KR20040111227A - Niosome containing vitamins and amaranth oil. and Cosmetic compositions containing the same. - Google Patents

Abstract

PURPOSE: Provided are niosome typed multilamellar vesicle(MLV) containing vitamin A, vitamin C, vitamin E, linoleic acid, amaranth oil, and meadowfoam seed oil, and cosmetic compositions containing the same to improve a skin condition by moisturization and antioxidation effects and physiological activity promotion. CONSTITUTION: The niosome typed multilamellar vesicle(MLV) is composed of phytosterol 3%, cholesterol 3%, ceteth-24 2%, chlorite-24 2%, cetyl phosphate 0.5%, glycerin 10%, ceramide 1%, retinyl palmitate 3%, panthenol 1%, tocopheryl acetate 5%, vitamin C 1.00%, linoleic acid 1%, meadowfoam seed oil 2%, amaranth oil 0.5%, dimethicone 15% and purified water.

Description

Niosome containing vitamins and amaranth oil and cosmetic compositions containing same {Niosome containing vitamins and amaranth oil. and Cosmetic compositions containing the same.}

Liposomes are spherical vesicles in which the phospholipid bilayer surrounds the water phase. The lipid membrane is an amphiphilic phospholipid consisting of two hydrophobic fatty acid groups and a hydrophilic phosphate group, forming a double membrane in aqueous solution, which forms a closed vesicle like an artificial cell. In the double membrane structure, the non-polar fatty acid tail faces the inside of the membrane and the polar head faces outward. Liposomes are largely classified into two types according to the number of lamellas. One of them, Multilamellar Vesicle (MLV), consists of five or more lamellae, and is about 100nm to 1㎛ in size. Secondly, Unilamellar vesicles have a single bilayer structure, less than 100nm is called SUV, and more than 100nm is called LUV. In the field of cosmetics, liposomes aim to maximize the effect and increase skin absorption by stabilizing unstable substances from external oxygen and light using phospholipids, which are skin-friendly substances. In order to make such liposomes, a lot of lecithin is usually used, and the liposomes are made by using a nonionic surfactant due to its high price. Liposomes composed of nonionic surfactants are sometimes called niosomes and are called nonionic surfactant vesicles (NSV). These NSVs are similar in structure to liposomes, but there are differences. Stabilization of these vesicles depends on the cholesterol or phytosterol component that maintains the membrane. The nonionic surfactant is composed of polyoxyethylene alkyl ether, polyoxyethylene alkyl ester and saccharose diester. NSV composed of nonionic surfactants can not be expected to act like lipid alone by nonionic surfactants alone, and should be similar to natural lipid components. It is mainly used to make amphiphilic properties by incorporating phosphate derivatives into glycerin skeleton. .

The vitamin seed applied here is very unstable to the existing ascorbyl acid, which increases the stability. In our recent study of controlling L-ascobic acid (Asc) to improve solubility in oily substances, we found one interesting thing. Lipophilic Asc-derivatives 2, 3, 5, 6, -O-tetra-2-hexyldecanoyl-L-ascorbic acid (VC-IP) have been developed that do not impair the beneficial Asc-activity and provide high thermal stability in cosmetic formulations. It is a colorless and transparent liquid. Efficient comparisons of VC-IP and Asc provide: (1) SOD-like activity, (2) a stable role in reducing radicals, (3) singlet oxygen-reducing activity, and (4) UV-B photo-oxidation in human sebum. Protective activity, (5) HM-3-KO melanoma cells using melanoma production inhibitory effect was evaluated. Furthermore, the biochemical activity of VC-IP is (6) measured by the amount of VC-IP condensed and absorbed as intracellular Asc and (7) cells of VC-IP for cell mortality due to UV-B irradiation to cutaneous keratinocytes. The protective effect was also tested. From this study we concluded that VC-IP is a highly effective substance in skin care formulations. The relationship between skin aging caused by the activity of oxygen species such as superoxide anion radicals, hydrogen peroxide, hydroxyl radicals and singlet oxygen or free radicals and damage to skin cell components has been demonstrated. These types of free radicals, mainly caused by the effects of environmental oxidation, cause many diseases, such as oxidation of proteins or lipids, cross-linking of proteins, and damage to DNA or tissues. For a long time, L-ascorbic acid (Asc) has been used in skin care products as a whitening ingredient for inhibiting melanin formation formed by eumelanin resulting from the reduction of scavenger and intermediate dopaquinone against free radicals to prevent these diseases and the production of melanin. .

Despite these good properties, Asc has not been successfully used in cosmetics because it does not dissolve well in heat-stable and useful materials. This new lipophilic Asc derivative, 2,3,5,6, -O-tetra-2-hexyldecanoyl-L-asc-obic acid (VC-IP), has high thermal stability in cosmetic formulations without loss of beneficial Asc-activity. It is a colorless transparent liquid. (A) a SOD-like activity, (B) a stable radical that reduces activity, (C) a singlet oxygen reducing activity, (D) a protective role against UV-B photo-oxidation in human sebum, (E) HM-3- Inhibitory effects of melanin production using K0 human melanoma cells, and (F) the effect of VC-IP on the skin on the cell death rate by UV-S irradiation on keratinocytes. did.

In other words, VC-IP is a wrinkling and whitening process that eliminates free radicals, promotes collagen synthesis, promotes collagen mRAN synthesis, prevents photoaging, inhibits DNA damage, inhibits melanogenesis and reduces preformed melanin, and prevents brain aging. It is an effective raw material.

Tocopherol is also called vitamin E, and the substance on which vitamin E functions is tocol, that is, derivative of chromane based on 2-methyl-2- [trimethyl-tridecyl] -6-hydroxychromane as a backbone. The side chain of the tocol is derived from phytol, and trienol having a double bond at the 3 ', 7' and 11 'positions of the side chain has a structure similar to the tocol. Tocol and trienoyl are various isomers by the position and number of methyl groups in the croman ring. Tocopherol species include alpha, beta, gamma and delta-tocopherol. Tocopherol has antioxidant activity and prevents the oxidation of vitamin A in vivo. In addition, toothpaste is effective in preventing periodontitis. Antioxidant activity is alpha: beta: gamma: delta = 1: 1.3: 1.8: 2.7 at room temperature, which is superior to delta tocopherol. Tocopherol itself is unstable and uses a lot of its derivatives, especially vitamin acetate, vitamin palmitate and various derivatives exist. Vitamin E is effective against severe periodontal disease. If your teeth are silver plated, the antioxidant effects of tocopherol are essential. Mercury depletes the antioxidant enzymes SOD, glutathione peroxidase and catalase in silver tissues. Animal testing has shown that tocopherol reduces silver toxicity.

Vitamin A contains synthetic palmitic retinol or synthetic palmitic retinol containing vegetable oil in an amount of 1.5 million or more vitamin A units per 1g. All animals need a supply of vitamin A from the outside. This is called provitamin A because it does not exist as A but as carotene. Since the body has the ability to convert carotene to active vitamins, vitamin A or carotene is expressed as a vitamin A value.

Vitamin A plays an important role in vision. That is, cis-type vitamin A is an aldehyde form of vitamin A aldehyde, which is involved in visual action, which combines with specific protein opsin in the dark to form the visual pigment rhodopsin. It receives light and separates it into more stable forms, all-trans-retinal and opsin. The exercise at this time stimulates the optic nerve, which is transmitted to the furnace. The all-trans-retinal is converted back to 1,1-cis-retinal and this visual action circuit is repeated. Therefore, lack of vitamin A will cause night blindness. It reduces the roughness of the skin surface, increases the elasticity of the skin, and regenerates and grows the skin with the activity of cells.

The first discoveries of evening primroses were indigenous Indians who lived across the east coast of the United States and now in Canada. They have harvested wild evening primroses from over a thousand years ago, grinding whole leaves, stems, and berries and applying them to wounds on trauma, or to rashes or boils on the affected area. In addition, it was used as an internal medicine to relieve asthma and cough of pulmonary tuberculosis as well as external medicine, and to soothe pain medication and seizure.

At this time, he knew only that Evening Primrose had its medicinal effect, and its scientific basis was that in the 1930s, according to the development of nutritional physiology, a large amount of essential fatty acid (unsaturated fatty acid that can be consumed only in plants) is contained in the oil obtained from the Evening Primrose seeds. I knew it was. It was named vitamin F at the time, but today it is known as linoleic acid. It was once called the panacea of kings in Europe, and the British government chose evening primrose oil as a national medicine. Later, further studies on the components of evening primroses were spurred on, and the reason they finally benefited the human body was found to be Gamma Linolenic acid. Evening Primrose Gamma Linolenic acid There are many unsaturated fatty acids in the human body, one of which is γ (gamma) -linolenic acid. It is an unsaturated fatty acid that cannot be synthesized in the body and must be consumed as a plant from the outside. In nature, it is contained only in a limited amount, such as a iris flower or breast milk. Γ (gamma) -linolenic acid in evening primrose oil is an essential ingredient for the in vivo synthesis of prostaglandins. Prostaglandins are effective in lowering blood cholesterol levels in 1982 by doctors who have already won the Nobel Prize in Physiology. Linoleic acid (about 70%) contained in evening primrose oil, which is itself an unsaturated essential fatty acid that is not synthesized by the human body, but is rich in vegetable oils such as beans, brown rice, wheat, cotton seeds, sunflowers, and corn.

However, the value of evening primrose oil is very important that Gamma Linolenic Acid (GLA), found only in breast milk, contains more than 7-8% of all fatty acids in natural form. Gamma Linolenic Acid is the first synthetic compound to change linoleic acid into various compounds after it enters the body. To convert from linoleic acid to gamma-linolenic acid, you need a substance (enzyme) that mediates it. The enzyme is called Delta6-desaturase. An enzyme called Dclta6-desaturase may not function or be deficient in some people. Because the enzyme may not work by inhibiting linoleic acid into gammalinolenic acid by some inhibitor. This means that no matter how much linoleic acid you eat, it may not be synthesized as gamma linolenic acid in your body. Therefore, such a person should consume a plant containing gamma-linolenic acid directly, since fats and oils containing gamma-linolenic acid in its natural form are not found at this time except seed oil of breast milk and evening primrose.

The components of evening primrose oil ① ① linoleic acid 67.5% ② gamma linolenic acid 7.5% ③ other fatty acids 25.0%. The effect and characteristics of evening primrose oil (gamma linolenic acid, omega-6 fatty acid) are improved blood circulation, physical function and stamina, anti-arthritis Effects (clinical results), inflammatory reactions in the body and inhibitory substances (e.g. prostaglandin-prostaglandin), disease prevention, health promotion: breast / prostate cancer / high cholesterol / Zn deficiency / diabetes / inflammatory diseases such as atopic dermatitis and other skin Diseases, Women's Health PMS Syndrome (Premenstrual Syndrome), Breast Pain, Skin Health, Pregnancy or Breastfeeding, Maternal and Child Health, Essential Fatty Acids-Helps With Fetal Development-Preventing Pregnancy Hypertension, Child Health: Hyperactivity Effect-Distracted children. The effects and effects of gamma linoleic acid have the effect of preventing the aging by promoting the activity of prostaglandins by ingesting GLA (gammarinolic acid) to prevent aging. As a result of maintaining skin health, Dr. J. Weipierre announced that the application of GLA (gammalinolenic acid) as an ointment to human and rat skin was very slow and partially absorbed and continued to work for a long time in the subcutaneous structure. Gammalinolenic acid energizes the cells to prevent skin aging, prevents skin from drying out and nourishes.

In addition, a researcher with atopic dermatitis reported that clinical results using Evening Primrose Oil improved symptoms by administering 180 mg of gamma linolenic acid daily for 12 weeks. It is speculated that one of the causes of atopic dermatitis, which occurs frequently in infants and is rapidly increasing in recent years, is a lack of GLA (gammalinolenic acid). This is because a decrease in GLA (gammarinolenic acid) metabolism was found in patients with atopic dermatitis. A lactating infant has the softest, most elastic, lustrous, fresh skin in the world. However, the infant's skin also lacks breast milk, so if you replace it with artificial nutrition milk or move to baby food, eczema often occurs. Most of these are atopic. In this regard, Dr. Horrobin, a former professor at the University of Montreal, the first element of evening primrose research, and now head of the Efamol Institute in Canada, does not contain GLA (Gammalinolenic Acid) in breast milk. Announced. GLA deficiency can lead to atopic dermatitis or asthma and rarely heals. Currently, Preston University in the UK prescribes evening primrose oil to such babies, which is a very good treatment. Is saying. In general, atopic dermatitis decreases as an adult develops in infancy and becomes less adult, but there is no complete recovery. Especially, a woman is sensitive to cosmetics, so treatment is important.

Amaranth seed oil is extracted by carbon dioxide extraction method and contains squalene, phytosterol and vitamin E derivatives (alpha, beta, gamma, delta and tocotrienol) and oils oleic acid and linoleic acid It contains a large amount of water, which is excellent for skin moisturizing and antioxidant effects.Methofoam seed oil has an excellent antioxidant effect because it contains tocopherol.

In the present invention, as a collagen synthesis or whitening agent of the skin, vitamins that strengthen the intercellular lipids of the skin and promotes metabolism and enhances the biological function of the skin and regenerates the cells of each function of the human body to supply nutrition Its purpose is to stabilize oils that prevent aging with multi-lamella vesicles by preventing disease and anti-oxidant effect, and apply to skin care. In the material composition used in the present invention, light, heat, air using phytosterol 3%, cholesterol 3%, cethes-24 2%, chlores-24 2%, cetyl phosphate 0.5%, glycerin 10%, ceramide 1% Unstable Retinyl Palmitate 3%, Panthenol 1%, Tocopheryl Acetate 5%, Vitamin C 1.00%, Linoleic Acid 1%, Meadowfoam Oil 2%, Amaranth Oil 0.5%, Dimethicone 15%, Multi as purified water Lamellar vesicles have increased their stability, penetration of the skin and body further.

The composition of the multilamella vesicle used in the present invention is as follows.

Phytosterol 3%

Cholesterol 3%

Setes-24 2%

Chlores-24 2%

Secyl phosphate 0.5%

Glycerin 10%

Ceramide 1%

Retinyl Palmitate 3%

Panthenol 1%

Tocopheryl Acetate 5%

Vitamin C 1.00%

Linoleic Acid 1%

Meadowfoam oil 2%

Amaranth Oil 0.5%

Dimethicone 15%

We make purified water total 100

Example 1 A composition example of a lotion using a multi lamella vesicle is as follows.

Example 2 The composition of the skin toner using the multi lamella vesicle is as follows.

The manufacturing process of the multilamella vesicle is as follows.

Multilamella vesicles include 3% phytosterol, 3% cholesterol, 2% cetez-24, 2% Chlores-24, 2% Cetylphosphate 0.5% Glycerin 10%, Ceramide 1%, Retinyl Palmitate, 1% Panterol Tocopheryl Acetate 5% Vitamin C 1.00%, Linoleic Acid 1%, Meadowfoam Oil 2%, Amaranth Oil 0.5% Dimethicone 15% After passing through continuously, cooling and defoaming is completed.

Preparation of Examples 1 and 2 is a general homomixer using a general emulsification method with a component dissolved in oil as an oil phase component and a component dissolved in purified water as an aqueous phase component at a constant temperature (80-82 degrees). After homogeneous mixing, the resin component as a middle agent is neutralized and then cooled, followed by addition of a multilamella vesicle, cooling, and defoaming to complete the manufacturing process.

The data of the present invention is as follows.

1) Particle distribution of multi-lamella vesicles (Malvern, Zetasizer 1000HS measurement)

The particle distribution was measured by Malvern, Zetasizer 1000HS and the particle size was 200-300nm. (Figure 1)

2) Particle photograph of multilamella vesicle

(photo Graphing Freeze-Fracture Scanning Electron Microscopy)

Since the particle size is so small that it cannot be measured by a general optical microscope, it was taken using a frozen electron microscope (Figure 2).

3) Skin improvement measure (IMAGE ANALYZER)

The photo taken with IMAGE ANALYZER was taken two weeks after applying the multilamella vesicles to the lotion, and it can be seen that the keratin through the multilamella vesicles disappeared after two weeks (Figure 3).

4) Comparison of moisturizing power when adding multi-lamella vesicle in lotion prescription (CORNEOMETER)

After applying the multilamella vesicle lotion with CORNEOMETER CM850, the moisturizing power was measured, and the lotion containing the multilamella vesicle was superior to the lotion without the added lotion.

5) Antioxidant and Free Radical Scavenging Effects of Multilamella vesicles

Neo Tetrazolium Blue (NBT) method (anti O2, H2O2 activity)

a) solution

-phosphate buffer pH = 7.8

-substrat / reactive

. Triton ....................... 1.6ML

. EDTA ............... 2.9Mg

. NBT ..................... 24Mg

. hypoxanthin ........ 5.4Mg

. Phosphate buffer ............. 100ML

Enzyme

.Xanthin oxydase ............... 12uL

.Phosphate buffer .............. 10ML

b) Add 0.5 mL of solution, 100 μL of multilamellae vesicles and 0.5 mL of enzyme to the UV spectrometer, and incubate at 37 ° C for 30 minutes and measure at 540 nm.

Antioxidant Effect of Multilamella vesicles (Figure 5)

It has been reported that multilamella vesicles, which enhance capillary vessels, have a synergistic effect on antioxidant effects when applied with vitamin C.

When applied with Vitamin-C, multilamellar shows a greater synergy effect when used alone, and higher antioxidant activity than BHT (Butyrated hydroxytoluene), a representative synthetic material used as a preservative.

A: Vitamin C alone, B: Nano vesicle alone, C: Vitamin C + nano vesicle in combination, BHT: Butyrated hydroxytoluene

※ Anti-oxidant activity of each compound is expressed as log ΔA47O / min

* Free Radical Scavenging activity test (Figure 6)

Reactive oxygen species are by-products of energy production in aerobic metabolism and can bind to macromolecules such as DNA when they are not neutralized by various defense systems in the body, causing mutations in genes in the skin. Promotes aging

Free radicals are also produced by characteristic enzyme reactions in the body, by smoking, by exposure to pollutants or in direct sunlight, and destroy the intracellular substances by a chain reaction. In particular, the oxidation of lipids is initiated, i.e., oxidation of lipids by free radicals is initiated by oxides produced by addition reactions in unsaturated fatty acids and via autooxidation to destroy cell membranes, while lO2 (or The lipid peroxide formed by OH) can be oxidized or reduced to peroxyradical or alkoxyradical in the presence of metal ions such as Fe2 +.

Free radicals can induce apoptosis, and many phyto-chemicals with plant-derived antioxidant properties can regulate several genes involved in apoptosis. In addition, dopachrome produced by tyrosinase is automatically oxidized to melanin, where CCM reacts with these peroxyradicals involved in the autooxidation chain reaction of these substances to help terminate the chain reaction.

The intercellular lipids are between 200-300nm, but when the multilamella vesicles are applied to the skin at 200-300nm, they will penetrate into the skin very quickly and show an excellent effect.The lotion containing multilamella vesicles with CORNEOMETER CM850 does not contain After applying the lotion, the moisture was measured, and the lotion containing the multilamella vesicle was found to be superior to the lotion without the lotion. As a result of the particle photographs, it was found that the multilamella vesicles were formed very well. Wrinkles were alleviated as a result of the image analyzer, and the multilamella vesicles penetrated the skin very quickly, so the moisturizing effect was excellent.The antioxidant effect was measured, and the antioxidant effect was very excellent due to the effects of amaranth oil, meadowfoam oil, and tocopherol. Appeared.

Claims (3)

Phytosterol 3%, Cholesterol 3%, Ceteth-24 2%, Chlores-24 2%, Cecyl Phosphate 0.5%, Glycerin 10%, Ceramide 1%, Retinyl Palmitate 3%, Panthenol 1%, Tocopheryl Acetate 5 Emulsion composition of multilamella vesicles consisting of%, vitamin C 1.00%, linoleic acid 1%, meadowfoam oil 2%, amaranth oil 0.5%, dimethicone 15%, purified water Composition of lotion containing multilamella vesicle of claim 1 A composition of skin toner containing the multilamella vesicle of claim 1