Structural repair intelligent polypeptide anti-aging composition as well as preparation method and application thereof

Abstract

The invention belongs to the field of cosmetic compositions, and particularly relates to a structure-repairing intelligent polypeptide anti-aging composition as well as a preparation method and application thereof. The composition comprises repair polypeptide, efficacy optimization polypeptide and a system synergistic composition, and the mass ratio of the repair polypeptide to the efficacy optimization polypeptide to the system synergistic composition is (1-8): (3-16): (3.5-13). The repairing polypeptide comprises acetyl hexapeptide-8, palmitoyl pentapeptide-5, snake venom peptide and arginine / lysine polypeptide; the efficacy optimization polypeptide is acetyl tetrapeptide-2 and palmitoyl tripeptide-5; the system synergistic composition is prepared from nicotinamide, hydroxypropyl tetrahydropyrantriol and a Thermus thermophilus fermentation product. Through multi-channel synergistic anti-aging, the problems of single efficacy, poor synergism and low bioavailability in the prior art are solved, tests show that the effects of reducing wrinkles, improving elasticity and the like are remarkably superior to those of existing products, and the composition can be used for preparing cosmetics.

Description

TECHNICAL FIELD

[0001] The present application belongs to the field of cosmetic compositions, and in particular relates to a structure repair intelligent polypeptide anti-aging composition and its preparation method and application. BACKGROUND

[0002] Skin aging is a complex multi-dimensional change process in the natural physiological process of the human body, involving multi-pathway, multi-target damage and functional decline of skin tissue from the cellular level to the macroscopic structure. Specifically, it is characterized by core problems such as deepening of dynamic expression lines caused by imbalance of neuromuscular signal transmission, loss of skin elasticity caused by degradation of dermal matrix components, and insufficient skin nutrition supply and metabolic waste accumulation caused by dysfunction of microcirculation system. With the continuous upgrading of consumers' demand for anti-aging skin care, active polypeptides have become the core active ingredient in the current anti-aging cosmetic field due to their high biological activity, strong targeting and low irritation. Among them, acetyl hexapeptide-8 and palmitoyl tripeptide-5, as classic polypeptide ingredients, have shown clear efficacy in inhibiting nerve signals and stimulating collagen synthesis, respectively, and are widely used in various anti-aging skin care products, promoting the upgrading of anti-aging technology from traditional ingredients to bioactive ingredients.

[0003] However, the existing anti-aging technology based on active polypeptides still has certain technical defects, which is difficult to meet the needs of consumers for comprehensive, efficient and long-lasting anti-aging. Existing products mostly use single polypeptide or simple compounding, which only plays a role in a certain pathway of skin aging, such as relying only on acetyl hexapeptide-8 to improve dynamic lines, or only repairing dermal structure through palmitoyl tripeptide-5, which cannot realize the synergistic intervention of multiple pathways such as nerve signal, matrix repair and microcirculation regulation, resulting in one-sided anti-aging effect and difficulty in solving the overall problem of skin aging. Conventional polypeptide compounding is mostly a simple addition of effects, without considering the correlation and interaction between different polypeptide ingredients. Some compounding schemes even have efficacy interference due to the conflict of physicochemical properties or competition of action targets, which cannot form a synergistic effect of 1+1>2, violating the core demand of anti-aging technology for ingredient synergy. At the same time, polypeptide ingredients have the natural bottleneck of transdermal absorption difficulty due to their large molecular weight and strong hydrophilicity, and are easily decomposed by skin surface aminopeptidases and endopeptidases, resulting in a much lower effective concentration in the target tissue than the added concentration.

[0004] Based on the above defects of the existing technology, there is an urgent need in the art for a skin anti-aging composition that can overcome the problems of single efficacy, poor synergy and low bioavailability, achieve multi-level intervention on multiple pathways of skin aging through systematic ingredient design and mechanism innovation, and achieve efficient and long-lasting anti-aging effect, in order to fill the gap in the overall and efficient anti-aging technology. SUMMARY

[0005] In order to solve the above technical problems, the first aspect of the present application provides a structure repair intelligent polypeptide anti-aging composition, which is prepared from a repair polypeptide, an efficacy optimization polypeptide and a system synergistic composition; the repair polypeptide comprises a nerve signal inhibition dipeptide, a palmitoyl pentapeptide-5 and an arginine / lysine polypeptide.

[0006] As an implementable case, the mass ratio of the repair polypeptide, the efficacy optimization polypeptide and the system synergistic composition is (1-8):(3-16):(3.5-13).

[0007] As an implementable case, the nerve signal inhibition dipeptide comprises acetyl hexapeptide-8 and snake venom peptide (dipeptide diaminobutyryl benzyl amide diacetate).

[0008] As an implementable case, the efficacy optimization polypeptide comprises acetyl tetrapeptide-2 and palmitoyl tripeptide-5.

[0009] Further, the mass ratio of the acetyl tetrapeptide-2 and the palmitoyl tripeptide-5 is (1-8):(2-8).

[0010] Acetyl hexapeptide-8: As a key component of the nerve signal inhibition dipeptide, by specifically inhibiting the expression and activity of synaptosomal-associated protein 25 (SNAP-25), it blocks the signal transmission pathway at the neuromuscular junction, reduces the release of acetylcholine, and thus reduces the frequency and intensity of facial muscle overcontraction. It is one of the core efficacy sources of the composition for improving dynamic expression lines caused by excessive conduction of neuromuscular signals in skin aging, and it realizes rapid and accurate intervention, and forms a synergistic effect with snake venom peptide.

[0011] Snake venom peptide: As another component of the nerve signal inhibition dipeptide, by simulating the action mode of conotoxin, it competitively binds to the nicotinic acetylcholine receptor at the neuromuscular junction, further blocks the transmission of nerve signals to muscles, and its target is different from that of acetyl hexapeptide-8, forming a double blocking mechanism. At the same time, snake venom peptide and acetyl hexapeptide-8 synergistically act to make up for the limitations of single polypeptide in inhibiting nerve signals, significantly improve the smoothing speed and high efficiency of dynamic lines, and solve the one-sided defects of single polypeptide anti-aging pathway in the prior art.

[0012] Palmitoyl pentapeptide-5: an important component of dermal matrix remodeling dipeptide, by activating the activity of skin fibroblasts, promote the synthesis and cross-linking of dermal-epidermal junction (DEJ) related structural proteins in the dermal layer, enhance the structural stability and integrity of DEJ. DEJ is the key structure connecting the dermal layer and the epidermal layer, its degradation will lead to skin nutrition transmission blocked, decreased elasticity, palmitoyl pentapeptide-5 by repairing DEJ, for the overall reconstruction of dermal matrix provides a structural basis, with palmitoyl tripeptide-5 form matrix synthesis-connection synergistic reinforcement, realize the overall repair of dermal layer structure.

[0013] Palmitoyl tripeptide-5: as another component of dermal matrix remodeling dipeptide, by simulating the signal peptide sequence of human body itself, activate the TGF-β / Smad signaling pathway in fibroblasts, directly promote the synthesis of collagen and glycosaminoglycan, while inhibit the activity of matrix metalloproteinase, reduce collagen degradation. For skin laxity, loss of elasticity caused by degradation of dermal matrix in skin aging, supplement the structural material of dermal layer, with palmitoyl pentapeptide-5 synergistic construction of dermal matrix synthesis-connection layer strengthening complete repair pathway, is the core raw material of the composition to improve skin firmness and elasticity.

[0014] Acetyl tetrapeptide-2: as the only microcirculation regulating peptide in the system, by inhibiting the activity of angiotensin converting enzyme, reduce the generation of angiotensin Ⅱ, thereby dilate the capillary vessels in the dermal layer of skin, improve the perfusion capacity of capillary vessels, promote blood flow. At the same time, acetyl tetrapeptide-2 solves the problem of insufficient nutrition and accumulation of metabolic waste caused by microcirculation disorder in skin aging, provides sufficient oxygen and nutrients for dermal fibroblasts, and accelerates the excretion of metabolic waste, indirectly provides a good microenvironment for the dermal repair of palmitoyl tripeptide-5 and palmitoyl pentapeptide-5, is the key supplement to realize multi-pathway synergistic anti-aging.

[0015] Arginine / lysine polypeptide: as the core ingredient of matrix efficiency optimization layer, it plays the dual functional carrier role of polypeptide protection and transdermal delivery. Arginine / lysine polypeptide has positive charge due to its rich content of arginine and lysine, which can preferentially combine with the negative degrading enzymes on the surface of skin, inhibit the combination of these enzymes with the polypeptides in the core active layer by competitive inhibition, reduce the probability of inactivation of core polypeptides by enzymolysis, thereby avoiding the failure of core active polypeptides before reaching the target site, significantly prolonging their half-life in the skin. At the same time, as a typical cell-penetrating peptide, its special amino acid sequence can disturb the lipid bilayer structure of the stratum corneum of skin, temporarily open the hydrophilic channel, and its positive charge can interact with the negative area on the surface of skin cell membrane by electrostatic interaction, promote palmitoyl tripeptide-5 and acetyl tetrapeptide-2 to enter the dermal layer by endocytosis or direct penetration, thereby breaking through the bottleneck of transdermal absorption of polypeptides due to their large molecular weight and strong hydrophilicity, significantly improving the effective concentration of core active layer polypeptides in the dermal layer.

[0016] The five polypeptides of acetyl hexapeptide-8, a snake venom peptide, palmitoyl pentapeptide-5, palmitoyl tripeptide-5 and acetyl tetrapeptide-2 can effectively solve the problem of one-sidedness of the anti-aging pathway in the prior art in view of the three core pathways of skin aging, namely, nerve signal, dermal structure and microcirculation. The arginine / lysine polypeptide of the matrix efficiency optimization layer plays a role of escorting and protecting. Through the dual mechanisms of enzyme degradation protection and transdermal absorption promotion, the technical bottleneck of low bioavailability of core polypeptides is broken, and the efficacy of the core polypeptides is effectively ensured. The polypeptide components of the two layers synergize with each other to form an intelligent anti-aging system with precise target and controllable efficiency, which becomes a technical effect for realizing multi-level and high-efficiency anti-aging.

[0017] As an implementable case, the system synergistic composition comprises nicotinamide, hydroxypropyl tetrahydropyrane triol and Thermus Thermophillus fermentation product.

[0018] Further, the mass ratio of the nicotinamide, hydroxypropyl tetrahydropyrane triol and Thermus Thermophillus fermentation product is (2-5):(1-4):(0.5-4).

[0019] Nicotinamide: As a direct precursor of nicotinamide adenine dinucleotide (NAD⁺, a key coenzyme for cellular energy metabolism), it can inhibit abnormal proliferation of keratinocytes, promote ordered differentiation of the stratum corneum, improve the integrity of the skin barrier structure and reduce trans-epidermal water loss. In view of the process of repairing the dermal matrix by palmitoyl tripeptide-5 and palmitoyl pentapeptide-5 in the core layer, nicotinamide can enhance the energy level of fibroblasts and their ability to synthesize collagen and glycosaminoglycans. At the same time, by optimizing the barrier of the stratum corneum and reducing the stimulation of the external environment to the skin, it provides a stable cellular metabolic environment for the core polypeptides to play a role, indirectly amplifying the anti-aging effect of dermal repair and nerve signal inhibition. It is the core source of energy supply in the system synergistic layer.

[0020] Hydroxypropyl tetrahydropyran triol (bovine): As a small molecule xylose derivative, hydroxypropyl tetrahydropyran triol can penetrate the stratum corneum to reach the dermis, regulate the TGF-β / Smad signaling pathway and the Wnt / β-catenin signaling pathway by activating the receptors on the surface of fibroblasts, on the one hand, promote fibroblasts to synthesize glycosaminoglycan and proteoglycan, fill the interstitial space of the dermis, and enhance the fullness of the skin; on the other hand, strengthen the structural stability of the DEJ, and promote the ordered arrangement of laminin and collagen fibers in the DEJ region. At the same time, hydroxypropyl tetrahydropyran triol and palmitoyl pentapeptide-5 in the core layer strengthen the DEJ and palmitoyl tripeptide-5 to form collagen, and provide structural support for the core polypeptide to repair the dermal structure, solve the problem of lack of environmental cooperation in the matrix synthesis of single polypeptide to repair the dermis; at the same time, the glycosaminoglycan synthesized by it can improve the water retention capacity of the skin, and together with niacinamide, improve the skin moisture and enhance the elasticity and firmness of the skin.

[0021] Thermus thermophilus fermentation product: The thermus thermophilus fermentation product is rich in high-temperature resistant DNA repair enzymes, heat shock proteins, amino acids, small molecule peptides and other nutrients; among them, the DNA repair enzyme can recognize and repair the DNA single-strand break, pyrimidine dimer and other defects caused by ultraviolet rays and free radicals in skin cells, and reduce cell apoptosis; the heat shock protein can help damaged proteins to fold correctly and maintain protein homeostasis in cells. In view of the process of core polypeptide intervention in skin aging, the thermus thermophilus fermentation product can repair DNA damage of skin cells, maintain protein homeostasis, improve cell survival ability and self-repair efficiency, and avoid the reduction of efficacy caused by low cell activity when the core polypeptide acts.

[0022] The second aspect of the present application provides a preparation method of the structure repair intelligent polypeptide anti-aging composition, comprising: mixing the repair polypeptide, the efficacy optimization polypeptide and the system synergistic composition, and adjusting the pH of the system to be weakly acidic, to obtain the structure repair intelligent polypeptide anti-aging composition.

[0023] As an implementable case, the pH is 5.5-6.5.

[0024] The second aspect of the present application provides the application of the structure repair intelligent polypeptide anti-aging composition, which is applied in the preparation of cosmetics.

[0025] In the application of the structure repair intelligent polypeptide anti-aging composition in the preparation of cosmetics, functional additives can also be reasonably added according to the actual performance needs of the product, including but not limited to water, humectants, thickening agents, emulsifiers and preservatives.

[0026] Beneficial effects (I) The polypeptide anti-aging composition provided by the present application constructs a three-dimensional action network of nerve signal inhibition, dermal matrix remodeling, and microcirculation regulation through a core action layer, breaks through the limitations of single-path intervention in the prior art, can simultaneously improve multiple types of aging problems such as dynamic wrinkles, skin relaxation, and insufficient nutrition supply, realizes comprehensive coverage of the core dimensions of skin aging, and has more overall and systematic anti-aging efficacy.

[0027] (II) The arginine / lysine polypeptide in the present application has the dual functions of enzyme degradation protection and transdermal enhancement, can reduce the inactivation of the core polypeptide by competitively binding to skin degradation enzymes, prolong the half-life of the core polypeptide, and can also disturb the lipid structure of the stratum corneum, promote the transdermal absorption of the core polypeptide by means of electrostatic action, break through the technical bottlenecks of polypeptide transdermal difficulty and easy degradation from two dimensions of reducing loss and increasing absorption, significantly improve the effective concentration and action efficiency of the core polypeptide, and ensure that the theoretical efficacy is realized.

[0028] (III) The nicotinamide, hydroxypropyl tetrahydropyrane triol, and thermophilic thermus fermentation product in the system synergistic composition in the present application form a synergy, provide a suitable cellular metabolic environment, structural support foundation, and healthy cell state for the action of the core polypeptide, can not only enhance the ability of fibroblasts to synthesize collagen and glycosaminoglycans, but also reduce external interference and cell damage, amplify the anti-aging efficacy of the core component from the environmental level, and realize a synergistic effect of 1+1>2.

[0029] (IV) The acetyl hexapeptide-8 and snake venom peptide in the present application can quickly inhibit neuromuscular signals to achieve immediate smoothing of dynamic wrinkles; at the same time, palmitoyl tripeptide-5, palmitoyl pentapeptide-5, and the hydroxypropyl tetrahydropyrane triol of the system synergistic layer can continuously promote the synthesis and structure repair of the dermal matrix, and acetyl tetrapeptide-2 improves microcirculation to maintain long-term healthy state of the skin, forming an anti-aging chain of immediate improvement, medium-term consolidation, and long-term repair, which not only meets the immediate needs of consumers for quick results, but also realizes long-term intervention of skin aging, covers different stages of anti-aging demands, and improves product use value and user satisfaction. DETAILED DESCRIPTION

[0030] Example 1 The preparation raw materials of the structure repair intelligent polypeptide anti-aging composition provided in this example are shown in Table 1.

[0031] Table 1

[0032] In the examples 1 and comparative examples 1-3, the iron peptide plus includes acetyl hexapeptide-8, palmitoyl pentapeptide-5, acetyl hexapeptide-3, arginine / lysine polypeptide, ethylhexylglycerin, 1,2-hexanediol and water. The preparation raw materials of the iron peptide plus include, by mass percentage, 0.02-0.2% acetyl hexapeptide-8, 0.02-0.2% palmitoyl pentapeptide-5, 0.02-0.3% acetyl hexapeptide-3, 0.001-0.2% arginine / lysine polypeptide, 0.05-0.15% ethylhexylglycerin, 0.1-1.5% 1,2-hexanediol, 97.63-99.789% water, and the sum of the raw materials is 100%.

[0033] The preparation method of the structural repair intelligent polypeptide anti-aging composition in example 1 is to mix the repair polypeptide, the efficacy optimization polypeptide and the system synergistic composition, and adjust the pH of the system to 6, so as to obtain the structural repair intelligent polypeptide anti-aging composition. The structural repair intelligent polypeptide anti-aging composition can be applied to the preparation of cosmetics.

[0034] The raw material information involved in example 1 and comparative example 1-4 of the present application is shown in table 2.

[0035] Table 2

[0036] The example 1 of the present application is the optimal implementation case, which includes all the preparation raw materials.

[0037] The preparation raw materials in comparative example 1 only include the iron peptide plus. The difference between comparative example 2 and example 1 is that the raw materials do not include the system synergistic composition.

[0038] The difference between comparative example 3 and example 1 is that the raw materials do not include the efficacy optimization polypeptide.

[0039] The comparative example 4 is a conventional polypeptide composition, which only includes acetyl hexapeptide-8, palmitoyl pentapeptide-5 and acetyl hexapeptide-3.

[0040] Performance evaluation Test object: the compositions prepared in example 1 and comparative examples 1-4.

[0041] Test method: human efficacy evaluation (double-blind, half-face control), lasting for 8 weeks. Image analysis (wrinkle), mechanical test (elasticity), moisture test (hydration-indirectly reflecting barrier health), and the experimental results are shown in table 3.

[0042] Table 3

[0043] Example 1 showed the best effect in all evaluation indexes such as wrinkle depth reduction, skin elasticity improvement, tightness improvement, water content improvement and subject satisfaction, while Comparative Example 1 showed only 40%-50% of the effect of Example 1, Comparative Example 2 showed the worst effect and was lower than Comparative Example 1, and Comparative Example 3 showed an effect better than Comparative Example 1 but significantly lower than Example 1. The above comparison clearly proves that the integrity of the repair polypeptide, the efficacy optimization polypeptide and the system synergistic composition is the prerequisite for achieving excellent anti-aging effect, and the absence of any layer or the incomplete core layer will lead to a significant decline in the final effect, highlighting the necessity of the synergistic existence of each layer.

[0044] The comparison between Comparative Example 1 and Example 1 shows that the core polypeptide without the efficacy optimization polypeptide and the system synergistic composition will have a significant discount in effect due to fast degradation, low absorption and poor action environment, which confirms the supporting role of the non-core layer on the landing of the core polypeptide effect; the results of Comparative Example 2 show that the Anagrand plus itself has no independent anti-aging effect and must rely on the complete and multi-target core action layer to play its value, which clearly defines the core position of the core layer; the test data of Comparative Example 3 further highlights the effect of the efficacy optimization polypeptide; even with the synergistic action of the system synergistic layer and the core layer, the absence of the optimization layer will still lead to the inability of the core polypeptide to efficiently reach the action target, and the theoretical effect is severely limited, which confirms that it is the key link to activate the core effect.

Claims

1. A structural repair intelligent polypeptide anti-aging composition, characterized in that, The raw materials for preparation include repair peptides, efficacy-enhancing peptides, and system synergistic compositions; The repair peptides include a neurotransmitter inhibitory dipeptide, palmitoyl pentapeptide-5, and an arginine / lysine peptide.

2. The structural repair intelligent polypeptide anti-aging composition according to claim 1, characterized in that, The mass ratio of the repair peptide, the efficacy-optimizing peptide and the system synergistic composition is (1-8):(3-16):(3.5-13).

3. The structural repair intelligent polypeptide anti-aging composition according to claim 1, characterized in that, The aforementioned neurosignal-inhibiting dipeptide includes acetyl hexapeptide-8 and snake venom peptide.

4. The structural repair intelligent polypeptide anti-aging composition according to claim 1, characterized in that, The efficacy-enhancing peptides include acetyl tetrapeptide-2 and palmitoyl tripeptide-5.

5. The structural repair intelligent polypeptide anti-aging composition according to claim 4, characterized in that, The mass ratio of acetyl tetrapeptide-2 to palmitoyl tripeptide-5 is (1-8):(2-8).

6. The structural repair intelligent polypeptide anti-aging composition according to claim 1, characterized in that, The system synergistic composition comprises nicotinamide, hydroxypropyl tetrahydropyrantriol, and thermophilic bacteria fermentation products.

7. The structural repair intelligent polypeptide anti-aging composition according to claim 6, characterized in that, The mass ratio of nicotinamide, hydroxypropyltetrahydropyrantriol and thermophilic bacteria fermentation product is (2-5):(1-4):(0.5-4).

8. A method for preparing a structural repair intelligent polypeptide anti-aging composition according to any one of claims 1-7, characterized in that, It includes the following steps.

9. Mix the repair peptides, efficacy-optimizing peptides, and system synergistic composition, and adjust the pH of the raw material system to a weakly acidic state to obtain the structure-repairing intelligent peptide anti-aging composition.

10. The method for preparing the structural repair intelligent polypeptide anti-aging composition according to claim 8, characterized in that, The pH of the raw material system is 5.5-6.

5.

11. The application of a structural repair intelligent polypeptide anti-aging composition according to any one of claims 1-7, characterized in that, It is used in the preparation of cosmetics.

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