CN114042006B - Centella asiatica ethosome and preparation method thereof - Google Patents
Centella asiatica ethosome and preparation method thereof Download PDFInfo
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- CN114042006B CN114042006B CN202111288084.XA CN202111288084A CN114042006B CN 114042006 B CN114042006 B CN 114042006B CN 202111288084 A CN202111288084 A CN 202111288084A CN 114042006 B CN114042006 B CN 114042006B
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- Prior art keywords
- ethosome
- mixture
- madecassoside
- centella asiatica
- mixing
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- 235000004032 Centella asiatica Nutrition 0.000 title claims abstract description 32
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- 239000000203 mixture Substances 0.000 claims description 36
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- 125000000913 palmityl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 229940101267 panthenol Drugs 0.000 description 1
- 235000020957 pantothenol Nutrition 0.000 description 1
- 239000011619 pantothenol Substances 0.000 description 1
- 229940100460 peg-100 stearate Drugs 0.000 description 1
- WXZMFSXDPGVJKK-UHFFFAOYSA-N pentaerythritol Chemical compound OCC(CO)(CO)CO WXZMFSXDPGVJKK-UHFFFAOYSA-N 0.000 description 1
- 229920000435 poly(dimethylsiloxane) Polymers 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 239000002244 precipitate Substances 0.000 description 1
- 230000001681 protective effect Effects 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- 230000008439 repair process Effects 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 231100000241 scar Toxicity 0.000 description 1
- 229940010747 sodium hyaluronate Drugs 0.000 description 1
- YWIVKILSMZOHHF-QJZPQSOGSA-N sodium;(2s,3s,4s,5r,6r)-6-[(2s,3r,4r,5s,6r)-3-acetamido-2-[(2s,3s,4r,5r,6r)-6-[(2r,3r,4r,5s,6r)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2- Chemical compound [Na+].CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 YWIVKILSMZOHHF-QJZPQSOGSA-N 0.000 description 1
- 229940032094 squalane Drugs 0.000 description 1
- 238000013112 stability test Methods 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 210000000434 stratum corneum Anatomy 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- OULAJFUGPPVRBK-UHFFFAOYSA-N tetratriacontyl alcohol Natural products CCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCO OULAJFUGPPVRBK-UHFFFAOYSA-N 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 238000013271 transdermal drug delivery Methods 0.000 description 1
- 150000003648 triterpenes Chemical class 0.000 description 1
- 239000013598 vector Substances 0.000 description 1
- 230000002087 whitening effect Effects 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 238000000733 zeta-potential measurement Methods 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- 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
- A61K8/63—Steroids; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
- A61K8/14—Liposomes; Vesicles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- 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
- A61K8/34—Alcohols
- A61K8/345—Alcohols containing more than one hydroxy group
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- 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
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
- A61K8/4993—Derivatives containing from 2 to 10 oxyalkylene groups
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- 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
- A61K8/55—Phosphorus compounds
- A61K8/553—Phospholipids, e.g. lecithin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/10—General cosmetic use
Abstract
The invention discloses a centella asiatica ethosome and a preparation method and application thereof. The ethosome comprises the following raw material components: 0.5-12wt% of centella asiatica, 2-15wt% of phospholipids, 10-30wt% of water, 15-30wt% of moisturizer, 5-30wt% of cosurfactant, 20-30wt% of polyhydric alcohol and 0-3wt% of preservative.
Description
Technical Field
The invention relates to the technical field of cosmetics, in particular to a centella asiatica ethosome and application thereof in cosmetics.
Background
Centella asiatica is a perennial herb of centella (Centella Asialica) of Umbelliferae. The extract contains various alpha-amyrin alcohol type triterpene components, wherein asiaticoside and madecassoside are water-soluble, and asiatic acid and madecassoside are generally only used in low dosage due to poor water solubility, and cannot achieve the effect to the greatest extent.
The ethosome is a novel transdermal drug delivery carrier, and the field is urgent to provide a quadriplex asiatica ethosome which can be used for compositely wrapping asiatic acid, asiaticoside, madecassic acid and madecassoside, is convenient to use, and can be widely used in various cosmetic formulas and production.
Disclosure of Invention
The invention aims to provide a centella asiatica ethosome.
In a first aspect of the invention, there is provided a centella asiatica ethosome, comprising the following raw material components, based on the total weight of the ethosome:
in another embodiment, the raw material component further comprises 15-30wt% of humectant.
In another embodiment, the Phosphatidylcholine (PC) content is not less than 50%, preferably not less than 60% by total weight of the phospholipid.
In another embodiment, the polyol is ethoxydiglycol and/or propylene glycol.
In another embodiment, the co-surfactant is polysorbate-80 and/or lysophosphatidylcholine.
In another embodiment, the preservative is selected from one or more of the following: p-hydroxyacetophenone, 1, 2-hexanediol, pentanediol, octanediol, phenoxyethanol, ethylhexyl glycerol, and p-anisic acid.
In another embodiment, the humectant is selected from one or more of the following: glycerol, diglycerol and polyglycerol-3.
In another embodiment, the starting components of the ethosome are 0.5-12wt% centella asiatica, 2-15wt% phospholipids, 10-30wt% water, 15-30wt% humectants, 5-30wt% co-surfactants, 20-30wt% polyols, and 0-3wt% preservatives.
In another embodiment, the ethosome is a pale yellow to yellow homogeneous liquid or a powder that continues to be spray dried.
In another embodiment, the ethosome particle size is 10-200nm, PDI <0.3, zeta potential absolute value is not less than 30mV.
In a second aspect of the present invention, there is provided a method for preparing an ethosome according to the present invention as described above, the method comprising the steps of:
(1) Mixing centella asiatica, phospholipids and co-surfactant to obtain mixture 1;
(2) Mixing the mixture 1 with a polyol to obtain a mixture 2;
(3) Mixing the mixture 2 with water, and homogenizing to obtain a mixture 3; and
(4) The mixture 3 was circulated 2 to 8 times through a homogenizer at 600 to 1000bar to obtain the ethosomes provided by the present invention as described above.
In another embodiment, step (3) is to homogenize mixture 2 after mixing with water and a humectant to obtain mixture 3.
In another embodiment, step (4) may further comprise adding a preservative after the homogenizer cycle.
In a third aspect of the invention there is provided the use of an ethosome as provided herein above for the preparation of a dermatological product.
In a fourth aspect of the invention there is provided a dermatological product comprising an ethosome as provided herein above and a cosmetically acceptable carrier.
In a fifth aspect of the present invention there is provided a method of preparing a dermatological product as provided by the present invention as described above, the method comprising the steps of: the ethosomes provided by the invention as described above are mixed with a cosmetically acceptable carrier to obtain the dermatological product provided by the invention as described above.
Accordingly, the invention provides a quadriplex asiaticoside plastid which is used for compositely wrapping asiatic acid, asiaticoside, madecassic acid and madecassoside, is convenient to use, and can be widely used in various cosmetic formulas and production.
Detailed Description
Through extensive and intensive studies, the inventor obtains a compound formula by selecting proper phospholipids and polyalcohols, and prepares the ethosome convenient to use by adopting a high-pressure process, thereby effectively solving the application problems of asiatic acid and madecassic acid. The present invention has been completed on the basis of this finding.
As used herein, "centella asiatica" refers to a mixture of centella asiatica (CAS registry number 464-92-6), asiaticoside (CAS registry number 16830-15-2), madecassoside (CAS registry number 18449-41-7) and madecassoside (CAS registry number 34540-22-2), wherein the weight ratio of centella asiatica to madecassoside is 1:1, the weight ratio of asiaticoside to madecassoside is 1-3:1, the weight ratio of the sum of asiaticoside and madecassoside to the sum of asiatic acid and madecassoside is 2-4:3, and the purities of centella asiatica, asiaticoside and madecassoside are respectively greater than or equal to 90% (HPLC). HPLC assays can be performed according to methods conventional in the art, such as, but not limited to, "asiatic acid: isolation, purification and content determination of centella asiatica acid (university of capital medical science, 2011,32 (4): 538-540) "; "madecassic acid: the method for separating and measuring madecassic acid in centella asiatica total aglycone by using a beta-cyclodextrin mobile phase additive method (chromatograph, 2007,25 (3): 316-318) "; "asiaticoside and madecassoside: one test method for multiple evaluation simultaneously measures 3 components (Chinese patent medicine, 2020,42 (9): 2280-2284) "in centella asiatica total glycosides and 2 preparations thereof.
As used herein, "phospholipid" refers to glycerophospholipids formed by the esterification of the hydroxyl groups on C1 and C2 of glycerol with fatty acid, the esterification of the hydroxyl group on C3 with phosphoric acid, and the linkage of phosphoric acid with a polar alcohol (X-OH), specifically phosphatidylcholine; in one embodiment of the invention, the Phosphatidylcholine (PC) content is not less than 50wt%, preferably not less than 60wt%, more preferably 60-100wt%, based on the total weight of the phospholipids; such as, but not limited to, phospholipids having a PC content of 90% or more and hydrogenated lecithins having a PC content of 60% or more.
As used herein, "room temperature" refers to 15-40 ℃, preferably 20-35 ℃, such as, but not limited to, 25-30 ℃, and the like.
As used herein, the term "cosmetically acceptable carrier" refers to a carrier that makes the cosmetic or personal care product applicable, including various excipients and diluents, which are not per se essential active ingredients, and which are not overly toxic after application. Suitable vectors are well known to those of ordinary skill in the art. A sufficient discussion of cosmetically acceptable excipients can be found in cosmetic hygiene specifications 2015. Such carriers in the ethosomes may include moisturizers, emulsifiers, thickeners, chelators, emollients, and the like. Such as, but not limited to, water, 1, 2-hexanediol, p-hydroxyacetophenone, butanediol, panthenol, dipotassium glycyrrhizinate, arginine, glycerol, betaine, sodium hyaluronate, propylene glycol, glycerol stearate/PEG-100 stearate, glycerol stearate, xanthan gum, hydroxyethyl cellulose, carbomer, disodium EDTA, isohexadecane, isooctyl palmitate, cetostearyl alcohol, polydimethylsiloxane, citric acid or salts thereof, behenyl alcohol, behenyl polyether, cetyl polyether, pentaerythritol tetra (ethylhexanoate), squalane, cetyl ethyl hexanoate, and the like.
The invention provides an ethosome, which comprises the raw material components of centella asiatica, phospholipid, water, auxiliary surfactant and polyalcohol, further comprises humectant, further comprises preservative; in one embodiment of the invention, the amounts of the components are, based on the total weight of the feed components:
in one embodiment of the invention, the amounts of the components are, based on the total weight of the feed components:
in one embodiment, the raw material composition contains 2-6wt% of centella asiatica; and/or 5-12wt% of a phospholipid; and/or 10-20wt% water; and/or 15-25wt% humectant; and/or 12-30wt% of a co-surfactant; and/or 20-25wt% of a polyol; and/or 0-2wt% preservative.
In one embodiment of the present invention, centella asiatica is obtained by uniformly mixing centella asiatica, asiaticoside, madecassic acid and madecassoside at room temperature.
The phospholipid which can be used in the present invention is a phospholipid mainly comprising phosphatidylcholine.
In one embodiment of the present invention, deionized water having a pH of 4-6 is used.
The present invention can use a protective substance capable of forming an oil film on the skin surface as a moisturizing agent, or can use a moisturizing agent capable of enhancing the water absorption and water binding ability of the stratum corneum. In one embodiment of the present invention, the humectant used is selected from one or more of the following: glycerol, diglycerol and polyglycerol-3.
In the invention, instead of glycerin as a polyol raw material component, ethoxydiglycol and/or propylene glycol are selected as specific polyol raw material components; wherein the propylene glycol can be 1, 3-propylene glycol and/or 1, 2-propylene glycol.
The raw material components of the ethosome provided by the invention must contain auxiliary surfactants, namely polysorbate-80 and/or hydrogenated lysophosphatidylcholine (the PC content is not less than 60%).
The preservative which can be used in the present invention is selected from one or two or more of the following: p-hydroxyacetophenone, 1, 2-hexanediol, pentanediol, octanediol, phenoxyethanol, ethylhexyl glycerol, and p-anisic acid.
In one embodiment of the present invention, the starting components of the ethosome may be composed of centella asiatica, phospholipids, water, humectants, co-surfactants, and polyols; can also be composed of centella asiatica, phospholipid, water, humectant, cosurfactant, polyalcohol and preservative.
The ethosome provided by the invention is light yellow to yellow uniform liquid; the particle size can be controlled within the range of 10-200nm, PDI is less than 0.3, zeta potential absolute value is not less than 30mv, and centrifugation is not layered and separated out at 10000rpm for 30 minutes; the product is stored at 45 ℃ for three months at normal temperature and 5 ℃ respectively, does not delaminate or precipitate, and has good stability.
The preparation method of the ethosome provided by the invention comprises the following steps:
firstly, mixing centella asiatica, phospholipid and a cosurfactant to obtain a mixture 1;
step two, evenly mixing the polyol with the mixture 1 to obtain a mixture 2;
thirdly, uniformly mixing the humectant with the mixture 2 and homogenizing to obtain a mixture 3;
fourth, the mixture 3 is subjected to high-pressure homogenization cycle treatment, thereby obtaining the ethosome of the present invention.
In one embodiment of the present invention, the phospholipid and the cosurfactant are mixed and added to centella asiatica in the first step, for example, the phospholipid and the cosurfactant are uniformly mixed and heated to 80-90 ℃ to completely dissolve the phospholipid and then added to centella asiatica; complete dissolution may be achieved by methods conventional in the art, such as, but not limited to, stirring, sonication, high speed dispersion, and the like.
In one embodiment of the invention, the polyol is added to mixture 1 in the second step described above, and the polyol is added to mixture 1 and mixed uniformly while maintaining the temperature of the first step (e.g., 80-90 ℃); the mixing may be made uniform by methods conventional in the art such as, but not limited to, stirring, sonication, high speed dispersion, and the like.
In one embodiment of the present invention, in the third step, water and humectant are uniformly mixed at 80-85 ℃ and then added into the mixture 2; homogenizing at 5000-10000rpm for 2-10 min.
In one embodiment of the present invention, the fourth step is carried out at 80-90℃and may be carried out by circulating through a high-pressure homogenizer 2-8 times at 600-1000 bar; preferably, the exit temperature of the high pressure homogenizer is ensured to obtain the ethosome or primary ethosome of the present invention at 70-80 ℃.
In one embodiment of the present invention, the fourth step is to cool the primary ethosome obtained after the high-pressure homogenizing cycle treatment, add a preservative, and cool the primary ethosome to room temperature to obtain the ethosome provided by the present invention.
The ethosome provided by the invention can be used for manufacturing skin products. In the process of manufacturing the skin product, the ethosome provided by the invention is generally used as a single phase, or can be used as a component in an oil phase and added into other phases or a mixture of phases.
The skin products comprise skin care products and cosmetics, and the skin products are not limited to specific dosage forms, and can be developed in forms of skin softening water, nourishing lotion, massage cream, nourishing cream, facial mask, essence, ointment, color make-up BASE, foundation cream, emulsion, gel, face cream, spray and the like.
Notwithstanding that the numerical ranges and parameters setting forth the broad scope of the invention are approximations, the numerical values set forth in the specific examples are reported as precisely as possible. However, any numerical value inherently contains certain standard deviations found in their respective testing measurements. As used herein, "about" generally means that the actual value is within plus or minus 10%, 5%, 1% or 0.5% of a particular value or range. Alternatively, the term "about" means that the actual value falls within an acceptable standard error of the average value, as determined by one of ordinary skill in the art. Except in the experimental examples, or where otherwise explicitly indicated, all ranges, amounts, values, and percentages used herein (e.g., to describe amounts of materials, lengths of time, temperatures, operating conditions, ratios of amounts, and the like) are to be understood to be modified by the term "about". Accordingly, unless indicated to the contrary, the numerical parameters set forth in the present specification and attached claims are approximations that may vary depending upon the desired properties. At least these numerical parameters should be construed as the number of significant digits and by applying ordinary rounding techniques.
Unless defined otherwise herein, the meanings of scientific and technical terms used herein are the same as commonly understood and used by one of ordinary skill in the art. Furthermore, as used in this specification, the singular noun encompasses the plural version of the noun without conflict with the context; plural nouns as used also encompasses singular versions of the noun.
So that those skilled in the art can appreciate the features and effects of the present invention, a general description and definition of the terms and expressions set forth in the specification and claims follows. Unless otherwise defined, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention belongs, and in the event of a conflict, the present specification shall control.
The theory or mechanism described and disclosed herein, whether right or wrong, is not meant to limit the scope of the invention in any way, i.e., the present disclosure may be practiced without limitation to any particular theory or mechanism.
In this document, all features, such as values, amounts, and concentrations, are for brevity and convenience only, as defined in the numerical or percent range. Accordingly, the description of a numerical range or percentage range should be considered to cover and specifically disclose all possible sub-ranges and individual values (including integers and fractions) within the range.
The above-mentioned features of the invention, or of the embodiments, may be combined in any desired manner. All of the features disclosed in this specification may be used in combination with any combination of features, provided that the combination of features is not inconsistent and all such combinations are contemplated as falling within the scope of the present specification. The various features disclosed in the specification may be replaced by alternative features serving the same, equivalent or similar purpose. Thus, unless expressly stated otherwise, the disclosed features are merely general examples of equivalent or similar features.
The invention has the main advantages that: the asiaticoside, asiatic acid, madecassoside and madecassoside with high purity are prepared into the ethosome according to a certain proportion, and the active ingredients of the asiatic centella can be matched in the skin product, so that the use is convenient, and the effect of the asiatic centella is truly realized.
The invention will be further illustrated with reference to specific examples. It is to be understood that these examples are illustrative of the present invention and are not intended to limit the scope of the present invention. The experimental procedures, which do not address the specific conditions in the examples below, are generally carried out under conventional conditions or under conditions recommended by the manufacturer. All percentages, ratios, proportions, or parts are by weight unless otherwise indicated. The units in weight volume percent are well known to those skilled in the art and refer, for example, to the weight of solute in 100 milliliters of solution. Unless defined otherwise, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art. In addition, any methods and materials similar or equivalent to those described herein can be used in the methods of the present invention. The preferred methods and materials described herein are presented for illustrative purposes only.
The raw material component sources in the following examples:
asiatic acid: available from SEPPIC s.a.
Asiaticoside: available from SEPPIC s.a.
Madecassic acid: available from SEPPIC s.a.
Madecassoside: available from SEPPIC s.a.
Phospholipid: purchased from Lipoid
Hydrogenated lecithin: purchased from Lipoid and Nikkol
Hydrogenated lysolecithin: purchased from Tsuji Oil Mills co., ltd.
Tween 80: purchased from Croda
Glycerol: purchased from Wilmar Oleo
Diglycerol: purchased from Sakamoto Yakuhin Kogyo
Propylene glycol: purchased from Shell Chemicals
1, 3-butanediol: purchased from DAICEL CORPORATION
Ethoxydiglycol: purchased from Gattefosse SAS
Phenoxyethanol: available from DOW chemistry
Ethylhexyl glycerol: purchased from Ashland
Pentanediol: purchased from THOR
Particle size, PDI and Zeta potential measurement methods in the following examples: test instrument Anton Paar Litesizer500 using dynamic light scattering techniques
Examples
1. Raw material components and corresponding ethosome properties
The corresponding ethosomes were prepared according to the ingredients listed in table 1 below, comprising the following steps:
(1) Weighing and uniformly mixing the raw material components A1-4 at room temperature;
(2) Accurately weighing B, C raw material components, adding the mixture A1-4, heating to 80-90 ℃ and stirring until phospholipid is completely dissolved;
(3) Adding the component D into the mixture, and uniformly stirring and mixing at 80-90 ℃;
(4) Heating the raw material component E to 80-85 ℃, uniformly mixing, adding the mixture obtained in the step (3), and homogenizing for 2-10min at 5000-10000 rpm;
(5) Circulating the mixture obtained in the step (4) through a high-pressure homogenizer for 2-8 times at 80-90 ℃ and 600-1000 bar;
(6) And (3) adding the component F, stirring, cooling to room temperature, discharging and detecting.
TABLE 1
* The content is based on the total weight of each raw material component in the ethosome
By/is meant centrifugal precipitation, or as such precipitation, indicating that no ethosome encapsulation has formed and that the active is precipitated, thus eliminating the need for particle size or other tests
2. High pressure homogenizer operating conditions and corresponding ethosome properties
For example 1, the appearance and physicochemical indexes of the obtained ethosome were compared by different pressures and cycle times to determine the preparation process of the ethosome; the corresponding ethosomes were obtained according to the starting material components and the preparation steps of example 1 of table 1 above, except that some changes were made in the operating parameters of the high pressure homogenizer of step (5). Details are shown in Table 2.
TABLE 2
The results show that the process conditions with a pressure in the range 600-1000bar and a number of cycles in the range 2-8 are suitable for obtaining the ethosomes of the invention. The particle size of the prepared ethosome is larger due to too low pressure or too low or too high cycle times, and a small amount of precipitation possibly exists, so that the use and the stability of the ethosome are affected.
3. Stability test of ethosome
The ethosomes of example 1 and comparative example 1 were each tested for their properties after being left at 5 ℃, room Temperature (RT) and 45 ℃ for 1 month, 2 months and 3 months, respectively. The results are shown in Table 3.
TABLE 3 Table 3
The results show that the ethosome provided by the invention has good stability.
Application example 1
Whitening essence
Accurately weighing the phase A raw materials, stirring and mixing at room temperature uniformly, heating to 85 ℃ to dissolve until the raw materials are transparent, then starting to cool, cooling to about 45 ℃, sequentially adding the phase B, stirring uniformly, then adding the phase C which is uniformly mixed in advance, stirring until the raw materials are transparent, starting to cool, cooling to room temperature, detecting and discharging until the raw materials are qualified.
Application example 2
Skin soothing emulsion
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Accurately weighing the phase A, uniformly stirring and mixing, heating to 80-85 ℃ for uniform dissolution, heating and dissolving the phase B to 80-85 ℃ for complete dissolution, adding the phase B into the phase A for homogenizing at 3000rpm for 2-5min, then stirring and cooling to 65 ℃, adding the phase C, uniformly stirring and cooling to 45 ℃, adding the phase D diluted by water, uniformly stirring, adding the phase E, uniformly stirring, cooling to room temperature, and detecting to be qualified and discharging.
Application example 3
Scar repair lotion
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Accurately weighing the phase A, uniformly stirring and mixing, heating to 80-85 ℃ for uniform dissolution, cooling to 50 ℃, adding the phase C, uniformly stirring, mixing the phase B at room temperature, slowly adding the phase A into the phase B under stirring, completely adding the phase A, homogenizing at 3000-5000rpm for 2-5min, stirring and cooling to 35 ℃, adding the phase D, uniformly stirring, cooling to room temperature, and detecting to be qualified, and discharging.
The foregoing description is only illustrative of the preferred embodiments of the present invention and is not intended to limit the scope of the invention, which is defined broadly in the appended claims, and any person skilled in the art to which the invention pertains will readily appreciate that many modifications, including those that fall within the metes and bounds of the claims, or equivalence of such metes and bounds thereof.
Claims (11)
1. The quadric centella asiatica ethosome is characterized by comprising the following raw material components in terms of total weight of the ethosome:
0.5-12wt% of herba Lespedezae Cuneatae
2-15wt% of phospholipid
10-30wt% of water
Cosurfactant 10-30wt%
20-30wt% of polyol
0-3wt% of preservative;
the centella asiatica is a mixed substance consisting of asiatic acid, asiaticoside, madecassic acid and madecassoside; the auxiliary surfactant is polysorbate-80 and/or lysophosphatidylcholine; the polyalcohol is ethoxydiglycol and/or propylene glycol;
the preparation method of the ethosome comprises the following steps:
(1) Mixing centella asiatica, phospholipids and co-surfactant to obtain mixture 1;
(2) Mixing the mixture 1 with a polyol to obtain a mixture 2;
(3) Mixing the mixture 2 with water, and homogenizing to obtain a mixture 3;
(4) The mixture 3 is circulated through a homogenizer 2 to 8 times at 600 to 1000bar to obtain the ethosome.
2. The ethosome of claim 1, wherein the feed component further comprises 15-30wt% humectant.
3. The ethosome of claim 1, wherein the preservative is selected from one or more of the following: p-hydroxyacetophenone, 1, 2-hexanediol, pentanediol, octanediol, phenoxyethanol, ethylhexyl glycerol, and p-anisic acid.
4. The ethosome of claim 2, wherein the humectant is selected from one or more of the following: glycerol, diglycerol and polyglycerol-3.
5. The ethosome of claim 1, wherein the starting components of the ethosome are 0.5-12wt% centella asiatica, 2-15wt% phospholipids, 10-30wt% water, 15-30wt% humectants, 5-30wt% co-surfactants, 20-30wt% polyols, and 0-3wt% preservatives.
6. The ethosome of claims 1 to 5, wherein the ethosome has a particle size of 10 to 200nm, a pdi <0.3, and a zeta potential absolute value of not less than 30mV.
7. The plastid according to any one of claims 1 to 5, wherein the weight ratio of centella asiatica to madecassoside is 1:1, the weight ratio of asiaticoside to madecassoside is 1-3:1, the weight ratio of the sum of asiaticoside and madecassoside to the sum of asiatic acid and madecassoside is 2-4:3, and the purities of asiatic acid, asiaticoside, madecassoside and madecassoside are respectively equal to or higher than 90%.
8. A method of preparing an ethosome according to any one of claims 1 or 3, comprising the steps of:
(1) Mixing centella asiatica, phospholipids and co-surfactant to obtain mixture 1;
(2) Mixing the mixture 1 with a polyol to obtain a mixture 2;
(3) Mixing the mixture 2 with water, and homogenizing to obtain a mixture 3;
(4) Circulating the mixture 3 through a homogenizer at 600-1000bar for 2-8 times to obtain the ethosome;
optionally step (4) further comprises: and adding a preservative after circulating by a homogenizer.
9. Use of an ethosome according to any one of claims 1 to 7 for the preparation of a dermatological product.
10. A dermatological product, characterized in that it comprises an ethosome according to any one of claims 1 to 7 and a cosmetically acceptable carrier.
11. A method of preparing a dermatological product according to claim 10, wherein the method comprises the steps of: mixing an ethosome according to any one of claims 1 to 7 with a cosmetically acceptable carrier to obtain a dermatological product according to claim 10.
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| CN104010622A (en) * | 2011-10-31 | 2014-08-27 | 富士胶片株式会社 | Aqueous dispersion and method for producing same |
| CN107375139A (en) * | 2017-08-01 | 2017-11-24 | 佛山市三水区嘉华化学研究院（普通合伙） | A kind of elastic force with senile-resistant efficacy compacts eye mask |
| CN113230172A (en) * | 2021-05-24 | 2021-08-10 | 泉州达浔生物科技有限公司 | Cosmetic or dermatological composition, preparation method and application thereof |
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| CN104010622A (en) * | 2011-10-31 | 2014-08-27 | 富士胶片株式会社 | Aqueous dispersion and method for producing same |
| CN107375139A (en) * | 2017-08-01 | 2017-11-24 | 佛山市三水区嘉华化学研究院（普通合伙） | A kind of elastic force with senile-resistant efficacy compacts eye mask |
| CN113230172A (en) * | 2021-05-24 | 2021-08-10 | 泉州达浔生物科技有限公司 | Cosmetic or dermatological composition, preparation method and application thereof |
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