CN117412744A - Skin care product and process for its production - Google Patents
Skin care product and process for its production Download PDFInfo
- Publication number
- CN117412744A CN117412744A CN202280039737.7A CN202280039737A CN117412744A CN 117412744 A CN117412744 A CN 117412744A CN 202280039737 A CN202280039737 A CN 202280039737A CN 117412744 A CN117412744 A CN 117412744A
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- China
- Prior art keywords
- equal
- lipid
- lipid particle
- fatty acids
- wax
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
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Classifications
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/36—Carboxylic acids; Salts or anhydrides thereof
- A61K8/361—Carboxylic acids having more than seven carbon atoms in an unbroken chain; Salts or anhydrides thereof
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- A—HUMAN NECESSITIES
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Abstract
The present invention is a lipid particle and a method for producing the same. The lipid particle comprises a matrix and at least one antioxidant incorporated into the matrix. In one embodiment of the invention, the lipid particles are used to locally inhibit ROS in the skin of a patient ("reactive oxygen species"). In one embodiment of the invention, a skin care product comprising the lipid particles is used for topical inhibition of ROS in the skin of a patient.
Description
Technical Field
The present invention relates to lipid particles, in particular for use in skin care products.
Background
Recently, skin care products such as creams, lotions or essences have become widespread, which consist of a fluid substance, usually a gel, incorporating lipid particles containing one or more molecules of cosmetic active ingredients.
Examples of such active ingredients are vitamins, such as for example vitamin A, C, E and its derivatives, coenzyme Q10, minerals, antioxidants, natural extracts and peptides.
Among the factors known to cause skin damage are the so-called "free radicals". These are responsible for lipid peroxidation. Among these, so-called ROS (reactive oxygen species), which contain electron-deficient molecular oxygen ("peroxy"), in particular, cause damage in excess, the most serious of which is premature aging of the skin.
During lipid peroxidation, lipids containing unsaturated fatty acids and esters thereof are oxidized directly by molecular oxygen, and damage can propagate through the chain reaction, since electron-deprived lipids tend to re-integrate lost by subtracting electrons from neighboring molecules, even involving proteins and DNA of the central core.
Thus, after these reactions, some possible damage is: lipid peroxidation, peroxidation of amino acids and proteins, enzymatic changes and damage to protein structure.
ROS produced in mitochondria can react and directly damage mtDNA and other mitochondrial components. ROS can also damage nuclear DNA.
For all these reasons, oxidative modification of some proteins may be an important aging factor. Thus, products containing antioxidant active ingredients capable of interacting with ROS and inhibiting its activity are known and widespread. For example, these products are commercialized as:
-derm internes 10% pure vitamin C (L' Or al Paris),
resveratrol B E antioxidant night concentrates (Skincents)
High-grade multiple-protection antioxidant skin lotion SPF 15 (Estee Lauder)
Anteolos AOX daytime antioxidant essence (La Roche-Posay) containing sunscreens
However, products available today for reducing ROS in skin have limitations. For example, these products, while containing active ingredients that are sensitive to ROS, have the disadvantage that the active ingredients are in a free state or incorporated into lipid particles with a stable matrix, i.e. a containment envelope (containment envelope), designed to protect the content or to carry the content in a controlled and specific manner but without affinity for ROS.
Such matrices are generally composed mainly of saturated polymers and/or lipids that are stable to oxidation (Comunian et al, "Protection and controlled release of vitamin C by different micro/nanocarriers", crit Rev Food Sci Nutr.2020, 12 months 22; 1-22).
The purpose of the matrix used in the products known so far is to protect the incorporated active ingredients, making them more bioavailable, i.e. able to reach the circulatory system, and to increase skin penetration and gradual release.
For these reasons, however, the activity of the active ingredient is equally represented over the whole area of skin to which the product is applied, irrespective of the local concentration of ROS, and not preferentially in areas of higher ROS concentration, which would be of greater demand.
Furthermore, in order to produce similar products, it is necessary to use organic solvents such as methylene chloride, chloroform, diethyl ether and ether-methanol mixtures, which may be toxic, or to use high temperatures above 60℃and up to 100℃ (Ghasemieh et al, "Solid lipid nanoparticles and nanostructured lipid carriers as novel drug delivery systems: applications, advantages and disadvantages", res Pharm Sci.2018, month 8; 13 (4): 288-303). This results in an economically and energy-intensive process.
Disclosure of Invention
In view of the limitations of the prior art described above, a primary object of the present invention is to provide a skin care product and method of manufacturing the same that can improve upon the prior art with respect to one or more of the above aspects.
Within this aim, an object of the present invention is to provide lipid particles which have a high sensitivity to ROS and which are capable of delivering active ingredients incorporated therein to areas with ROS, and in particular those areas with a higher ROS concentration.
It is another object of the present invention to provide a skin care product that has a greater affinity for ROS than similar products known to date. It is another object of the present invention to provide a method for manufacturing a skin care product that does not use organic solvents and does not use high temperatures.
It is a primary object of the present invention to provide a skin care product and a method of manufacturing the same that is highly reliable, relatively easy to implement and cost competitive.
This task, as well as these and other objects, which will become apparent later, are achieved by lipid particles, wherein the particles each comprise:
- (a) a substrate comprising:
(i) From greater than or equal to 20 wt% to less than or equal to 60 wt% of a lipid component based on the total weight of the lipid particle, the lipid component characterized by a melting temperature of greater than or equal to 40 ℃ to less than or equal to 55 ℃;
(ii) From greater than or equal to 20 wt% to less than or equal to 30 wt% of one or more unsaturated fatty acids, based on the total weight of the lipid particle;
(iii) From greater than or equal to 10 wt% to less than or equal to 12 wt% of one or more excipients selected from the group consisting of surfactants, suspending agents, humectants, and mixtures thereof, based on the total weight of the lipid particle;
and (b) at least one antioxidant incorporated into the matrix.
The aim and objects of the invention are also achieved by a method for preparing a lipid particle according to the invention, comprising the steps of:
(i) Melting the lipid component;
(ii) Dispersing one or more unsaturated fatty acids in the fusogenic lipid component of step (i);
(iii) Dispersing in water preheated to a temperature of greater than or equal to 40 ℃ to less than or equal to 50 ℃ the following:
-at least one antioxidant; and
-one or more excipients;
(iv) Adding the dispersion obtained in step (ii) to the aqueous dispersion obtained in step (iii) under stirring to obtain an emulsion;
(v) Cooling the emulsion obtained in step (iv) to a temperature of greater than or equal to 5 ℃ to less than or equal to 15 ℃ to obtain an emulsion consisting of lipid particles in the aqueous phase.
Furthermore, the task and object of the present invention are also achieved by lipid particles for the topical treatment of a condition associated with ROS ("reactive oxygen species") accumulation in the skin of a patient, wherein the lipid particles each comprise:
(a) A substrate, the substrate comprising:
(i) Lipid component;
(ii) One or more unsaturated fatty acids;
(iii) One or more excipients selected from the group consisting of surfactants, suspending agents, humectants, and mixtures thereof;
and
(b) At least one antioxidant incorporated into the matrix.
The aim and objects of the present invention are also achieved by a skin care product comprising the lipid particle according to the present invention.
Finally, the objects and purposes of the present invention are also achieved by a lipid particle according to the present invention or a skin care product according to the present invention for the topical treatment of a condition associated with ROS accumulation in the skin of a patient.
Other features and advantages of the present invention will become apparent from the following detailed description.
Detailed Description
In a first aspect, the present invention relates to lipid particles, wherein the particles each comprise a matrix and at least one antioxidant incorporated therein.
The matrix of the lipid particle of the invention comprises from greater than or equal to 20 wt% to less than or equal to 60 wt% of a lipid component having a melting temperature of from greater than or equal to 40 ℃ to less than or equal to 55 ℃, based on the total weight of the lipid particle.
Advantageously, the aforementioned melting temperature is closer to the temperature of the skin (37 ℃) than the melting temperature of other waxes used to produce lipid particles, such as microcrystalline wax, carnauba wax, beeswax, which have melting temperatures higher than 65 ℃.
In a preferred embodiment, the lipid component is a mixture of at least two of the following: mimosa wax (acacia decurrens)), jojoba seed wax, sunflower seed wax, polyglycerol, pentaerythritol distearate and transesterification products of polyglycerol with at least one wax selected from jojoba wax, mimosa wax and sunflower seed wax.
Furthermore, the matrix of the lipid particle according to the invention comprises (ii) from greater than or equal to 20 wt% to less than or equal to 30 wt% based on the total weight of the lipid particle of one or more unsaturated or preferably polyunsaturated fatty acids, which provide the lipid particle of the invention with the property of interacting with ROS by having a high affinity for ROS, thereby releasing the active ingredient in a targeted manner. Thus, the lipid particles of the present invention have a matrix characterized by a high affinity for ROS.
In the present specification, the term "affinity" means the tendency of active ingredients or lipid particles comprising them to have interactions with ROS.
As described above, ROS affinity is measured by iodine index.
As mentioned above, lipid particles commonly used today have an oxidation stable matrix.
In the present specification, the expression "stable matrix" means a matrix stable to oxidation, and in the case of a lipid matrix, this means an iodine index of less than 60g iodine per 100g, wherein the iodine index is measured according to ASTM D1959-97.
In a preferred embodiment, the matrix of lipid particles according to the invention has an iodine index higher than or equal to 60g iodine per 100g, wherein the iodine index is measured according to ASTM D1959-97.
The matrix of the particles of the present invention comprises one or more unsaturated fatty acids, preferably selected from the group consisting of C16-C24 unsaturated fatty acids and mixtures thereof. In a preferred embodiment, the one or more unsaturated fatty acids are selected from the group consisting of linoleic acid, linolenic acid, alpha-linolenic acid, oleic acid, and mixtures thereof.
Preferably, the one or more unsaturated fatty acids of the matrix comprise at least 60 wt% polyunsaturated fatty acids based on the total weight of unsaturated fatty acids.
The lipid particle of the present invention comprises at least one antioxidant incorporated into a matrix.
Preferably, the at least one antioxidant is selected from BHT (butylhydroxytoluene), vitamin E, vitamin C, BHA (butylhydroxyanisole), polyphenols, carotenoids, superoxide dismutase and bisulphites.
In the context of the present specification, the term "vitamin C" refers to ascorbic acid and its derivatives, such as, for example, sodium ascorbyl phosphate, ascorbyl tetraisopalmitate, 3-O-cetyl ascorbic acid and ascorbyl glucoside.
Thus, a matrix enriched in lipid particles of unsaturated and polyunsaturated fatty acids that provide high affinity for ROS allows to selectively deliver antioxidants incorporated therein and act as "scavengers" in ROS-enriched skin areas, allowing to neutralize them.
Preferably, in the lipid particle of the present invention, the content of the at least one antioxidant is comprised between 5% and 20% by weight based on the total weight of the lipid particle.
The matrix of the lipid particle according to the present invention further comprises (iii) from greater than or equal to 10 wt% to less than or equal to 12 wt% of one or more excipients selected from the group consisting of surfactants, suspending agents, wetting agents and mixtures thereof, based on the total weight of the lipid particle.
Preferably, the at least one excipient is selected from polysorbates, polyacrylates, xanthan gums, alkyl glucosides and glycols.
In addition, the lipid particle of the present invention may further comprise one or more active ingredients incorporated into the matrix, wherein the one or more active ingredients are selected from vitamins, peptides, minerals, growth factors, and natural extracts.
The active ingredients have the functions of restoring physiological balance, repairing and stimulating the mechanism of self-repair of skin damaged by excessive concentration of ROS.
The term "active ingredient" in this specification refers to a substance that is biologically active or affects the appearance and condition of the skin.
In the present specification, the expression "bioactive" means that such a substance has an effect on biological tissues (in this case skin), or has a cosmetic effect on them.
In a second aspect, the present invention relates to a method for preparing a lipid particle according to the present invention, the method comprising the steps of:
(i) Melting the lipid component;
(ii) Dispersing the one or more unsaturated fatty acids in the fusogenic lipid component of step (i);
(iii) Dispersing in water preheated to a temperature of greater than or equal to 40 ℃ to less than or equal to 50 ℃ the following:
-said at least one antioxidant; and
-said one or more excipients;
(iv) Adding the dispersion obtained in step (ii) to the aqueous dispersion obtained in step (iii) under stirring to obtain an emulsion;
(v) Cooling the emulsion obtained in step (iv) to a temperature of greater than or equal to 5 ℃ to less than or equal to 15 ℃ to obtain an emulsion consisting of lipid particles in the aqueous phase.
In step (iv), the stirring is preferably carried out at a constant speed of 1000 to 8000 revolutions per minute.
Preferably, prior to step (v), the emulsion obtained in step (iv) is sieved through a mesh having pores ranging in size from greater than or equal to 0.1 μm to less than or equal to 50 μm, obtaining an emulsion consisting of lipid particles in the aqueous phase ranging in size from greater than or equal to 0.1 μm to less than or equal to 50 μm. After cooling in step (v), the emulsion may then be dried in vacuo at a temperature below 40 ℃ and/or stabilized by adding preservatives like for example sodium benzoate, potassium sorbate, isothiazolinones, phenoxyethanol, formaldehyde scavengers, chelators.
In a preferred embodiment of the method according to the invention, the lipid component is a mixture of at least two of the following: transesterification products of mimosa wax (vitex negundo), jojoba seed wax, sunflower seed wax, polyglycerol, pentaerythritol distearate, polyglycerol 3 with at least one wax selected from the group consisting of jojoba wax, mimosa wax and sunflower seed wax;
the choice of the above wax mixture advantageously allows the preparation of particles by a process that does not require high temperatures or organic solvents.
In a preferred embodiment, the process according to the invention does not comprise the use of organic solvents.
The lipid particles of the invention obtained as described above can then be incorporated into skin care products selected from the group consisting of lotions, creams and lotions, and they are mixed with said skin care products at a temperature lower than or equal to 40 ℃ and at a speed of 100-200 revolutions per minute until completely homogenized.
The invention therefore also relates to a skin care product comprising the lipid particle according to the invention. The product, preferably selected from the group consisting of a concentrate, a cream and a lotion, is optionally packaged in an airtight container, protected from ROS formation inside it.
The present invention also relates to the above lipid particles and the above skin care products for the topical treatment of conditions associated with ROS accumulation in the skin of a patient.
Skin conditions associated with ROS accumulation include premature aging, loss of elasticity, loss of hydration, hyperpigmentation, skin discoloration, acne, and imbalance in physiological balance.
The invention also relates to lipid particles for use in the topical treatment of a condition associated with ROS accumulation in the skin of a patient, wherein each lipid particle comprises:
(a) A substrate, the substrate comprising:
(i) Lipid component;
(ii) One or more unsaturated fatty acids;
(iii) One or more excipients selected from the group consisting of surfactants, suspending agents, humectants, and mixtures thereof;
and
(b) At least an antioxidant, which is incorporated into the matrix.
The present invention of course also relates to a method of treating a condition associated with ROS accumulation in the skin of a patient by administering the above lipid particle or skin care product to the patient.
The invention will now be described with reference to the following non-limiting examples.
Example 1: preparation of lipid particles according to the invention.
To prepare 1kg of a composition comprising the lipid particle of the present invention for use as an intermediate in the preparation of cosmetics, the procedure is as follows:
(i) 90g of blend of jojoba wax, mimosa wax and sunflower seed waxMB, ACTICIRE-GATTE FOSSE) and 30g of natural polyunsaturated fatty acids obtained from safflower oil (Vitamin F for, CLR Berlin) were melted in a beaker under magnetic stirring at 200rpm by heating at a temperature of 55℃for 10 minutes until the phases were completely melted;
(ii) Adding 30g of a mixture of natural polyunsaturated fatty acids obtained from safflower oil (vitaminf for, CLR Berlin) to the molten lipid mixture obtained in step (i) while magnetically stirring at 200rpm, while maintaining the temperature at 55 ℃, until a homogeneous "fat" molten mixture is obtained;
(iii) An aqueous dispersion was prepared by adding 758ml of water heated to 45 ℃ followed by stirring (500 rpm,10 min):
-20g of decyl glucoside, the concentration of which is chosen,
100g of sodium ascorbyl phosphate,
-2g of hyaluronic acid;
(iv) Adding the aqueous dispersion prepared in point (iii) to the fat mixture prepared in point (ii) by maintaining the temperature at 48 ℃ and stirring at 3500rpm for 10 minutes to obtain an emulsion of lipid particles in the aqueous phase;
(iv-a) sieving the emulsion obtained in step (iv) through a mesh having pores with a diameter of 25 μm to obtain an emulsion of lipid particles with a diameter of at most 25 μm in an aqueous phase;
(v) Cooling the emulsion obtained in step (iv-a) to 10 ℃ by means of a water bath to accelerate the solidification of the lipid fraction;
indeed, it has been found that the present invention achieves the intended aim and objects by producing lipid particles and skin care products which are characterized by a high affinity for ROS and are capable of delivering active ingredients incorporated in the matrix of the lipid particles to areas with ROS, and in particular those areas with a higher ROS concentration.
Skin care products incorporating lipid particles according to the invention advantageously have a greater affinity for ROS than similar products on the market today.
Furthermore, the present invention perfects a method for manufacturing a skin care product that does not include the use of organic solvents and the use of high temperatures.
The invention thus conceived is susceptible of numerous modifications and variations, all of which are within the scope of the inventive concept; furthermore, all the details may be replaced by other technically equivalent elements.
In fact, the materials employed may be any according to the requirements and the state of the art, provided that they are compatible with the specific use, as well as the contingent shapes and dimensions.
Claims (14)
1. Lipid particles, wherein each particle comprises:
- (a) a substrate comprising:
(i) From greater than or equal to 20 wt% to less than or equal to 60 wt% of a lipid component, based on the total weight of the lipid particle, the lipid component having a melting temperature of greater than or equal to 40 ℃ to less than or equal to 55 ℃;
(ii) From greater than or equal to 20 wt% to less than or equal to 30 wt% of one or more unsaturated fatty acids, based on the total weight of the lipid particle;
(iii) From greater than or equal to 10% to less than or equal to 12% by total weight of the lipid particle of one or more excipients selected from the group consisting of surfactants, suspending agents, humectants, and mixtures thereof;
and (b) at least one antioxidant incorporated into the matrix.
2. The lipid particle of claim 1, wherein the lipid component is a mixture of at least two of: transesterification products of mimosa wax (vitex virginiana), jojoba seed wax, sunflower seed wax, polyglycerol, pentaerythritol distearate and polyglycerol with at least one wax selected from the group consisting of jojoba wax, mimosa wax and sunflower seed wax.
3. The lipid particle of claim 1 or 2, wherein the matrix has an iodine index of greater than or equal to 60g iodine per 100g, wherein the iodine index is measured according to ASTM D1959-97.
4. The lipid particle of one or more of the preceding claims, wherein the one or more unsaturated fatty acids comprise at least 60 wt.% polyunsaturated fatty acids based on the total weight of the unsaturated fatty acids.
5. Lipid particle according to one or more of the preceding claims, wherein the content of the at least one antioxidant is from greater than or equal to 5 wt% to less than or equal to 20 wt%, based on the total weight of the lipid particle.
6. Lipid particle according to one or more of the preceding claims, wherein the one or more unsaturated fatty acids are selected from the group consisting of C16-C24 fatty acids and mixtures thereof.
7. Lipid particle according to one or more of the preceding claims, wherein the at least one excipient is selected from polysorbates, polyacrylates, xanthan gums, alkyl glucosides and glycols.
8. Lipid particle according to one or more of the preceding claims, wherein the at least one antioxidant is selected from BHT (butylhydroxytoluene), vitamin E, vitamin C, BHA (butylhydroxyanisole), polyphenols, carotenoids, superoxide dismutase and bisulphite.
9. Lipid particle according to one or more of the preceding claims, further comprising one or more active ingredients incorporated into the matrix, wherein the one or more active ingredients are selected from vitamins, peptides, minerals, growth factors and natural extracts.
10. A process for preparing a lipid particle according to the invention, the process comprising the steps of:
(i) Melting the lipid component;
(ii) Dispersing one or more unsaturated fatty acids in the fusogenic lipid component of step (i);
(iii) Dispersing in water preheated to a temperature of greater than or equal to 40 ℃ to less than or equal to 50 ℃ the following:
-at least one antioxidant: and
-one or more excipients:
(iv) Adding the dispersion obtained in step (ii) to the aqueous dispersion obtained in step (iii) with stirring to obtain an emulsion:
(v) Cooling the emulsion obtained in step (iv) to a temperature of greater than or equal to 5 ℃ to less than or equal to 15 ℃ to obtain an emulsion consisting of lipid particles in the aqueous phase.
11. The method of claim 10, wherein the method does not include the use of an organic solvent.
12. Lipid particles for use in the topical treatment of a condition associated with ROS ("reactive oxygen species") accumulation in the skin of a patient, wherein each lipid particle comprises:
(a) A substrate, the substrate comprising:
(i) Lipid component;
(ii) One or more unsaturated fatty acids:
(iii) One or more excipients selected from the group consisting of surfactants, suspending agents, humectants, and mixtures thereof;
and
(b) At least one antioxidant incorporated into the matrix.
13. Skin care product comprising the lipid particle according to one or more of claims 1-9.
14. Lipid particles according to one or more of claims 1-9 or a skin care product according to claim 13 for use in the topical treatment of a condition associated with ROS accumulation in the skin of a patient.
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| IT102021000014330 | 2021-06-01 | ||
| IT102021000014330A IT202100014330A1 (en) | 2021-06-01 | 2021-06-01 | Skin care product and process for making it. |
| PCT/US2022/031333 WO2022256256A1 (en) | 2021-06-01 | 2022-05-27 | Skin care product and procedure for its production |
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| CN117412744A true CN117412744A (en) | 2024-01-16 |
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| LU85130A1 (en) * | 1983-12-12 | 1985-09-12 | Oreal | AQUEOUS COSMETIC OR ANHYDROUS COMPOSITION CONTAINING A FATTY PHASE BASED ON SHEA OIL |
| DE10253042A1 (en) * | 2002-11-14 | 2004-06-03 | Wacker-Chemie Gmbh | Cosmetic preparation containing a complex of cyclodextrin and vitamin F. |
| US9056050B2 (en) * | 2009-04-13 | 2015-06-16 | Curemark Llc | Enzyme delivery systems and methods of preparation and use |
| EP3154529B1 (en) * | 2014-06-10 | 2020-07-08 | Capsugel Belgium NV | Orally disintegrating tablet containing solid lipid particles and methods for their preparation and use |
| JP6602834B2 (en) * | 2014-06-30 | 2019-11-06 | ターベダ セラピューティクス インコーポレイテッド | Targeted conjugates and particles and formulations thereof |
| CN105816423B (en) * | 2016-03-16 | 2018-07-20 | 福建天泰医药科技有限公司 | edaravone dosage form |
| US20190201350A1 (en) * | 2016-08-15 | 2019-07-04 | Corr-Jensen Inc. | Time release of fat-soluble actives |
| IT201900022764A1 (en) * | 2019-12-03 | 2021-06-03 | Skb Llc | SKIN CARE PRODUCT AND PROCEDURE FOR ITS REALIZATION |
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2021
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| AU2022284776A1 (en) | 2023-11-09 |
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| JP2024520341A (en) | 2024-05-24 |
| KR20240017376A (en) | 2024-02-07 |
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