Whitening, wrinkle-removing and anti-aging pterostilbene liposome composition, preparation method thereof, cosmetic and preparation method thereof
The problem of poor stability of rosalis in cosmetics is solved through liposome wrapping technology, which improves its permeability and bioavailability in the skin, and achieves more significant whitening, wrinkle removal and anti-aging effects.
Patent Information
- Application Number
- CN202411090076.8
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2024-08-09
- Publication Date
- 2025-01-10
Smart Images

Figure CN119280083A_ABST
Abstract
Description
Technical Field
[0001] The invention belongs to the technical field of skin whitening compositions, and relates to a cosmetic, in particular to a whitening, wrinkle-removing and anti-aging pterostilbene liposome composition and a preparation method thereof, and a cosmetic and a preparation method thereof. Background Art
[0002] Pterostilbene extract has been shown to significantly inhibit melanin production, and its inhibitory effect on melanin production is achieved by intervening in the activity of key enzymes such as tyrosinase. At the same time, pterostilbene may also affect the activity of melanin cells and the pigmentation process, helping to reduce spots and improve skin tone uniformity.
[0003] In addition, pterostilbene can reduce wrinkles and fine lines and improve skin hydration and elasticity. The presence of methoxy groups in pterostilbene increases its lipophilicity and membrane permeability, and this property increases its molecular activity. The Nrf2 signaling pathway plays an important regulatory role in cells and can regulate the antioxidant response in cells. Pterostilbene promotes the expression of antioxidant enzymes in cells by activating the Nrf2 signaling pathway, improves the antioxidant capacity of cells, and effectively removes a variety of free radicals, thereby reducing the damage of oxidative stress to cells. By activating the nuclear factor erythroid 2-related factor 2 (Nrf2) signaling pathway, pterostilbene successfully removes several free radicals, effectively reduces oxidative stress, and thus enhances the antioxidant function of cells.
[0004] Wrinkles and fine lines are common problems that occur with aging and skin damage. Pterostilbene can also reduce the appearance of wrinkles and fine lines, making the skin smoother and more elastic by stimulating collagen synthesis, increasing elastin content, and promoting cell regeneration. In addition, the presence of methoxy groups in pterostilbene not only increases its lipophilicity and membrane permeability, but also may affect its interaction with cell membranes, thereby enhancing its activity within cells. This enhanced activity helps pterostilbene interact more effectively with biomolecules within cells, thereby exerting its antioxidant and anti-aging effects.
[0005] However, pterostilbene has the defects of poor stability and low bioavailability. Specifically, pterostilbene is unstable in light and air, and its hydroxyl group is easily oxidized, thus losing its efficacy; pterostilbene is highly lipid-soluble but very poorly water-soluble, so its bioavailability is relatively low.
[0006] In view of this, there is an urgent need to design a new skin improving composition so as to overcome at least part of the above-mentioned defects of the existing skin improving composition. Summary of the invention
[0007] The invention provides a whitening, wrinkle-removing and anti-aging pterostilbene liposome composition and a preparation method thereof, cosmetics and a preparation method thereof, and uses liposome encapsulation technology to solve the problems of easy discoloration, poor solubility, easy crystallization and the like of pterostilbene in cosmetic formulas; by encapsulating active ingredients such as nicotinamide, tetrahydrocurcumin and pterostilbene with liposomes, it is prevented that the active ingredients are easily degraded by factors such as light, oxygen and heat, and the stability of the active ingredients in the cosmetics is improved, so as to better exert their efficacy.
[0008] To solve the above technical problem, according to one aspect of the present invention, the following technical solution is adopted:
[0009] A whitening, wrinkle-removing and anti-aging pterostilbene liposome composition comprises: 0.5-10 parts by weight of nicotinamide, 0.01-5 parts by weight of tetrahydrocurcumin, 0.01-5 parts by weight of pterostilbene and 1-30 parts by weight of lecithin.
[0010] As an embodiment of the present invention, the whitening, wrinkle-removing and anti-aging pterostilbene liposome composition further comprises 1 to 15 parts by weight of an emulsifier and / or an emulsifier aid.
[0011] As an embodiment of the present invention, the whitening, wrinkle-removing and anti-aging pterostilbene liposome composition comprises: 1 to 10 parts by weight of niacinamide, 1 to 3 parts by weight of tetrahydrocurcumin, 1 to 5 parts by weight of pterostilbene, 1 to 30 parts by weight of lecithin and 1 to 15 parts by weight of cholesterol.
[0012] As an embodiment of the present invention, the whitening, wrinkle-removing and anti-aging pterostilbene liposome composition comprises: 6 parts by mass of niacinamide, 1 part by mass of tetrahydrocurcumin, 2 parts by mass of pterostilbene, 8 parts by mass of lecithin and 3 parts by mass of cholesterol.
[0013] According to another aspect of the present invention, the following technical solution is adopted: a cosmetic comprising the above-mentioned whitening, wrinkle-removing and anti-aging pterostilbene liposome composition.
[0014] As an embodiment of the present invention, the cosmetic is an essence lotion, an emulsion, a face cream, a freeze-dried powder or a skin care lotion.
[0015] As an embodiment of the present invention, the cosmetic further comprises a water phase component, an oil phase component, a pH adjuster and a third composition;
[0016] The water phase component includes a thickener, a first skin conditioning agent and a first moisturizer; the oil phase component includes a second skin conditioning agent, an emulsifier and an excipient; and the third composition includes a fragrance, a preservative and a second moisturizer.
[0017] As an embodiment of the present invention, the thickener includes xanthan gum and carbomer, the first skin conditioning agent includes sodium hyaluronate and allantoin, and the first moisturizing agent includes glycerin and jojoba oil;
[0018] The second skin conditioning agent includes cetyl alcohol, the emulsifier includes cetearyl glucoside and cetearyl alcohol, and the excipient includes squalane;
[0019] The pH adjuster includes arginine; the fragrance includes essence; the preservative includes phenoxyethanol; and the second moisturizer includes ethylhexylglycerin.
[0020] According to another aspect of the present invention, the following technical scheme is adopted: a method for preparing a whitening, wrinkle-removing and anti-aging pterostilbene liposome composition, the preparation method comprising:
[0021] Step S1, dissolving 0.5-10 parts by weight of nicotinamide in water to obtain a phase A mixed solution; dissolving 0.01-5 parts by weight of tetrahydrocurcumin and 0.01-5 parts by weight of pterostilbene in oil to obtain a phase B mixed solution;
[0022] Step S2, adding an emulsifier to the phase B mixed solution and 1 to 30 parts by weight of lecithin to obtain a phase C mixed solution;
[0023] Step S3, extracting an appropriate amount of phase C mixed solution, injecting an appropriate amount of phase A mixed solution, to obtain a phase D mixed solution; the mass fraction of nicotinamide in the phase D mixed solution is 0.5-10, the mass fraction of tetrahydrocurcumin is 0.01-5, the mass fraction of pterostilbene is 0.01-5, and the mass fraction of lecithin is 1-30;
[0024] Step S4, drying the phase D mixed solution to obtain the whitening, wrinkle-removing and anti-aging pterostilbene liposome composition.
[0025] As an embodiment of the present invention, in step S1, the oil includes at least one of C13-C16 alkane, C5-19 alkane, semi-squalane, and caprylic capric triglyceride;
[0026] In step S2, the emulsifier includes at least one of cholesterol, polysorbate 40, polysorbate 60, and polysorbate 80;
[0027] In the step S3, the extracted phase B mixed solution is injected into the stirred phase A mixed solution at a rate of 2 to 5 μl / min to obtain a phase C mixed solution;
[0028] In the step S4, the phase C mixed solution is concentrated under reduced pressure at a pressure of ≤70 kPa, then ultrasonicated, and frozen and dried at a temperature of -40°C to -45°C to obtain a whitening, wrinkle-removing and anti-aging pterostilbene liposome composition.
[0029] According to another aspect of the present invention, the following technical solution is adopted: a method for preparing the above-mentioned cosmetics, the preparation method comprising:
[0030] Step a, placing water in a container with a stirring device and stirring, adding the aqueous phase components after fully wetting and mixing them into the water, stirring them fully until they are completely dissolved, and heating them to 75-80°C;
[0031] Step b, mixing the oil phase components, heating to 75-80°C, and stirring until completely dissolved;
[0032] Step c, adding the mixture obtained in step b to the aqueous phase obtained in step a, stirring at 200-400 rpm and homogenizing at 2000-4000 rpm for 10-30 minutes;
[0033] Step d, adding a pH adjuster, stirring at 200-400 rpm and homogenizing at 2000-4000 rpm for 10-30 minutes; stirring and cooling to a set temperature (such as 30° C. to 50° C., such as 45° C.);
[0034] Step e, adding the third composition, stirring at 200-400 rpm and homogenizing at 2000-4000 rpm for 10-50 minutes, and sterilizing by filtration;
[0035] Step f: after the temperature drops to 35-38° C., add the above-mentioned whitening, wrinkle-removing and anti-aging pterostilbene liposome composition, stir at 200-400 rpm and homogenize at 2000-4000 rpm for 5-20 minutes to obtain the cosmetics.
[0036] The beneficial effects of the present invention are as follows: the whitening, wrinkle-removing and anti-aging pterostilbene liposome composition and its preparation method, the cosmetics and its preparation method proposed by the present invention use liposome encapsulation technology to solve the problems of easy discoloration, poor solubility and easy crystallization of pterostilbene in cosmetic formulas; by using liposomes to encapsulate active ingredients such as nicotinamide, tetrahydrocurcumin and pterostilbene, it is avoided that they are easily affected by factors such as light, oxygen and heat and thus degraded, and the stability of the active ingredients in the cosmetics is improved, so as to better exert their efficacy.
[0037] Because the tiny vesicle structure of liposomes is similar to that of the skin surface, they can interact with the skin more easily and promote the penetration and absorption of active ingredients. By encapsulating active ingredients, their permeability and bioavailability in the skin are improved, thereby better exerting their efficacy.
[0038] In one usage scenario of the present invention, the present invention adjusts the usage ratio of the three ingredients, and the ratio of niacinamide (0.5-10%), tetrahydrocurcumin (0.01-5%), and pterostilbene (0.01-5%) is 6-10:1:2-5, which can achieve the best whitening, anti-wrinkle and anti-aging effects.
[0039] Niacinamide is a vitamin B3 derivative that can promote the metabolism of skin cells, increase the skin's barrier function, and regulate skin pigmentation, thus having whitening, anti-aging and moisturizing effects. Tetrahydrocurcumin is a curcumin derivative that can inhibit the synthesis of melanin, reduce the formation of spots and wrinkles, and has an antioxidant effect. Pterostilbene is a natural plant extract that can promote the synthesis of collagen in the skin and increase skin elasticity and firmness. BRIEF DESCRIPTION OF THE DRAWINGS
[0040] Figure 1 The present invention is a flowchart of a method for preparing pterostilbene liposomes according to an embodiment of the present invention.
[0041] Figure 2 This is a schematic diagram of the effect of the niacinamide anti-aging efficacy experiment in one embodiment of the present invention.
[0042] Figure 3 This is a schematic diagram of the effect of the experiment on the anti-jaundice and anti-aging efficacy of pterostilbene in one embodiment of the present invention. DETAILED DESCRIPTION
[0043] The preferred embodiments of the present invention are described in detail below with reference to the accompanying drawings.
[0044] In order to further understand the present invention, preferred embodiments of the present invention are described below in conjunction with examples. However, it should be understood that these descriptions are only for further illustrating the features and advantages of the present invention, rather than limiting the claims of the present invention.
[0045] The description in this section is only for several typical embodiments, and the present invention is not limited to the scope of the embodiments. The same or similar prior art means and some technical features in the embodiments are mutually replaced within the scope of the present invention.
[0046] The description of the steps in each embodiment in the specification is only for the convenience of explanation, and the implementation method of the present application is not limited by the order of implementation of the steps.
[0047] Pterostilbene extract has a significant inhibitory effect on melanin production, can reduce spots and improve skin tone uniformity, can also reduce wrinkles and fine lines, and improve skin hydration and elasticity. Pterostilbene is an oil-soluble ingredient that is easily faded by light and heat. Pterostilbene has whitening and anti-aging effects, can inhibit melanin, resist ultraviolet rays, anti-inflammatory and anti-glycation, and is an excellent natural active ingredient for whitening and anti-aging. Tetrahydrocurcumin has a strong activity in inhibiting tyrosinase and niacinamide has anti-wrinkle, oil-control and whitening effects, both of which are soluble in water. The combination of the three can obtain a new whitening combination, which reduces the poor color stability of pterostilbene and the low solubility of tetrahydrocurcumin, and increases its transdermal efficacy through encapsulation technology.
[0048] Nicotinamide can also inhibit the synthesis of melanin and reduce the production of spots and freckles. It works by inhibiting the activity of tyrosinase. Tyrosinase is a key enzyme in the synthesis of melanin. It participates in the activation process of polyphenol oxidase, so that tyrosine is oxidized to dopa and dopaquinone, and then synthesizes melanin. Nicotinamide can block this process, thereby reducing the formation of melanin. Nicotinamide can also promote the synthesis of collagen in the body. Collagen is the most important structural protein in the skin, which can provide support, elasticity and firmness. With age, the synthesis of collagen gradually decreases, resulting in sagging skin and wrinkles. Nicotinamide improves this problem by promoting the process of collagen synthesis, making the skin firmer and smoother. The main changes in skin aging: decreased skin elasticity; deterioration of structure, wrinkles; slower epidermal renewal; decreased protein and collagen synthesis rate; the most important cell metabolic coenzyme is depleted with age. When nicotinamide is cultured with fibroblasts from the elderly, it can repair the level of NADH / NADPH; therefore, nicotinamide can resist many changes of age.
[0049] Tetrahydrocurcumin has been found to promote the production of type I collagen in cells. With age and the influence of external factors, collagen in the skin is gradually lost, leading to sagging skin and wrinkles. By stimulating cells to produce more type I collagen, tetrahydrocurcumin helps increase the elasticity and firmness of the skin and reduce the appearance of wrinkles. Tetrahydrocurcumin can effectively inhibit tyrosinase and slow down the production of melanin, and is more effective than whitening agents such as kojic acid, arbutin, and vitamin C. At the same time, the powerful antioxidant activity of tetrahydrocurcumin can also delay the production of melanin, thereby brightening the skin tone and achieving a whitening effect. In addition, free radicals on the surface of the skin are produced by ultraviolet rays, chemicals or other stress factors that catalyze skin aging. Tetrahydrocurcumin can scavenge free radicals, thereby preventing the formation of free radicals. In addition, tetrahydrocurcumin can inhibit the proliferation of free radicals and inhibit the oxidation of fats. It can be added to the formula as a natural antioxidant to extend the shelf life of cosmetics.
[0050] The whitening mechanism is mainly through inhibiting the production and deposition of melanin, reducing pigmentation spots, and making the skin more uniform and bright. Niacinamide can inhibit the activity of tyrosinase, thereby reducing the production of melanin, helping to fade spots, freckles, etc., and making the skin more uniform. Tetrahydrocurcumin has a strong antioxidant and anti-inflammatory effect. The antioxidant and anti-inflammatory properties of tetrahydrocurcumin help slow down the aging process of the skin. Pterostilbene can significantly reduce the number of melanosomes in cells, activate the Nrf2 antioxidant pathway, and increase the expression of antioxidant proteins. By promoting the engulfment of melanosomes by autophagosomes, pterostilbene can inhibit melanosome formation and melanin synthesis, thereby achieving a whitening effect.
[0051] Oxidative damage to cells by free radicals can lead to aging. The use of antioxidants can capture these free radicals and prevent them from damaging cell structure and function, thereby slowing down the aging process. In addition, promoting collagen regeneration, inhibiting sebaceous gland secretion and improving skin microcirculation are also important anti-aging methods. Nicotinamide is a component of coenzyme I (NAD+) and coenzyme II (NADP+), which play a key role in cellular energy metabolism and redox reactions. By promoting cell metabolism, niacinamide helps maintain the normal function and vitality of cells, thereby fighting the aging process. Nicotinamide can promote the synthesis of collagen by skin fibroblasts, increase skin elasticity and reduce the formation of wrinkles. Collagen is an important component of the skin and is essential for maintaining the firmness and elasticity of the skin. Tetrahydrocurcumin has significant antioxidant activity and can capture and neutralize free radicals, reducing free radical damage to cell membranes and DNA. By reducing the level of free radicals in cells, tetrahydrocurcumin can delay the cellular aging process, thereby exerting an anti-aging effect. Pterostilbene is a powerful antioxidant that can scavenge free radicals in the body and reduce oxidative stress. Oxidative stress is one of the main causes of aging, and pterostilbene can protect cells from oxidative damage by neutralizing free radicals, thereby delaying the aging process. Pterostilbene has anti-inflammatory effects, can inhibit inflammatory responses, and reduce the damage of inflammation to cells.
[0052] It can be seen that niacinamide, tetrahydrocurcumin and pterostilbene are three common skin care ingredients, each with unique whitening, wrinkle removal and anti-aging effects. Niacinamide can effectively inhibit melanin production, reduce spots, and promote collagen synthesis to improve skin elasticity. Tetrahydrocurcumin has the property of inhibiting tyrosinase activity, which helps to reduce melanin deposition, while also promoting collagen synthesis and reducing wrinkles. Pterostilbene has antioxidant properties, which can reduce oxidative stress damage to the skin and delay the skin aging process. When these three ingredients are used effectively in combination, they can synergize with each other and work together. When used in combination, niacinamide inhibits melanin production, tetrahydrocurcumin reduces melanin deposition, and pterostilbene inhibits oxidative stress, thereby providing a comprehensive whitening effect; at the same time, niacinamide, tetrahydrocurcumin and pterostilbene jointly promote collagen synthesis, improve skin elasticity, reduce the appearance of wrinkles and fine lines, and achieve a more significant wrinkle removal effect; in addition, the antioxidant properties of the three complement each other, jointly resisting the damage of free radicals to the skin, delaying the skin aging process, and keeping the skin young and healthy. Therefore, the synergistic effect of niacinamide, tetrahydrocurcumin and pterostilbene provides a full range of care and repair for the skin, making the skin more uniform, smooth and youthful. This comprehensive effect is not only reflected in the enhancement of a single effect, but more importantly, the three cooperate with each other to make up for each other's limitations in skin care, achieving a more comprehensive and effective skin care effect. The combination of niacinamide, tetrahydrocurcumin and pterostilbene can not only target multiple skin problems, but also provide long-term comprehensive protection, help the skin resist damage caused by the external environment to the skin, and delay the skin aging process. Therefore, when choosing skin care products, consider products that contain these three ingredients for a more comprehensive and powerful skin care effect, leaving your skin radiant with healthy radiance.
[0053] However, when niacinamide, tetrahydrocurcumin and pterostilbene are used in combination, the following problems exist:
[0054] (1) Poor stability and low bioavailability.
[0055] Pterostilbene is unstable in light and air, and its hydroxyl group is easily oxidized, thus losing its efficacy. Pterostilbene is highly lipid soluble, but very poorly water soluble, so its bioavailability is relatively low. Curcumin has poor stability (easily decomposed by light), poor water solubility, and low bioavailability. Niacinamide is easily degraded by factors such as light, oxygen, and heat, so its application in cosmetics requires the selection of a suitable stabilizer to improve its stability to ensure that its efficacy can last.
[0056] (2) Security issues.
[0057] Although the effective concentration of niacinamide is above 1%, it can improve pigmentation when the concentration reaches 2% to 5%, and it is more effective in brightening the skin when it is greater than 5%. However, high concentrations of niacinamide will cause greater irritation to the skin.
[0058] (3)Solubility and compatibility issues.
[0059] Tetrahydrocurcumin has low solubility in water, so its application in cosmetics requires the selection of appropriate solvents to improve its solubility to ensure that its efficacy can be fully exerted. The compatibility of niacinamide, tetrahydrocurcumin and pterostilbene in cosmetics is also a challenge. The physical and chemical properties of these ingredients can lead to interactions or instabilities in specific formulations, affecting the overall quality and stability of the product.
[0060] (4) Effectiveness issues.
[0061] Although these ingredients have whitening, anti-aging and anti-wrinkle effects, their effects in actual application may vary due to many factors, such as formula, concentration, pH value, etc. Therefore, further research is needed to determine the optimal conditions of use and formula combinations to achieve the best whitening and spot-removing effects.
[0062] (5) The optimal concentration and ratio are difficult to determine.
[0063] Too low a concentration may not be effective, while too high a concentration may cause irritation or other adverse reactions. In addition, the tolerance of different skin types to these ingredients needs to be considered to ensure the safety and effectiveness of the product. Some skin types may be allergic or intolerant to certain ingredients, so careful selection of ingredients and adequate skin testing are required in the formula.
[0064] The invention discloses a whitening, wrinkle-removing and anti-aging pterostilbene liposome composition, which comprises: 1 to 10 parts by weight of nicotinamide, 0.01 to 5 parts by weight of tetrahydrocurcumin, 0.01 to 5 parts by weight of pterostilbene, and 1 to 30 parts by weight of lecithin.
[0065] The whitening, wrinkle-removing and anti-aging pterostilbene liposome composition may further include 1 to 15 parts by weight of an emulsifier or / and an auxiliary emulsifier. The emulsifier may be cholesterol, or phytosterol, oleth-20, Tween 20, Tween 80, etc.; its main function is to help stabilize the liposome.
[0066] In one embodiment of the present invention, the whitening, wrinkle-removing and anti-aging pterostilbene liposome composition comprises: 1 to 10 parts by weight of nicotinamide, 1 to 3 parts by weight of tetrahydrocurcumin, 1 to 5 parts by weight of pterostilbene, 1 to 30 parts by weight of lecithin and 1 to 15 parts by weight of cholesterol. In one embodiment, the pterostilbene liposome comprises: 6 parts by weight of nicotinamide, 1 part by weight of tetrahydrocurcumin, 2 parts by weight of pterostilbene, 8 parts by weight of lecithin and 3 parts by weight of cholesterol.
[0067] The present invention also discloses a cosmetic, which comprises the above-mentioned whitening, wrinkle-removing and anti-aging pterostilbene liposome composition. The cosmetic can be an essence lotion, emulsion, face cream, freeze-dried powder or skin care water.
[0068] In one embodiment of the present invention, the cosmetic further includes an aqueous phase component, an oil phase component, a pH adjuster and a third composition; the aqueous phase component includes a thickener, a first skin conditioner and a first moisturizer; the oil phase component includes a second skin conditioner, an emulsifier and an excipient; the third composition includes a fragrance, a preservative and a second moisturizer.
[0069] In one embodiment, the thickener includes xanthan gum and carbomer, the first skin conditioning agent includes sodium hyaluronate and allantoin, the first moisturizing agent includes glycerin and jojoba oil; the second skin conditioning agent includes cetyl alcohol, the emulsifier includes cetearyl glucoside and cetearyl alcohol, the excipient includes squalane; the pH regulator includes arginine; the fragrance includes essence, the preservative includes phenoxyethanol, and the second moisturizing agent includes ethylhexylglycerin.
[0070] The present invention further discloses a method for preparing a whitening, wrinkle-removing and anti-aging pterostilbene liposome composition. Figure 1 FIG. 1 is a flow chart of a method for preparing pterostilbene liposomes according to an embodiment of the present invention; Figure 1 , the preparation method comprises:
[0071] [Step S1] Dissolve 0.5 to 10 parts by weight of nicotinamide in water to obtain a phase A mixed solution; dissolve 0.01 to 5 parts by weight of tetrahydrocurcumin and 0.01 to 5 parts by weight of pterostilbene in oil to obtain a phase B mixed solution.
[0072] In one embodiment, when niacinamide is dissolved in water, polyols (propylene glycol, butylene glycol, dipropylene glycol, ethanol, etc.) may be added to assist dissolution.
[0073] The oil includes at least one of C13-C16 alkane, C5-19 alkane, semisqualane, and caprylic acid capric acid triglyceride. The oil can also be polar oil (such as octyldodecanol, oleyl oleate, IPM, IPP, etc.).
[0074] [Step S2] Compound the phase B mixed solution and 1 to 30 parts by weight of lecithin to obtain a phase C mixed solution.
[0075] In one embodiment, the phase B mixed solution and lecithin and an emulsifier in 1 to 30 parts by weight can be compounded to obtain a phase C mixed solution; the emulsifier includes at least one of cholesterol, phytosterol, oleth-20, polysorbate-20 (Tween 20), polysorbate-40 (Tween 40), polysorbate-60 (Tween 60), and polysorbate-80 (Tween 80);
[0076] [Step S3] Extract an appropriate amount of phase C mixed liquid and inject it into an appropriate amount of phase A mixed liquid to obtain a phase D mixed liquid; the mass fraction of niacinamide in the phase D mixed liquid is 0.5-10, the mass fraction of tetrahydrocurcumin is 0.01-5, the mass fraction of pterostilbene solvent is 0.01-5, and the mass fraction of lecithin is 1-30.
[0077] In one embodiment, the extracted C-phase mixed solution is injected into the stirring A-phase mixed solution at a rate of 2-5 μl / min to obtain a D-phase mixed solution.
[0078] [Step S4] Dry the phase D mixed solution to obtain the whitening, anti-wrinkle and anti-aging pterostilbene liposome composition.
[0079] In one embodiment, the mixed solution of phase C is concentrated under reduced pressure at a pressure of ≤70 kPa, then ultrasonicated, and frozen and dried at a temperature of -40°C to -45°C to obtain pterostilbene liposomes.
[0080] The present invention also discloses a method for preparing the above cosmetics, the method comprising:
[0081] Step a, placing water in a container with a stirring device and stirring, adding the aqueous phase components after fully wetting and mixing them into the water, stirring them fully until they are completely dissolved, and heating them to 75-80°C;
[0082] Step b, mixing the oil phase components, heating to 75-80°C, and stirring until completely dissolved;
[0083] Step c, adding the mixture obtained in step b to the aqueous phase obtained in step a, stirring at 200-400 rpm and homogenizing at 2000-4000 rpm for 10-30 minutes;
[0084] Step d, adding a pH adjuster, stirring at 200-400 rpm and homogenizing at 2000-4000 rpm for 10-30 minutes; stirring and cooling to 45°C.
[0085] Step e, adding the third composition, stirring at 200-400 rpm and homogenizing at 2000-4000 rpm for 10-50 minutes, and sterilizing by filtration;
[0086] Step f: after the temperature drops to 35-38° C., add the above-mentioned whitening, wrinkle-removing and anti-aging pterostilbene liposome composition, stir at 200-400 rpm and homogenize at 2000-4000 rpm for 5-20 minutes to obtain the cosmetics.
[0087] In one embodiment of the present invention, the method for preparing the cosmetic comprises:
[0088] Step a, placing water in a container with a stirring device and stirring, adding the aqueous phase components after fully wetting and mixing them into the water, stirring them fully until they are completely dissolved, and heating them to 75-80°C;
[0089] Step b, mixing the oil phase components, heating to 75-80°C, and stirring until completely dissolved;
[0090] Step c, adding the mixture obtained in step b to the aqueous phase obtained in step a, stirring at 200-400 rpm and homogenizing at 2000-4000 rpm for 10-30 minutes;
[0091] Step d, adding a pH adjuster, stirring at 200-400 rpm and homogenizing at 2000-4000 rpm for 10-30 minutes; stirring and cooling to a set temperature (such as 30° C. to 50° C., such as 45° C.);
[0092] Step e, adding the third composition, stirring at 200-400 rpm and homogenizing at 2000-4000 rpm for 10-50 minutes, and sterilizing by filtration;
[0093] Step f: after the temperature drops to 35-38° C., add the above-mentioned whitening, wrinkle-removing and anti-aging pterostilbene liposome composition, stir at 200-400 rpm and homogenize at 2000-4000 rpm for 5-20 minutes to obtain the cosmetics.
[0094] Example 1
[0095] The mass fraction ratio of nicotinamide (0.5-10%), tetrahydrocurcumin (0.01-5%) and pterostilbene (0.01-5%) is 6-10:1:2-5.
[0096] The preparation method of nanoliposomes comprises the following steps:
[0097] Step 1, dissolve nicotinamide in water by ultrasonication to obtain a phase A mixed solution; dissolve tetrahydrocurcumin and pterostilbene in oil to obtain a phase B mixed solution;
[0098] Step 2: Compound the phase B mixture and lecithin to obtain a phase C mixture.
[0099] In one embodiment, cholesterol can also be added during compounding; lecithin and cholesterol are mixed in a mass ratio of 1 to 5:1 (preferably, the mass ratio of lecithin to cholesterol is 8:3) and compounded with the phase B mixed solution.
[0100] Step 3, extract the phase C mixture and inject it into the stirring phase A mixture at a rate of 2 to 5 μl / min to obtain the phase D mixture;
[0101] Step 4, concentrate the phase D mixture under reduced pressure at a pressure of ≤70 kPa, ultrasonicate it, and freeze-dry it at a temperature of -40°C to -45°C to obtain liposome particles.
[0102] Based on 100 parts by weight, lecithin is 40 parts and cholesterol is 15 parts.
[0103] Table 1 Content of each component in liposomes (unit: mass fraction)
[0104]
[0105] In one embodiment of the present invention, each group of experiments is set up with essence as an example, but it is not limited to the use of essence. The composition can also be applied to various skin care products such as lotion, cream, freeze-dried powder, skin care water, etc. The essence is the above-mentioned key combination and skin care agent, thickener, chelating agent and pH regulator. Preferably, the raw materials for preparing the essence with barrier enhancement and anti-aging effects also include any one or a combination of at least two of preservatives and flavors. The total weight is 100 parts by weight, A is 86 to 92.9 parts, B is 1.5 to 2.5 parts, C is 0.1 to 0.5, D is 0.5 to 1.5 parts, and E is 5 to 10 parts.
[0106] Table 2 Proportions of various components in Example 1 (unit: wt%)
[0107]
[0108]
[0109] In one embodiment of the present invention, the cosmetic essence preparation process is:
[0110] a. Water phase: Place water in a container with a stirring device and stir. After fully wetting and mixing the other parts of the raw material combination A, add them into the water, stir thoroughly until completely dissolved, and heat to 75-80°C.
[0111] b. Oil phase: Mix raw material combination B, heat to 75-80°C, and stir until completely dissolved.
[0112] c. Emulsification: Add the mixture from step b to the aqueous phase from step a, stir at 300 rpm and homogenize at 3000 rpm for 5 minutes.
[0113] d. Add raw material C, stir at 300 rpm and homogenize at 3000 rpm for 3 minutes; stir and cool to 45°C.
[0114] e. Add raw material combination D, stir at 300 rpm and homogenize at 3000 rpm for 3 minutes, and filter sterilize by filtration.
[0115] All the above steps were strictly controlled for sterility.
[0116] f. After the temperature drops to 35-38°C, add combination E, stir at 300rpm and homogenize at 3000rpm for 3 minutes to obtain the required essence. Filter and sterilize before filling, and test the bacterial content, toxins, immunogenicity, etc. for quality control.
[0117] Table 3 Raw material composition ratio of Example 1 and Blank Examples 1-7 (unit: wt%)
[0118]
[0119]
[0120] Example 2, Example 3
[0121] The difference from Example 1 is only the addition of each active ingredient, the difference from Example 3 is only the reduction of each active ingredient, and the difference from Blank Examples 1-7 is only the lack of key composition components 1 to 3. The preparation method is the same as that of Example 1.
[0122] Change rate = (analysis value after using the product - analysis value before using the product) ÷ analysis value before using the product × 100%.
[0123] Test experiments and their results
[0124] (1) The skin melanin content was measured by an instrument. After using the product for 7 days, 28 days, and 56 days, 100% of the subjects had their skin whitening improved.
[0125] Table 4 Comparison of usage effects (melanin content)
[0126] sample After 7 days of use After 28 days of use After 56 days of use Example 1 -17.24% -19.65% -21.31% Example 2 -20.13% -23.95% -26.39% Example 3 -14.18% -16.20% -19.45% Blank example 1 -11.81% -14.14% -16.22% Blank example 2 -10.05% -13.56% -15.49% Blank example 3 -8.32% -11.77% -13.95% Blank example 4 -7.12% -8.75% -9.16% Blank example 5 -6.15% -7.94% -7.83% Blank example 6 -5.43% -6.22% -7.21% Blank example 7 -1.31% -2.11% -3.05%
[0127] (2) After measuring cheek wrinkles using a skin testing instrument, it was observed that the wrinkles of all subjects had significantly improved and became lighter on the 7th, 28th and 56th days after using the product.
[0128] Table 5 Comparison of usage effects (cheek wrinkles)
[0129] sample After 7 days of use After 28 days of use After 56 days of use Example 1 -11.21% -15.14% -18.67% Example 2 -14.88% -18.98% -23.64% Example 3 -9.43% -11.77% -15.69% Blank example 1 -7.98% -8.83% -10.24% Blank example 2 -6.65% -8.02% -9.26% Blank example 3 -5.37% -6.98% -8.68% Blank example 4 -4.19% -5.83% -7.46% Blank example 5 -3.89% -5.30% -6.85% Blank example 6 -3.21% -4.82% -5.71% Blank example 7 -1.12% -1.97% -2.67%
[0130] (3) Experiment on the anti-aging efficacy of niacinamide.
[0131] Figure 2 This is a schematic diagram of the effect of the niacinamide anti-aging effect experiment in one embodiment of the present invention; please refer to Figure 2 ,pass Figure 2 It can be seen that nicotinamide can enhance the synthesis of protein and collagen in skin fibroblasts. In aged fibroblasts, 500 μM nicotinamide was supplemented for 48 hours; hydroxyproline was used as a marker for collagen, and proline was used as a marker for total protein. Nicotinamide selectively stimulated the synthesis of collagen, and the total amount of collagen / total protein was significantly increased compared with the control sample.
[0132] (4) Experiment on the efficacy of Pterostilbene in removing jaundice and anti-aging.
[0133] Glycation reaction refers to the accumulation of excessive reducing sugars due to slow metabolism in the skin, which react with the collagen and elastin in the skin to form irreversible brown advanced glycation end products (AGEs), causing the collagen or elastin to denature and cross-link, causing wrinkles to appear on the skin and making it rough and dark yellow. Figure 3 This is a schematic diagram of the effect of the anti-jaundice and anti-aging effect experiment of pterostilbene in one embodiment of the present invention; please refer to Figure 3 ,pass Figure 3 It can be seen that pterostilbene can reduce the content of cross-linked proteins, inhibit glycation reactions, reduce the production of AGEs, and achieve the effect of removing yellowness and anti-aging.
[0134] Experimental conclusion: Using CML ELISA Assay Kit and aminoguanidine as positive control, the inhibition rate of AGEs generation was 11.96% when the concentration of pterostilbene was 31.25μg / ml. The inhibition rate of aminoguanidine was 32.53% when the concentration was 10mM (740.9μg / ml).
[0135] In summary, the whitening, wrinkle-removing and anti-aging pterostilbene liposome composition and its preparation method, cosmetics and their preparation method proposed in the present invention use liposome encapsulation technology to solve the problems of easy discoloration, poor solubility and easy crystallization of pterostilbene in cosmetic formulas; by using liposomes to encapsulate active ingredients such as nicotinamide, tetrahydrocurcumin and pterostilbene, they are prevented from being easily degraded by factors such as light, oxygen and heat, and the stability of the active ingredients in cosmetics is improved, so as to better exert their efficacy.
[0136] Because the tiny vesicle structure of liposomes is similar to that of the skin surface, they can interact with the skin more easily and promote the penetration and absorption of active ingredients. By encapsulating active ingredients, their permeability and bioavailability in the skin are improved, thereby better exerting their efficacy.
[0137] In one usage scenario of the present invention, the present invention adjusts the usage ratio of the three ingredients, and the ratio of niacinamide (0.5-10%), tetrahydrocurcumin (0.01-5%), and pterostilbene (0.01-5%) is 6-10:1:2-5, which can achieve the best whitening, anti-wrinkle and anti-aging effects.
[0138] Niacinamide is a vitamin B3 derivative that can promote the metabolism of skin cells, increase the skin's barrier function, and regulate skin pigmentation, thus having whitening, anti-aging and moisturizing effects. Tetrahydrocurcumin is a curcumin derivative that can inhibit the synthesis of melanin, reduce the formation of spots and wrinkles, and has an antioxidant effect. Pterostilbene is a natural plant extract that can promote the synthesis of collagen in the skin and increase skin elasticity and firmness.
[0139] The present invention adopts liposome encapsulation technology to improve the stability of active ingredients. The whitening, anti-wrinkle and anti-aging composition comprises nano-encapsulation of tetrahydrocurcumin, which helps dissolve tetrahydrocurcumin, prevents crystal precipitation, is more conducive to the stability and sustained release of active ingredients, and synergizes with other active ingredients to exert anti-wrinkle and repair effects.
[0140] The present invention integrates a variety of whitening, wrinkle-removing and anti-aging ingredients, and the formula is unique. Nicotinamide inhibits melanin production, tetrahydrocurcumin reduces melanin deposition, and pterostilbene inhibits oxidative stress, thereby providing a comprehensive whitening effect; at the same time, nicotinamide, tetrahydrocurcumin and pterostilbene jointly promote the synthesis of collagen, improve skin elasticity, reduce the appearance of wrinkles and fine lines, and achieve a more significant wrinkle-removing effect; in addition, the antioxidant properties of the three complement each other, jointly resist the damage of free radicals to the skin, delay the skin aging process, and keep the skin young and healthy. Therefore, the synergistic effect of nicotinamide, tetrahydrocurcumin and pterostilbene provides a full range of care and repair for the skin, making the skin more uniform, smooth and youthful. This comprehensive effect is not only reflected in the enhancement of a single effect, but more importantly, the three cooperate with each other to make up for each other's limitations in skin care, and achieve a more comprehensive and more effective skin care effect.
[0141] The technical features of the above-described embodiments may be arbitrarily combined. To make the description concise, not all possible combinations of the technical features in the above-described embodiments are described. However, as long as there is no contradiction in the combination of these technical features, they should be considered to be within the scope of this specification.
[0142] The description and application of the present invention here are illustrative, and it is not intended to limit the scope of the present invention to the above-mentioned embodiments. The effects or advantages involved in the embodiments may not be embodied in the embodiments due to interference from various factors, and the description of the effects or advantages is not used to limit the embodiments. The deformation and change of the embodiments disclosed here are possible, and the replacement of the embodiments and the various equivalent parts are well known to those of ordinary skill in the art. It should be clear to those skilled in the art that the present invention can be implemented in other forms, structures, arrangements, proportions, and with other components, materials and parts without departing from the spirit or essential features of the present invention. Other deformations and changes can be made to the embodiments disclosed here without departing from the scope and spirit of the present invention.
Claims
1. A whitening, wrinkle-removing and anti-aging pterostilbene liposome composition, characterized in that: The whitening, wrinkle-removing and anti-aging pterostilbene liposome composition comprises: 0.5-10 parts by weight of nicotinamide, 0.01-5 parts by weight of tetrahydrocurcumin, 0.01-5 parts by weight of pterostilbene and 1-30 parts by weight of lecithin.
2. The whitening, anti-wrinkle and anti-aging pterostilbene liposome composition according to claim 1, characterized in that: The whitening, wrinkle-removing and anti-aging pterostilbene liposome composition further comprises 1 to 15 parts by weight of an emulsifier or / and an auxiliary emulsifier.
3. The whitening, wrinkle-removing and anti-aging pterostilbene liposome composition according to claim 2, characterized in that: The whitening, wrinkle-removing and anti-aging pterostilbene liposome composition comprises: 1 to 10 parts by weight of nicotinamide, 1 to 3 parts by weight of tetrahydrocurcumin, 1 to 5 parts by weight of pterostilbene, 1 to 30 parts by weight of lecithin and 1 to 15 parts by weight of cholesterol.
4. A cosmetic, characterized in that: The cosmetic comprises the whitening, anti-wrinkle and anti-aging pterostilbene liposome composition according to any one of claims 1 to 3.
5. The cosmetic according to claim 4, characterized in that: The cosmetics are essence lotion, emulsion, facial cream, freeze-dried powder or skin care water.
6. The cosmetic according to claim 4, characterized in that: The cosmetic further comprises a water phase component, an oil phase component, a pH adjuster and a third composition; The water phase component includes a thickener, a first skin conditioning agent and a first moisturizer; the oil phase component includes a second skin conditioning agent, an emulsifier and an excipient; and the third composition includes a fragrance, a preservative and a second moisturizer.
7. The cosmetic according to claim 6, characterized in that: The thickener includes xanthan gum and carbomer, the first skin conditioning agent includes sodium hyaluronate and allantoin, and the first moisturizing agent includes glycerin and jojoba oil; The second skin conditioning agent includes cetyl alcohol, the emulsifier includes cetearyl glucoside and cetearyl alcohol, and the excipient includes squalane; The pH adjuster includes arginine; the fragrance includes essence; the preservative includes phenoxyethanol; and the second moisturizer includes ethylhexylglycerin.
8. A method for preparing a whitening, wrinkle-removing and anti-aging pterostilbene liposome composition, characterized in that: The preparation method comprises: Step S1, dissolving 0.5-10 parts by weight of nicotinamide in water to obtain a phase A mixed solution; dissolving 0.01-5 parts by weight of tetrahydrocurcumin and 0.01-5 parts by weight of pterostilbene in oil to obtain a phase B mixed solution; Step S2, compounding the phase B mixed solution and 1 to 30 parts by weight of lecithin to obtain a phase C mixed solution; Step S3, extracting an appropriate amount of phase C mixed solution, injecting an appropriate amount of phase A mixed solution, to obtain a phase D mixed solution; the mass fraction of nicotinamide in the phase D mixed solution is 0.5-10, the mass fraction of tetrahydrocurcumin is 0.01-5, the mass fraction of pterostilbene is 0.01-5, and the mass fraction of lecithin is 1-30; Step S4, drying the phase D mixed solution to obtain the whitening, wrinkle-removing and anti-aging pterostilbene liposome composition.
9. The preparation method according to claim 8, characterized in that: In step S1, the oil includes at least one of C13-C16 alkane, C5-19 alkane, semi-squalane, and caprylic capric triglyceride; In the step S2, the phase B mixed solution and 1 to 30 parts by weight of lecithin are compounded with an emulsifier to obtain a phase C mixed solution; the emulsifier includes at least one of cholesterol, polysorbate-40, polysorbate-60, and polysorbate-80; In the step S3, the extracted C phase mixed solution is injected into the stirred A phase mixed solution at a rate of 2 to 5 μl / min to obtain a D phase mixed solution; In the step S4, the phase D mixed solution is concentrated under reduced pressure at a pressure of ≤70 kPa, then ultrasonicated, and frozen and dried at a temperature of -40°C to -45°C to obtain a whitening, wrinkle-removing and anti-aging pterostilbene liposome composition.
10. A method for preparing the cosmetic according to claim 6 or 7, characterized in that: The preparation method comprises: Step a, placing water in a container with a stirring device and stirring, adding the aqueous phase components after fully wetting and mixing them into the water, stirring them fully until they are completely dissolved, and heating them to 75-80°C; Step b, mixing the oil phase components, heating to 75-80°C, and stirring until completely dissolved; Step c, adding the mixture obtained in step b to the aqueous phase obtained in step a, stirring at 200-400 rpm and homogenizing at 2000-4000 rpm for 10-30 minutes; Step d, adding a pH adjuster, stirring at 200-400 rpm and homogenizing at 2000-4000 rpm for 10-30 minutes; stirring and cooling to a set temperature; Step e, adding the third composition, stirring at 200-400 rpm and homogenizing at 2000-4000 rpm for 10-50 minutes, and sterilizing by filtration; Step f, after the temperature is lowered to 35-38° C., add the whitening, wrinkle-removing and anti-aging pterostilbene liposome composition according to any one of claims 1 to 3, stir at 200-400 rpm and homogenize at 2000-4000 rpm for 5-20 minutes to obtain the cosmetics.