-9, or Palmitoyl Pentapeptide-4 and Nonapeptide-1, or Palmitoyl Tripeptide-1 and Palmitoyl Tripeptide-5, or Palmitoyl Tripeptide-1 and Palmitoyl Tetrapeptide-2, or Palmitoyl Tripeptide-1 and Tripeptide-1, or Palmitoyl Tripeptide-1 and Tripeptide-9, or Palmitoyl Tripeptide-1 and Nonapeptide-1, or Palmitoyl Tripeptide-5 and Palmitoyl Tetrapeptide-2, or Palmitoyl Tripeptide-5 and Tripeptide-1, or Palmitoyl Tripeptide-5 and Tripeptide-9, or Palmitoyl Tripeptide-5 and Nonapeptide-1, or Palmitoyl Tetrapeptide-2 and Tripeptide-1, or Palmitoyl Tetrapeptide-2 and Tripeptide-9, or Palmitoyl Tetrapeptide-2 and Nonapeptide-1, or Tripeptide-1 and Tripeptide-9, or Tripeptide-1 and Nonapeptide-1, or Tripeptide-9 and Nonapeptide-1.

[0011] As a feasibility case, the number of signal peptides is three, namely: copper peptide, acetyl tetrapeptide-5 and acetyl tetrapeptide-9, or copper peptide, acetyl tetrapeptide-5 and palmitoyl pentapeptide-4, or copper peptide, acetyl tetrapeptide-5 and palmitoyl tripeptide-1, or copper peptide, acetyl tetrapeptide-5 and palmitoyl tripeptide-5, or copper peptide, acetyl tetrapeptide-5 and palmitoyl tetrapeptide-2, or copper peptide, acetyl tetrapeptide-5 and tripeptide-1, or copper peptide, acetyl tetrapeptide-5 and tripeptide-9, or copper peptide, acetyl tetrapeptide-5 and nonapeptide-1, or copper peptide, acetyl tetrapeptide-9 and palmitoyl pentapeptide-4, or copper peptide, acetyl tetrapeptide-9 and palmitoyl tripeptide-1, or copper peptide, acetyl tetrapeptide-9 and palmitoyl tripeptide-5, or copper peptide, acetyl tetrapeptide-9 and palmitoyl tetrapeptide-2, or copper peptide, acetyl tetrapeptide-9 and tripeptide-1, or copper peptide, acetyl tetrapeptide-9 and tripeptide-9, or copper peptide, acetyl tetrapeptide-9 and nonapeptide-1, or copper peptide, palmitoyl pentapeptide-4 and palmitoyl tripeptide-1, or copper peptide, palmitoyl pentapeptide-4 and palmitoyl tripeptide-5, or copper peptide, palmitoyl pentapeptide-4 and palmitoyl tetrapeptide-2, or copper peptide, palmitoyl pentapeptide-4 and tripeptide-1, or copper peptide, palmitoyl pentapeptide-4 and tripeptide-9, or copper peptide, palmitoyl pentapeptide-4 and nonapeptide-1, or copper peptide, palmitoyl tripeptide-1 and palmitoyl tripeptide-5, or copper peptide, palmitoyl tripeptide-1 and palmitoyl tetrapeptide-2, or copper peptide, palmitoyl tripeptide-1 and tripeptide-1, or copper peptide, palmitoyl tripeptide-1 and tripeptide-9, or copper peptide, palmitoyl tripeptide-1 and nonapeptide-1, or copper peptide, palmitoyl tripeptide-5 and palmitoyl tetrapeptide-2, or copper peptide, palmitoyl tripeptide-5 and tripeptide-1, or copper peptide, palmitoyl tripeptide-5 and tripeptide-9, or copper peptide, palmitoyl tripeptide-5 and nonapeptide-1, or copper peptide, palmitoyl tetrapeptide-2 and tripeptide-1, or copper peptide, palmitoyl tetrapeptide-2 and tripeptide-9, or copper peptide, palmitoyl tetrapeptide-2 and nonapeptide-1, or copper peptide, tripeptide-1 and tripeptide-9, or copper peptide, tripeptide-1 and nonapeptide-1, or copper peptide, tripeptide-9 and nonapeptide-1, or acetyl tetrapeptide-5, acetyl tetrapeptide-9 and palmitoyl pentapeptide-4, or acetyl tetrapeptide-5, acetyl tetrapeptide-9 and palmitoyl tripeptide-1, or acetyl tetrapeptide-5, acetyl tetrapeptide-9 and palmitoyl tripeptide-5, or acetyl tetrapeptide-5, acetyl tetrapeptide-9 and palmitoyl tetrapeptide-2, or acetyl tetrapeptide-5, acetyl tetrapeptide-9 and tripeptide-1, or acetyl tetrapeptide-5, acetyl tetrapeptide-9 and tripeptide-9, or acetyl tetrapeptide-5, acetyl tetrapeptide-9 and nonapeptide-1, or acetyl tetrapeptide-5, palmitoyl pentapeptide-4 and palmitoyl tripeptide-1, or acetyl tetrapeptide-5,Palmitoyl Pentapeptide-4 and Tripeptide-1, or Acetyl Tetrapeptide-5, Palmitoyl Pentapeptide-4 and Tripeptide-9, or Acetyl Tetrapeptide-5, Palmitoyl Pentapeptide-4 and Nonapeptide-1, or Acetyl Tetrapeptide-5, Palmitoyl Tripeptide-1 and Palmitoyl Tripeptide-5, or Acetyl Tetrapeptide-5, Palmitoyl Tripeptide-1 and Palmitoyl Tetrapeptide-2, or Acetyl Tetrapeptide-5, Palmitoyl Tripeptide-1 and Tripeptide-1, or Acetyl Tetrapeptide-5, Palmitoyl Tripeptide-1 and Tripeptide-9, or Acetyl Tetrapeptide-5, Palmitoyl Tripeptide-1 and Nonapeptide-1, or Acetyl Tetrapeptide-5, Palmitoyl Tripeptide-5 and Palmitoyl Tetrapeptide-2, or Acetyl Tetrapeptide-5, Palmitoyl Tripeptide-5 and Tripeptide-1, or Acetyl Tetrapeptide-5, Palmitoyl Tripeptide-5 and Tripeptide-9, or Acetyl Tetrapeptide-5, Palmitoyl Tripeptide-5 and Nonapeptide-1, or Acetyl Tetrapeptide-5, Palmitoyl Tetrapeptide-2 and Tripeptide-1, or Acetyl Tetrapeptide-5, Palmitoyl Tetrapeptide-2 and Tripeptide-9, or Acetyl Tetrapeptide-5, Palmitoyl Tetrapeptide-2 and Nonapeptide-1, or Acetyl Tetrapeptide-5, Tripeptide-1 and Tripeptide-9, or Acetyl Tetrapeptide-5, Tripeptide-1 and Nonapeptide-1, or Acetyl Tetrapeptide-5, Tripeptide-9 and Nonapeptide-1, or Acetyl Tetrapeptide-9, Palmitoyl Pentapeptide-4 and Palmitoyl Tripeptide-1, or Acetyl Tetrapeptide-9, Palmitoyl Pentapeptide-4 and Palmitoyl Tripeptide-5, or Acetyl Tetrapeptide-9, Palmitoyl Pentapeptide-4 and Palmitoyl Tetrapeptide-2, or Acetyl Tetrapeptide-9, Palmitoyl Pentapeptide-4 and Tripeptide-1, or Acetyl Tetrapeptide-9, Palmitoyl Pentapeptide-4 and Tripeptide-9, or Acetyl Tetrapeptide-9, Palmitoyl Pentapeptide-4 and Nonapeptide-1, or Acetyl Tetrapeptide-9, Palmitoyl Tripeptide-1 and Palmitoyl Tripeptide-5, or Acetyl Tetrapeptide-9, Palmitoyl Tripeptide-1 and Palmitoyl Tetrapeptide-2, or Acetyl Tetrapeptide-9, Palmitoyl Tripeptide-1 and Tripeptide-1, or Acetyl Tetrapeptide-9, Palmitoyl Tripeptide-1 and Tripeptide-9, or Acetyl Tetrapeptide-9, Palmitoyl Tripeptide-1 and Nonapeptide-1, or Acetyl Tetrapeptide-9, Palmitoyl Tripeptide-5 and Palmitoyl Tetrapeptide-2, or Acetyl Tetrapeptide-9, Palmitoyl Tripeptide-5 and Tripeptide-1, or Acetyl Tetrapeptide-9, Palmitoyl Tripeptide-5 and Tripeptide-9, or Acetyl Tetrapeptide-9, Palmitoyl Tripeptide-5 and Nonapeptide-1, or Acetyl Tetrapeptide-9, Palmitoyl Tetrapeptide-2 and Tripeptide-1, or Acetyl Tetrapeptide-9, Palmitoyl Tetrapeptide-2 and Tripeptide-9, or Acetyl Tetrapeptide-9, Palmitoyl Tetrapeptide-2 and Nonapeptide-1, or Acetyl Tetrapeptide-9, Tripeptide-1 and Tripeptide-9, or Acetyl Tetrapeptide-9, Tripeptide-1 and Nonapeptide-1, or Acetyl Tetrapeptide-9, Tripeptide-9 and Nonapeptide-1, or Palmitoyl Pentapeptide-4, Palmitoyl Tripeptide-1 and Palmitoyl Tripeptide-5, or Palmitoyl Pentapeptide-4, Palmitoyl Tripeptide-1 and Palmitoyl Tetrapeptide-2, or Palmitoyl Pentapeptide-4, Palmitoyl Tripeptide-1 and Tripeptide-1, or Palmitoyl Pentapeptide-4, Palmitoyl Tripeptide-1 and Tripeptide-9Either palmitoyl pentapeptide-4, palmitoyl tripeptide-1 and nonapeptide-1, or palmitoyl pentapeptide-4, palmitoyl tripeptide-5 and palmitoyl tetrapeptide-2, or palmitoyl pentapeptide-4, palmitoyl tripeptide-5 and tripeptide-1, or palmitoyl pentapeptide-4, palmitoyl tripeptide-5 and tripeptide-9, or palmitoyl pentapeptide-4, palmitoyl tripeptide-5 and nonapeptide-1, or palmitoyl pentapeptide-4, palmitoyl tetrapeptide-2 and tripeptide-1, or palmitoyl pentapeptide-4, palmitoyl tetrapeptide-2 and tripeptide-9, or palmitoyl pentapeptide-4, palmitoyl tetrapeptide-2 and nonapeptide-1, or palmitoyl pentapeptide-4, tripeptide-1 and tripeptide-9, or palmitoyl pentapeptide-4, tripeptide-1 and nonapeptide-1, or palmitoyl pentapeptide-4, tripeptide-9 and nonapeptide-1, or palmitoyl tripeptide-1, palmitoyl tripeptide-5 and palmitoyl tetrapeptide-2, or palmitoyl tripeptide-1, palmitoyl tripeptide-5 and tripeptide-1, or palmitoyl tripeptide-1, palmitoyl tripeptide-5 and tripeptide-9, or palmitoyl tripeptide-1, palmitoyl tripeptide-5 and nonapeptide-1, or palmitoyl tripeptide-1, palmitoyl tetrapeptide-2 and tripeptide-1, or palmitoyl tripeptide-1, palmitoyl tetrapeptide-2 and tripeptide-9, or palmitoyl tripeptide-1, palmitoyl tetrapeptide-2 and nonapeptide-1, or palmitoyl tripeptide-1, tripeptide-1 and tripeptide-9, or palmitoyl tripeptide-1, tripeptide-1 and nonapeptide-1, or palmitoyl tripeptide-1, tripeptide-9 and nonapeptide-1, or palmitoyl tripeptide-5, palmitoyl tetrapeptide-2 and tripeptide-1, or palmitoyl tripeptide-5, palmitoyl tetrapeptide-2 and tripeptide-9, or palmitoyl tripeptide-5, palmitoyl tetrapeptide-2 and nonapeptide-1, or palmitoyl tripeptide-5, tripeptide-1 and tripeptide-9, or palmitoyl tripeptide-5, tripeptide-1 and nonapeptide-1, or palmitoyl tripeptide-5, tripeptide-9 and nonapeptide-1, or palmitoyl tetrapeptide-2, tripeptide-1 and tripeptide-9, or palmitoyl tetrapeptide-2, tripeptide-1 and nonapeptide-1, or palmitoyl tetrapeptide-2, tripeptide-9 and nonapeptide-1, or tripeptide-1, tripeptide-9 and nonapeptide-1,

[0012] The situation where the types of signal peptides are 4 to 10 is similar, and the present invention will not elaborate on this, but their implementations are all within the protection scope of the present invention.

[0013] In the present invention, the neurotransmitter regulating peptide includes at least one of acetyl hexapeptide-8, viper venom peptide, and conotoxin peptide.

[0014] In the composition of the present invention, the number of neurotransmitter regulating peptides is 1 to 3, for example, it is 1, 2, or 3.

[0015] As a feasible case, the neurotransmitter regulating peptide is acetyl hexapeptide-8, viper venom peptide or conotoxin peptide, or acetyl hexapeptide-8 and viper venom peptide, or acetyl hexapeptide-8 and conotoxin peptide, or viper venom peptide and conotoxin peptide, or acetyl hexapeptide-8, viper venom peptide and conotoxin peptide.

[0016] In the composition provided by the present invention, the signal peptide specifically binds to membrane surface proteins, such as integrin receptors, to form microdomains locally on the cell surface membrane, attracting the aggregation of other components. At the same time, the interaction between the polypeptide and the membrane protein can change the fluidity of the local lipid bilayer, assisting the transmembrane transport of other polypeptides. The signal peptide selected in the present invention has the effects of specifically binding and regulating transforming growth factor-β or integrin receptors, etc. The signal peptide specifically binds to cell surface receptors, playing a synergistic role in guiding and delivering, and strengthening the absorption and action of neurotransmitter regulatory peptides.

[0017] In the present invention, the selection of neurotransmitter regulatory peptides and signal peptides is reasonable and appropriate, so that the composition can have a better effect in anti-aging and anti-wrinkle aspects. Preferably, the composition is composed of copper peptide, acetyl tetrapeptide-5, acetyl tetrapeptide-9, acetyl hexapeptide-8, snake venom-like peptide and conotoxin peptide. Experiments show that the composition composed of copper peptide, acetyl tetrapeptide-5, acetyl tetrapeptide-9, acetyl hexapeptide-8, snake venom-like peptide and conotoxin peptide can produce a more significant synergistic effect compared with the combination of other components.

[0018] The present invention optimizes the mass parts of each component in the composition. Preferably, the composition described in the present invention is composed of the following components in mass parts:

[0019]

[0020] In some embodiments, the composition is composed of 1-5 parts of copper peptide, 2-4 parts of acetyl tetrapeptide-5, 1-2 parts of acetyl tetrapeptide-9, 4-5 parts of acetyl hexapeptide-8, 5-6 parts of snake venom-like peptide and 0.1 part of conotoxin peptide.

[0021] In some other embodiments, the composition is composed of 2-5 parts of copper peptide, 2-3 parts of acetyl tetrapeptide-5, 1-3 parts of acetyl tetrapeptide-9, 2-5 parts of acetyl hexapeptide-8, 5 parts of snake venom-like peptide and 0.1-0.2 part of conotoxin peptide.

[0022] In some specific embodiments, the composition is composed of 5 parts of copper peptide, 2 parts of acetyl tetrapeptide-5, 1 part of acetyl tetrapeptide-9, 5 parts of acetyl hexapeptide-8, 5 parts of snake venom-like peptide and 0.1 part of conotoxin peptide.

[0023] In some other specific embodiments, the composition is composed of 1 part of copper peptide, 4 parts of acetyl tetrapeptide-5, 2 parts of acetyl tetrapeptide-9, 4 parts of acetyl hexapeptide-8, 6 parts of snake venom-like peptide and 0.1 part of conotoxin peptide.

[0024] In some other specific embodiments, the composition consists of 3 parts of copper peptide, 54 parts of acetyl tetrapeptide-5, 91 parts of acetyl tetrapeptide-9, 83 parts of acetyl hexapeptide-8, 5 parts of syn-ake peptide and 0.2 parts of conotoxin peptide.

[0025] In some other specific embodiments, the composition consists of 4 parts of copper peptide, 52 parts of acetyl tetrapeptide-5, 92 parts of acetyl tetrapeptide-9, 83 parts of acetyl hexapeptide-8, 6 parts of syn-ake peptide and 0.1 parts of conotoxin peptide.

[0026] In some other specific embodiments, the composition consists of 2 parts of copper peptide, 53 parts of acetyl tetrapeptide-5, 93 parts of acetyl tetrapeptide-9, 82 parts of acetyl hexapeptide-8, 5 parts of syn-ake peptide and 0.2 parts of conotoxin peptide.

[0027] Furthermore, the present invention provides the application of the active peptide composition as described above in the preparation of anti-aging and anti-wrinkle products.

[0028] Even further, the present invention also provides a microemulsion for anti-aging and anti-wrinkle, which comprises the active peptide composition as described above and excipients.

[0029] In the microemulsion of the present invention, the active polypeptide is encapsulated in the inner core aqueous phase to avoid degradation caused by direct contact with the external environment. The outer phase oil-based solution reduces the penetration resistance and expands the lipid gap based on the principle of similar phase solubility, breaks through the barrier limitation and improves the penetration ability. At the same time, the slow-release property of the water-in-oil prolongs the residence time of the active polypeptide component in the epidermis.

[0030] In some embodiments, the microemulsion comprises the following raw materials in mass fractions: signal peptide 0.01% - 1%, neurotransmitter regulatory peptide 0.01% - 2%, oil phase matrix 40% - 70%, emulsifier 5% - 20%, cosolvent 2% - 10%, preservative 0.1 - 1.0%, and the balance is water.

[0031] The microemulsion preparation provided by the present invention contains the active peptide composition of the present invention, and realizes high transdermal rate and high stability through the screening and optimization of excipients. Preliminary experiments show that the following excipients have a more positive significance for improving the transdermal rate and stability:

[0032] The excipients include at least one of water, emulsifier, cosolvent, oily matrix and preservative;

[0033] The oil phase matrix is selected from at least one of isopropyl myristate, isopropyl palmitate, ethylhexyl palmitate, caprylic / capric triglyceride, jojoba oil, olive oil, camellia seed oil, isononyl isononanoate, squalane, cyclohexasiloxane, hydrogenated polyisobutene, light mineral oil;

[0034] The emulsifier is selected from at least one of Tween 80, Span 80, Tween 20, Span 20, sucrose laurate, PEG-7 hydrogenated castor oil, cetyl PEG / PPG-10 / 1 polydimethylsiloxane;

[0035] The cosolvent is selected from at least one of ethanol, ethylene glycol, propylene glycol, glycerol, n-butanol;

[0036] The preservative is selected from at least one of phenoxyethanol, sorbic acid, caprylyl glycol, 1,2-hexanediol, p-hydroxyacetophenone.

[0037] In a specific embodiment, the microemulsion includes the following excipients: Tween, Span, absolute ethanol, isopropyl myristate, caprylic / capric triglyceride, squalane, and phenoxyethanol.

[0038] The excipients in the microemulsion of the present invention are not only applicable to the active peptide composition as described above, but also applicable to other polypeptides.

[0039] For example, the microemulsion of the present invention includes the active peptide composition as described above, Tween, Span, absolute ethanol, isopropyl myristate, caprylic / capric triglyceride, squalane, and phenoxyethanol.

[0040] Or the microemulsion of the present invention includes other polypeptides, Tween, Span, absolute ethanol, isopropyl myristate, caprylic / capric triglyceride, squalane, and phenoxyethanol. As a feasible case, the other polypeptides include but are not limited to at least one of carnosine, glutathione, nonapeptide-1, palmitoyl tripeptide-5, or tripeptide-29.

[0041] More specifically, the microemulsion includes the following components in parts by mass:

[0042] Copper peptide 0.01% - 0.05%, acetyl tetrapeptide-5 0.02% - 0.04%, acetyl tetrapeptide-9 0.01% - 0.03%, acetyl hexapeptide-8 0.02% - 0.05%, syn-ake peptide 0.05% - 0.06%, conotoxin peptide 0.001% - 0.002%, Tween-80 14.6% - 17%, Span-80 3% - 5.4%, absolute ethanol 4% - 5%, isopropyl myristate 40% - 55%, caprylic / capric triglyceride 5% - 20%, squalane 5% - 8%, phenoxyethanol 0.1%, and the balance is water.

[0043] Furthermore, the present invention also provides a preparation method of the microemulsion as described above, which includes:

[0044] Dissolving the active peptide composition and the preservative in water to obtain an aqueous phase;

[0045] Mixing the emulsifier, the cosolvent and the oily matrix to obtain an oil phase;

[0046] The oil phase and the water phase are subjected to high-speed stirring to obtain the microemulsion.

[0047] The present invention is used for preparing microemulsions by the low-energy method. The method is simple, suitable for encapsulating polypeptide compositions, easy to prepare and easy to scale up production. The obtained microemulsion is easy to be applied in cosmetics, has a high transdermal rate and strong stability.

[0048] In specific embodiments, the preparation of the microemulsion includes:

[0049] Mix the active polypeptide composition, phenoxyethanol and water as described above, and stir evenly to obtain the water phase;

[0050] Mix Tween-80 and Span-80, and sequentially add anhydrous ethanol, isopropyl myristate, triglyceride caprylate / caprate, and squalane thereto, and carry out sufficient stirring at room temperature to obtain the oil phase;

[0051] Keep the oil phase under stirring, and uniformly add the water phase to the oil phase, and control the time for adding the water phase to be 30 min; after adding the water phase, keep high-speed stirring for 1 h to obtain the microemulsion.

[0052] Furthermore, the present invention also provides an anti-aging and anti-wrinkle cosmetic, which comprises the active peptide composition or the microemulsion as described above.

[0053] The cosmetic dosage forms of the present invention include but are not limited to emulsions, aqueous solutions, gels, powders, creams, facial masks, eye creams, eye masks, aerosols, oils, sticks, lozenges, pens, lip glosses, gels, tinctures, suspensions, emulsions, serums, muds, waxes, foams, tablets, granules or films.

[0054] In some embodiments, the cosmetic comprises the microemulsion, an active substance, an oil, a humectant, sodium chloride and water;

[0055] The active substance is selected from at least one of vitamin E, retinol, bisabolol, arbutin, niacinamide, potassium methoxysalicylate, glabridin, asiaticoside, honeysuckle extract;

[0056] The oil is selected from at least one of octyl silicone oil BT-6034, cetyl PEG / PPG-10 / 1 dimethicone, petrolatum;

[0057] The humectant is selected from at least one of glycerol, butanediol, 1,2-hexanediol, hyaluronic acid.

[0058] In some embodiments, in the cosmetic, the mass fraction of the microemulsion as described above is 10% to 20%. For example, its mass fraction is 13% to 17%. More specifically, its mass fraction is 13%, 14%, 15%, 16%, 17%.

[0059] In a specific embodiment, the cosmetic comprises components in the following mass fractions: octyl silicone oil BT-603 44.0%, cetyl PEG / PPG-10 / 1 polydimethylsiloxane 0.8%, the microemulsion as described above 15%, vitamin E 0.1%, bisabolol 0.12%, petrolatum 4.0%, glycerol 8%, butylene glycol 10%, 1,2-hexanediol 1%, sodium chloride 1.5%, sodium hyaluronate 0.01%, and the balance is water.

[0060] The present invention also provides a method for preparing the cosmetic as described above, comprising:

[0061] Mixing the microemulsion, active substances and oils as described above to obtain phase A;

[0062] Mixing water and a moisturizer to obtain phase B;

[0063] Mixing phase A and phase B to obtain the cosmetic.

[0064] Furthermore, a method for anti-aging and wrinkle removal according to the present invention comprises applying the composition as described above, the microemulsion as described above or the cosmetic as described above on the skin surface.

[0065] In the present invention, the application methods as described above include but are not limited to coating, spraying, wiping, patting, massaging, applying, rubbing, dotting, smudging or airbrushing.

[0066] In the composition provided by the present invention, it includes a neurotransmitter regulating peptide and a signal peptide, and each component is properly selected, so that the composition can produce a better effect in anti-aging and anti-wrinkle aspects. Moreover, the purpose of the oil-soluble encapsulated anti-aging and anti-wrinkle composition prepared by the present invention is to be rapidly absorbed through the skin, effectively improving the utilization rate of active polypeptides. BRIEF DESCRIPTION OF THE DRAWINGS

[0067] Figure 1 Showing the product of Example 1;

[0068] Figure 2 Showing the product of Example 2;

[0069] Figure 3 Showing the product of Example 3;

[0070] Figure 4 Showing the product of Example 4;

[0071] Figure 5 Showing the product of Example 5;

[0072] Figure 6 Showing the products of Examples 6-10;

[0073] Figure 7Showing the changes in the eye wrinkles of the subjects (Example 1). Detailed implementation manners

[0074] The present invention provides an active peptide composition and its application in the preparation of anti-aging and anti-wrinkle products. Those skilled in the art can draw on the content of this article and appropriately improve the process parameters to achieve it. It should be particularly noted that all similar substitutions and modifications are obvious to those skilled in the art, and they are all regarded as included in the present invention. The methods and applications of the present invention have been described through preferred embodiments. It is obvious that relevant personnel can make changes or appropriate changes and combinations to the methods and applications in this article without departing from the content, spirit and scope of the present invention to implement and apply the technology of the present invention.

[0075] Unless otherwise defined in the present invention, scientific and technical terms related to the present invention shall have the meanings understood by those of ordinary skill in the art.

[0076] The terms "comprise", "include" and "have" can be used interchangeably, aiming to express the inclusiveness of the solution, meaning that the solution may have other elements in addition to the listed elements. At the same time, it should be understood that when using "comprise", "include" and "have" to describe in this article, the solution of "consisting of..." is also provided.

[0077] The term "and / or" describes the association relationship of associated objects, indicating that three relationships can exist. For example, A and / or B can mean: A exists alone, A and B exist simultaneously, and B exists alone. Where A and B can be singular or plural.

[0078] In this application, "at least one" means one or more, and "a plurality" means two or more. "At least one of the following" or its similar expressions refer to any combination of these items, including any combination of single item (s) or plural items (s).

[0079] The numerical ranges and parameters involved in the present invention have been presented as precisely as possible in the specific embodiments. However, any value inevitably contains standard deviations caused by individual test methods. Therefore, unless otherwise clearly stated, it should be understood that all numerical ranges or specific data used in this disclosure may have certain reasonable deviations within a certain range, for example: within ±10%, ±5%, ±1% or ±0.5%.

[0080] Some cases are recorded in the examples and comparative examples of the present invention. Among them, the examples show some implementation manners of the present invention. However, this does not mean that the effects of the present invention can only be achieved in these cases. In fact, good anti-aging and anti-wrinkle effects can be achieved at any concentration of each component between the two endpoint values shown in the examples.

[0081] The three comparative examples and several control samples also only list some cases with poor results in the experiments. In addition, many attempts were made during the research and development process, such as screening out components that can better produce synergistic effects from numerous polypeptides, and adjusting the concentration or ratio of each component to make the anti-aging effect more significant. However, the effects of these attempts are not as good as those of Examples 1 to 5, and will not be repeated here.

[0082] The test materials used in the present invention are all common commercial products and can be purchased on the market. Among them:

[0083] The CAS number of blue copper peptide is 49557-75-7.

[0084] The CAS number of acetyl tetrapeptide-5 is 82079-38-3.

[0085] The CAS number of acetyl tetrapeptide-9 is 32974-63-1.

[0086] The CAS number of acetyl hexapeptide-8 is 62806-37-3.

[0087] The CAS number of snake venom peptide is 823202-99-9.

[0088] The CAS number of conopeptide is 936616-33-0.

[0089] It should be understood that in various embodiments of the present application, the size of the sequence number of each process does not mean the order of execution, some or all of the steps can be executed in parallel or in sequence, and the execution order of each process should be determined by its function and internal logic, and should not constitute any limitation on the implementation process of the embodiments of the present application. The present invention is further described below in conjunction with the embodiments:

[0090] Examples 1-5

[0091] Preparation method:

[0092] Add active peptide ingredients, phenoxyethanol and purified water into a beaker and stir evenly to obtain an aqueous phase;

[0093] Tween-80 and Span-80 were compounded in a beaker according to the ratio in the table below, and after being fully stirred, anhydrous ethanol, isopropyl myristate, caprylic acid triglyceride, and squalane were added thereto in sequence, and the mixture was fully stirred at room temperature to obtain an oil phase;

[0094] The oil phase is kept in a stirring state, and the water phase is added to the oil phase at a uniform speed, and the time for adding the water phase is controlled to be 30 minutes. After adding the water phase, high-speed stirring is maintained for another hour to obtain the oil-soluble peptide.

[0095] Table 1. Composition ratio of Examples 1 to 5

[0096]

[0097]

[0098] Embodiment 6-10

[0099] The preparation method is the same as that of Example 1-5. The water-in-oil method is applicable to the encapsulation preparation of various other peptides.

[0100] Table 2. Ingredient ratios of Examples 6 to 10

[0101]

[0102]

[0103] Comparative Examples 1 to 11

[0104] Preparation method:

[0105] Add active peptides, phenoxyethanol and purified water into a beaker and stir evenly to obtain an aqueous phase;

[0106] Tween-80 and Span-80 were compounded in a beaker according to the ratio in the table below, and after being fully stirred, anhydrous ethanol, isopropyl myristate, caprylic acid triglyceride, and squalane were added thereto in sequence, and the mixture was fully stirred at room temperature to obtain an oil phase;

[0107] The oil phase is kept in a stirring state, and the water phase is added to the oil phase at a uniform speed, and the time for adding the water phase is controlled to be 30 minutes. After adding the water phase, high-speed stirring is maintained for another hour to obtain the oil-soluble peptide.

[0108] Table 3. Comparative Examples 1 to 11 composition ratio

[0109]

[0110]

[0111] Comparative Example 12

[0112] Preparation method:

[0113] Add blue copper peptide, acetyl tetrapeptide-5, acetyl tetrapeptide-9, acetyl hexapeptide-8, snake venom peptide, cono peptide, phenoxyethanol and purified water into a beaker, stir evenly to obtain a polypeptide composite aqueous solution.

[0114] Table 4. Preparation method of comparative example 12

[0115]

[0116]

[0117] Effect Detection

[0118] 1. Solubility Experiment

[0119] The oil-soluble peptides obtained in Examples 1-10 and Comparative Examples 1-12 were added to a beaker, and different oily solvents with different HLB values were added thereto, including triglyceride caprylate / caprate, isopropyl myristate, isopropyl palmitate, white oil, jojoba oil, olive oil, squalane, etc.

[0120] The oil-soluble peptides could be rapidly dispersed in the oily solvents but were insoluble in water.

[0121] Table 5. Dissolution of Polypeptide Oil Solution and Aqueous Solution in Different Solvents

[0122] solvent Examples 1 - 10, Comparative Examples 1 - 11 Comparative Example 12 water insoluble dissolved caprylic / capric triglyceride clarified after rapid dispersion and dissolution insoluble mineral oil clarified after rapid dispersion and dissolution insoluble jojoba oil clarified after rapid dispersion and dissolution insoluble olive oil clarified after rapid dispersion and dissolution insoluble squalane clarified after rapid dispersion and dissolution insoluble dioctyl ether clarified after rapid dispersion and dissolution insoluble isotridecyl isononanoate clarified after rapid dispersion and dissolution insoluble coco-caprylate / caprate clarified after rapid dispersion and dissolution insoluble gromwell seed oil clarified after rapid dispersion and dissolution insoluble ethylhexyl palmitate clarified after rapid dispersion and dissolution insoluble

[0123] 2. Stability Investigation

[0124] The content of the oil-soluble peptide prepared in Example 1 should be 95% - 105% of the standard amount.

[0125] Table 6. Stability Tracking of Polypeptide Oil Solution and Aqueous Solution

[0126]

[0127]

[0128] As can be seen from the above table, under the conditions of 4°C - 40°C, the polypeptide water-in-oil microemulsion showed good stability, with no obvious change in the appearance shape. After being placed at 40°C for 2 months, the content remained at 77.64%, while almost no active polypeptide was detected in the aqueous solution; it could also maintain stability for 2 months at room temperature; and it could maintain the stable property without stratification at 4°C.

[0129] Application Example 1

[0130] Prepare an emulsion of anti-aging and anti-wrinkle components, and there is no phenomenon of stratification.

[0131] Table 7. Polypeptide Oil Solution for Preparing Emulsion

[0132]

[0133]

[0134] Preparation Method:

[0135] ①All the materials in Phase A were added to an emulsifying pan, heated and stirred for dissolution;

[0136] ②Except for sodium hyaluronate in Phase B, other materials were added to a beaker, heated and dissolved at 75°C and kept warm;

[0137] ③Keep the temperature difference between phase B and phase A within 10°C. While maintaining the stirring of phase A, slowly add phase B to it. Finally, an anti-aging and anti-wrinkle emulsion is prepared.

[0138] Anti-aging and anti-wrinkle experiment

[0139] Samples: Examples 1 - 5, Comparative Examples 1 - 11. After being prepared by the same method as in Application Example 1, anti-wrinkle experiments are conducted. Comparative Example 12 is unstable in aqueous solution and no anti-wrinkle experiment is carried out.

[0140] Experimental instrument: Visia skin detector

[0141] Test procedure:

[0142] (1) At the first visit, explain the test to the subjects and have them sign the informed consent form.

[0143] (2) The subjects participating in the test are between 50 and 60 years old. For each sample, 5 people are screened and enrolled, ensuring that at least 3 people complete the test. Subjects are not allowed to use skin care products on the morning of the test day. After cleaning the face with a cleansing product, enter the constant temperature and humidity room and sit quietly for 30 minutes. After 30 minutes, screen and conduct instrument tests on the subjects participating in the test according to the test requirements, and record it as the initial value "W0". The test sequence is as follows: VISIACR shooting → Cutometer → PrimosCR shooting.

[0144] (3) After the test is completed, give the subjects instructions on product use. After the subjects listen to the instructions, distribute the products, and the subjects use the test samples continuously at home for 4 weeks. Each time of use, shoot a usage video and return it to the test center. The subjects are visited on-site after using the product continuously for 4 weeks according to the test instructions, and the instrument tests are carried out according to step ②, and are respectively recorded as the test value "W4", and the subjects conduct self-evaluations.

[0145] (4) Confirm the usage of the product at the start of the test and at the end of the return visit.

[0146] Table 8. Changes in the Ra value of wrinkles of the polypeptide combination oil solution at different time points

[0147]

[0148]

[0149] Table 9. Changes in the Ra value of wrinkles of the polypeptide combination oil solution at different time points

[0150]

[0151] The results showed that the microemulsions of Examples 1-5 all had good anti-wrinkle effects, significantly superior to those of each comparative example (p < 0.05), and according to the Bliss formula, calculations showed that the synergy coefficients of Examples 1-5 relative to the comparative examples were all greater than 1. This indicates that the formulations of Examples 1-5 can produce a synergistic effect in terms of anti-wrinkle effects.

[0152] The above are only the preferred embodiments of the present invention. It should be noted that for those of ordinary skill in the art, without departing from the principle of the present invention, several improvements and refinements can be made, and these improvements and refinements should also be regarded as the protection scope of the present invention.

Claims

1. An active peptide composition, which consists of copper peptide, acetyl tetrapeptide-5, acetyl tetrapeptide-9, acetyl hexapeptide-8, syn-ake peptide and conotoxin peptide.

2. The active peptide composition according to claim 1, characterized in that, It consists of the following components in parts by mass:

2. The application of the active peptide composition according to claim 1 or 2 in the preparation of anti-aging and anti-wrinkle products.

4. A microemulsion for anti-aging and anti-wrinkle, which comprises the active peptide composition according to claim 1 or 2 and excipients.

5. The microemulsion according to claim 4, characterized in that, The excipients include at least one of water, emulsifier, cosolvent, oily matrix and preservative; The oily matrix is selected from at least one of isopropyl myristate, isopropyl palmitate, ethylhexyl palmitate, caprylic / capric triglyceride, jojoba oil, olive oil, camellia seed oil, isononyl isononanoate, squalane, cyclohexasiloxane, hydrogenated polyisobutene, light mineral oil; The emulsifier is selected from at least one of tween 80, span 80, tween 20, span 20, sucrose laurate, PEG-7 hydrogenated castor oil, cetyl PEG / PPG-10 / 1 polydimethylsiloxane; The cosolvent is selected from at least one of ethanol, ethylene glycol, propylene glycol, glycerol, n-butanol; The preservative is selected from at least one of phenoxyethanol, sorbic acid, caprylyl glycol, 1,2-hexanediol, p-hydroxyacetophenone.

6. The microemulsion according to claim 4 or 5, characterized in that, It includes the following components in parts by mass: Copper peptide 0.01% - 0.05%, acetyl tetrapeptide-5 0.02% - 0.04%, acetyl tetrapeptide-9 0.01% - 0.03%, acetyl hexapeptide-8 0.02% - 0.05%, syn-ake peptide 0.05% - 0.06%, conotoxin peptide 0.001% - 0.002%, tween-80 14.6% - 17%, span-80 3% - 5.4%, absolute ethanol 4% - 5%, isopropyl myristate 40% - 55%, caprylic / capric triglyceride 5% - 20%, squalane 5% - 8%, phenoxyethanol 0.1%, and the balance is water.

7. The preparation method of the microemulsion according to any one of claims 4 - 6, which comprises: Dissolving the active peptide composition according to claim 1 or 2 and the preservative in water to obtain an aqueous phase; Mixing the emulsifier, cosolvent and oily matrix to obtain an oil phase; Subjecting the oil phase and the aqueous phase to high-speed stirring to obtain the microemulsion.

8. A cosmetic for anti-aging and wrinkle removal, characterized in that, It includes the active peptide composition according to claim 1 or 2 or the microemulsion according to any one of claims 4 - 6.

9. The cosmetic according to claim 8, characterized in that, It includes the microemulsion according to any one of claims 4 - 6, active substances, oils, humectants, sodium chloride and water; The active substances are selected from at least one of vitamin E, retinol, bisabolol, arbutin, niacinamide, potassium methoxysalicylate, glabridin, asiaticoside, honeysuckle extract; The oils are selected from at least one of octyl silicone oil BT-6034, cetyl PEG / PPG-10 / 1 polydimethylsiloxane, petrolatum; The humectants are selected from at least one of glycerol, butanediol, 1,2-hexanediol, hyaluronic acid.

10. The cosmetic according to claim 8 or 9, characterized in that, Among them, The mass fraction of the microemulsion according to any one of claims 4 - 6 is 10% - 20%.

11. The preparation method of the cosmetic according to any one of claims 8 - 10, which comprises: Mix the microemulsion, active substance, and oil and fat described in any one of claims 4 to 6 to obtain Phase A; Mix water and a humectant to obtain Phase B; Mix Phase A and Phase B to obtain the cosmetic.

12. An anti-aging and anti-wrinkle method, which includes applying the composition described in claim 1 or 2, the microemulsion described in any one of claims 4 to 6, or the cosmetic described in any one of claims 8 to 10 on the skin surface.

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