CN114886786B - Elastic liposome composition and preparation method and application thereof - Google Patents

Elastic liposome composition and preparation method and application thereof Download PDF

Info

Publication number
CN114886786B
CN114886786B CN202210577130.6A CN202210577130A CN114886786B CN 114886786 B CN114886786 B CN 114886786B CN 202210577130 A CN202210577130 A CN 202210577130A CN 114886786 B CN114886786 B CN 114886786B
Authority
CN
China
Prior art keywords
elastic liposome
liposome composition
water
elastic
component
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.)
Active
Application number
CN202210577130.6A
Other languages
Chinese (zh)
Other versions
CN114886786A (en
Inventor
黄美贞
张先杏
殷邵希
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Kema Cosmetics Wuxi Co ltd
Original Assignee
Kema Cosmetics Wuxi Co ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Kema Cosmetics Wuxi Co ltd filed Critical Kema Cosmetics Wuxi Co ltd
Priority to CN202210577130.6A priority Critical patent/CN114886786B/en
Publication of CN114886786A publication Critical patent/CN114886786A/en
Application granted granted Critical
Publication of CN114886786B publication Critical patent/CN114886786B/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/02Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/14Liposomes; Vesicles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34Alcohols
    • A61K8/345Alcohols containing more than one hydroxy group
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/55Phosphorus compounds
    • A61K8/553Phospholipids, e.g. lecithin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67Vitamins
    • A61K8/673Vitamin B group
    • A61K8/675Vitamin B3 or vitamin B3 active, e.g. nicotinamide, nicotinic acid, nicotinyl aldehyde
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/84Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions otherwise than those involving only carbon-carbon unsaturated bonds
    • A61K8/85Polyesters
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/10General cosmetic use

Abstract

The invention discloses an elastic liposome composition, a preparation method and application thereof, wherein the raw materials of the elastic liposome composition comprise a water phase component, a polyalcohol component and a lipid component; the water phase component comprises water and water-soluble active ingredients, the lipid component consists of lecithin and polyglycerol ester with the mass ratio of 1:0.01-0.3, the polyglycerol ester is obtained by esterification reaction of polyglycerol and stearic acid, the lipid component forms a phospholipid layer in the elastic liposome composition, the phospholipid layer coats the water-soluble active ingredients and forms an elastic liposome, and the water-soluble active ingredients account for 0.0001-10.0% by mass percent; the elastic liposome composition can be directly used or applied to cosmetics, can improve the skin permeability of water-soluble active ingredients, and has almost no irritation to skin.

Description

Elastic liposome composition and preparation method and application thereof
Technical Field
The invention relates to the field of cosmetics, in particular to an elastic liposome composition, and a preparation method and application thereof.
Background
In general, cosmetics refer to chemical industry or fine chemical products that are spread on any part of the surface of the human body, such as skin, hair, nails, lips, teeth, etc., by painting, spraying, or the like, to achieve cleaning, maintenance, beauty, modification, and change of appearance, or to correct odor of the human body, and to maintain a good state.
At present, common cosmetics with the effects of whitening, anti-wrinkle, antioxidation, anti-aging and the like generally act on a human body through skin, and then are absorbed into the interior through skin, so that the corresponding effects are exerted. The skin is divided into 3 parts, namely a stratum corneum, an epidermis layer and a dermis layer, wherein the stratum corneum is positioned at the outermost layer of the skin, keratinocytes taking keratin as a main component form a layered structure in the stratum corneum, the adjacent keratinocytes are filled with intercellular lipid, and the whole structure is similar to Brick and mortar (Brick and cement); meanwhile, unlike other biofilms composed of phospholipids, the stratum corneum is composed of lipid components such as Ceramide (Ceramide), cholesterol (Cholesterol), free fatty acids (Free fatty acids), and the like, which are connected in a straight line, so that the fat-soluble active ingredients are easily absorbed, but there is a problem that moisture and water-soluble active ingredients are more difficult to permeate the stratum corneum.
For example, niacinamide (Niacinamide), which is one of raw materials of anti-aging and whitening components, is a water-soluble vitamin B3, which is also known as Niacinamide, among vitamin B groups, and is known to have excellent moisturizing and whitening effects, but it has been studied that, since it is a water-soluble component, only a small amount of Niacinamide is simply formulated into cosmetics, there is a case where there is no significant effect, and in order to improve the effect, it is a general method to increase the amount of addition, however, there is a problem that there is a relatively significant irritation to the skin when it is added in a high content.
Therefore, how to overcome the skin barrier and thereby increase the penetration efficiency of water and water-soluble active ingredients in intercellular lipids is a technical problem to be solved in the art.
Disclosure of Invention
The invention aims to overcome the defects in the prior art and provide a novel elastic liposome composition which can improve the skin permeability of water-soluble active ingredients and has little irritation to skin.
The invention also provides a novel elastic liposome.
The invention also provides a preparation method of the elastic liposome composition.
The invention also provides a cosmetic composition containing the elastic liposome composition.
In order to achieve the above purpose, the invention adopts a technical scheme that:
an elastic liposome composition, which comprises the following raw materials: an aqueous phase component, a polyol component and a lipid component;
wherein the aqueous phase component comprises water, a water-soluble active ingredient;
the lipid component consists of lecithin and polyglycerol ester, wherein the mass ratio of the lecithin to the polyglycerol ester is 1:0.01-0.3, and the polyglycerol ester is obtained through esterification reaction of polyglycerol and stearic acid;
in the elastic liposome composition, the lipid component forms a phospholipid layer which coats the water-soluble active ingredient and forms an elastic liposome, and the water-soluble active ingredient accounts for 0.0001-10.0% by mass percent.
According to some preferred aspects of the invention, the ratio of the lipid component to the water-soluble active ingredient is 1:0.0001-2.5 by mass. Further, the mass ratio of the lipid component to the water-soluble active ingredient is 1:0.1-2.5.
In some embodiments of the invention, the ratio of the lipid component to the water-soluble active ingredient is 1:0.5-2.5 by mass.
According to some preferred aspects of the present invention, in the process of preparing the polyglycerol ester, the molar amount of stearic acid added is equal to or greater than the molar amount of the polyglycerol added, and for example, may be an equimolar amount reaction, may be that the molar amount of stearic acid added is 2 times the molar amount of the polyglycerol added, or the like; in some preferred and specific embodiments of the present invention, the polyglycerol ester may be polyglycerol-10 stearate and/or polyglycerol-10 distearate.
According to the present invention, lecithin is a yellow brown oily substance present in animal and plant tissues and yolk, and the constituent components include phosphoric acid, choline, fatty acid, glycerol, glycolipid, triglyceride and phospholipid, and are important constituent components of cell membranes, alveolar surfactant, lipoprotein and bile. Practice shows that the lecithin is compounded with the polyglycerol ester, so that the elasticity, softness and deformability of the elastic liposome can be improved, the elastic liposome is beneficial to passing through the stratum corneum, and finally the effect of conveying the effective components more efficiently can be achieved. In some preferred and specific embodiments of the present invention, the lecithin may be hydrogenated lecithin.
In the present invention, if the elastic liposome composition of the present invention is not prepared according to the weight percentage of lecithin to polyglycerol ester of 1:0.01 to 0.3, the softness, elasticity, deformability and coating efficiency of the water-soluble active ingredient of the elastic liposome are all significantly reduced. In some preferred and specific embodiments of the present invention, the mass ratio of the lecithin to the polyglycerol ester is 1:0.01-0.15. According to a specific aspect of the invention, the mass ratio of the lecithin to the polyglycerol ester is 1:0.025.
According to some preferred aspects of the invention, the water-soluble active ingredient includes, but is not limited to, niacinamide, but may be other water-soluble active ingredients.
According to some preferred and specific aspects of the present invention, the water-soluble active ingredient is niacinamide, and the niacinamide is 0.1% -10.0% in the elastic liposome composition. In some embodiments of the invention, the nicotinamide comprises 1% to 10.0% by mass of the elastic liposome composition.
According to some preferred aspects of the invention, the polyol component comprises 1% to 20% by mass of the elastic liposome composition.
According to some preferred aspects of the invention, the polyol component is a combination of one or more selected from glycerol, butanediol, 1, 3-propanediol, 1, 2-hexanediol, methylpropanediol, dipropylene glycol.
According to the invention, the elastic liposomes have an average particle size of 70-200nm.
In the present invention, the elastic liposome composition of the present invention may further comprise other additives, including, for example, but not limited to, moisturizers, preservatives, pH regulators, skin conditioners, and the like.
In some embodiments of the invention, the water in the elastic liposome composition can be deionized water.
The invention provides another technical scheme that: the preparation method of the elastic liposome composition comprises the following steps:
(1) Mixing and dispersing the components in the water phase component, and heating to 72-85 ℃;
(2) Mixing and dispersing the components in the polyol component, and heating to 72-85 ℃;
(3) Adding the lipid component into the polyol component treated in the step (2), and uniformly mixing;
(4) Adding the mixture obtained after the treatment in the step (3) into the water phase component obtained after the treatment in the step (1) under the stirring condition, and uniformly mixing;
(5) Cooling the mixture obtained after the treatment in the step (4) to 50-65 ℃, and homogenizing after cooling to prepare the elastic liposome composition.
According to the invention, the step (1) and the step (2) are not sequential.
According to some preferred aspects of the invention, in step (1) and step (2), heating is carried out to 75-82 ℃ respectively, and further heating is carried out to 78-80 ℃ respectively.
According to some preferred aspects of the invention, in step (5), cooling is carried out to 55-62 ℃.
In some embodiments of the invention, the homogenization treatment is performed using a dynamic ultra-high pressure homogenizer.
In some embodiments of the invention, the homogenization treatment may be performed multiple times, for example, 2 times, 3 times, or even more.
According to the present invention, in the elastic liposome composition, the formed elastic liposome is dispersed in a mixed system composed of water and a polyol component or the like.
The invention provides another technical scheme that: an elastic liposome in the above elastic liposome composition.
In the present invention, the elastic liposome may not contain water and a polyol component, but may be actually prepared with a small amount of water and polyol mixed therein.
In the present invention, the elastic liposome composition may be used directly on the skin, or may be used as one of the raw materials to prepare a cosmetic composition for use on the skin.
Further, the invention provides another technical scheme: a cosmetic composition comprising, in mass%, 0.0001% to 50% of the above-described elastic liposome composition.
The cosmetic composition of the present invention may contain, in addition to the above-mentioned elastic liposome composition, one or more components selected from the group consisting of moisturizers, solvents, thickeners, lipids, dissolving agents, concentrates, gelling agents, softeners, antioxidants, suspending agents, stabilizers, foaming agents, fragrances, surfactants, emulsifiers, fillers, chelating agents, preservatives, vitamins, blocking agents, humectants, oils, dyes, pigments, hydrophilic or lipophilic active agents, lipid vesicles, and the balance water.
The cosmetic composition of the present invention may be in the form of one of a toner, astringent, essence, emulsion, essence cream, essence, ampoule, face cream, eye cream, massage cream, mask, foundation, BB cream, pre-make-up cream, powder, sun cream, cleansing lotion, shampoo, conditioner, scalp essence, body cream, shower gel, body spray, but is not limited thereto.
In some embodiments of the invention, the cosmetic composition comprises a first component comprising water, a polyol, a chelating agent, an elastic liposome composition as described above, a thickening agent, and a second component comprising cetostearyl alcohol, polyglycerol-10 distearate, caprylic/capric triglyceride.
In some embodiments of the present invention, the polyol may be glycerin, 1, 2-hexanediol, etc., and the polyol may be 2% -15% by mass.
In some embodiments of the present invention, the chelating agent may be disodium ethylenediamine tetraacetate (EDTA-2 Na), and the chelating agent may be 0.001% -1% by mass.
In some embodiments of the present invention, the thickener may be an ammonium acryloyldimethyl taurate/VP copolymer, which is mainly used for thickening, rheological property and pleasant feeling after use, and is 0.05% -3% by mass.
In some embodiments of the present invention, the cosmetic composition comprises, in mass percent, 5% to 20% of the second component.
In some embodiments of the present invention, the water (which may be deionized water) in the first component may be used to make up the remaining content after the other component content is determined, based on 100% content in the cosmetic composition.
In some embodiments of the invention, the second component comprises the cetostearyl alcohol, the polyglycerol-10 distearate, and the caprylic/capric triglyceride in a mass ratio of 1:2 to 3:2 to 3.
In some embodiments of the invention, the cosmetic composition is prepared by the following method:
(1) Mixing and dispersing the first component uniformly, and heating to 70-80 ℃;
(2) Uniformly mixing the second component, heating to 70-80 ℃ and completely dissolving;
(3) Pouring the second component treated in the step (2) into the first component treated in the step (1), homogenizing and emulsifying in vacuum at 70-80deg.C (2500-3500 rpm), cooling to 40-50deg.C, emulsifying again (2500-3500 rpm), and cooling to obtain cosmetic composition.
Due to the application of the technical scheme, compared with the prior art, the invention has the following advantages:
the invention is based on the problem that the water-soluble active ingredients are difficult to pass through the stratum corneum, so that the percutaneous absorption rate is low. Based on a large number of experiments, it is unexpectedly found that when lecithin and polyglycerol ester (obtained by esterification reaction of polyglycerol and stearic acid) are adopted and combined according to a specific proportion, the effect of coating water-soluble active ingredients can be achieved in a mixed system of water and polyalcohol, the coating rate is high, the coated stable state can be maintained for a long time, and finally, elastic liposome dispersed in the mixed system of water and polyalcohol is formed.
Drawings
FIG. 1 is a schematic diagram of the structure of an elastic liposome in an elastic liposome composition prepared according to an embodiment of the present invention;
FIG. 2 is a schematic diagram showing the process of penetration of elastic liposomes into the stratum corneum according to an embodiment of the present invention.
Detailed Description
The main conception of the invention is that: provided is a novel vesicle having soft and flexible properties, namely, an elastic liposome of the present invention, which has a similar core-shell structure as shown in FIG. 1, a phospholipid layer as an outer layer and a water-soluble active ingredient as an inner core, and the phospholipid layer has excellent deformability and flexibility, and is deformed to conform to the shape of the interstices of the stratum corneum when facing the stratum corneum in a state where the lamellar structure and the lipid ingredient are linearly connected, thereby realizing circulation, and is stable in overall structure and not liable to break when penetrating the stratum corneum, and is capable of recovering the original form after penetration, and a schematic diagram of penetration of the stratum corneum is shown in FIG. 2.
Further, based on the above-described conception, the present inventors have found that when lecithin and polyglyceryl ester (obtained by esterification reaction of polyglycerin with stearic acid) are used in combination in a specific ratio, it is possible to achieve the effect of coating a water-soluble active ingredient in a mixed system of water and polyhydric alcohol with a high coating ratio, and finally an elastic liposome dispersed in the mixed system of water and polyhydric alcohol is formed, which has not only excellent deformability and flexibility but also good stability during deformation, and substantially does not suffer from failure of coating effect.
Based on the above, the invention provides an elastic liposome composition, which comprises the following raw materials: an aqueous phase component, a polyol component and a lipid component;
wherein the aqueous phase component comprises water, a water-soluble active ingredient;
the lipid component consists of lecithin and polyglycerol ester, wherein the mass ratio of the lecithin to the polyglycerol ester is 1:0.01-0.3, and the polyglycerol ester is obtained through esterification reaction of polyglycerol and stearic acid;
in the elastic liposome composition, the lipid component forms a phospholipid layer which coats the water-soluble active ingredient and forms an elastic liposome, and the water-soluble active ingredient accounts for 0.0001-10.0% by mass percent.
The elastic liposome composition can improve the skin permeability of water-soluble active ingredients, has almost no irritation to skin, has relatively high coating rate, and can realize the maximization effect of low-concentration active substances; in addition, the raw materials used in the invention have no safety dispute, and can be applied to human skin.
The above-described aspects are further described below in conjunction with specific embodiments; it should be understood that these embodiments are provided to illustrate the basic principles, main features and advantages of the present invention, and that the present invention is not limited by the scope of the following embodiments; the implementation conditions employed in the examples may be further adjusted according to specific requirements, and the implementation conditions not specified are generally those in routine experiments.
All starting materials are commercially available or prepared by methods conventional in the art, not specifically described in the examples below.
Examples 1 to 3
The present examples provide elastomeric liposome compositions and methods of making the same, the materials and amounts of which are shown in table 1 below.
TABLE 1
Note that: hydrogenated lecithin was purchased from NEUROPID under the trademark SOYA-SPL 75H (PF); polyglycerol-10 stearate is available from NIPPON SURFACTANT INDUSTRIES co., LTD, brand decaglycon 1-SV; butanediol: butyl glycol.
The preparation method of the elastic liposome composition comprises the following steps:
(1) Mixing and dispersing the components in the water phase component, and heating to 78-80 ℃;
(2) Mixing and dispersing the components in the polyol component, and heating to 78-80 ℃;
(3) Adding the lipid component into the polyol component treated in the step (2), and uniformly mixing;
(4) Adding the mixture obtained after the treatment in the step (3) into the water phase component obtained after the treatment in the step (1) under the stirring condition, and uniformly mixing;
(5) Cooling the mixture obtained after the treatment in the step (4) to 60 ℃, and homogenizing for 2 times by using a dynamic ultrahigh pressure homogenizer (about 1300 bar) after cooling to prepare the elastic liposome composition.
Comparative example 1
Substantially the same as in example 1, the only difference is that: the mass percentage of nicotinamide is adjusted to 15%. The elastic liposome composition prepared in this example was directly applied to the skin with stimulus feedback.
Comparative example 2
Substantially the same as in example 1, the only difference is that: polyglycerol-10 stearate was replaced with sorbitan stearate (SPAN 60) in equal amounts.
Comparative example 3
Substantially the same as in example 1, the only difference is that: polyglycerol-10 stearate was replaced with sorbitan oleate (SPAN 80) in the same amount.
Performance test 1
The liposomes prepared in example 1 and comparative examples 2 to 3 were subjected to the following performance tests, and specific results are shown in Table 2.
The test method is as follows:
(1) Particle size and ZETA potential: microtrac Flex (Microtrac, USA) using the principle of scattering of light was used. The average particle size was shown by a cubic analysis and the degree of distribution, i.e., polydispersity index, was resolved by the CONTIN algorithm. The measurement conditions of the particle size and ZETA potential were as follows, temperature: 25 ℃, scattering angle: 165 °, light source: argon laser.
(2) Coating rate: a certain amount of the elastic liposomes of example 1 and comparative examples 2 and 3 was filtered out with 0.45 μm syringfilter (Minisart CA 26 mm, germany), the uncoated nicotinamide was removed by repeating the same procedure 3 times, 1mL of the liposome composition treated in the above-mentioned manner was mixed with 10mL of ethanol to break the lipid membrane of the elastic liposome, the solvent was evaporated by a rotary evaporator, the water bath temperature was maintained at about 35℃and 1mL of ethanol was further added, and the coated nicotinamide of the elastic liposome was quantitatively analyzed by UV-vis spectrometer. In addition, the concentration of nicotinamide coated in the elastic liposome is calculated by preparing standard curves with different concentrations, and the coating rate of the elastic liposome is calculated according to the formula 1;
coating ratio (%) = (T-P)/t×100;
t: initial nicotinamide concentration;
p: nicotinamide concentration that did not pass 0.45 μm syringfilter.
(3) Deformation index: the extent of penetration of the elastic liposomes in the artificial permeation barrier was determined using a mini extruder. Specifically, after the elastic liposome was pressurized at a pressure of 0.2MPa for 1 minute and 30 seconds, the amount of Polycarbonate membrane elastic liposome passing through 0.08 μ pore was measured, and the particle size of elastic liposome passing through the artificial permeation barrier was determined. At this time, the elasticity of the elastic liposome membrane is expressed as follows;
deformation index=j Flux ×(r v /r p ) 2
J Flux : the amount of elastic liposomes by membrane;
r v : particle size of the elastic liposome after extrusion;
r p : pore size of membrane.
TABLE 2
Note that: polydispersity index: the ratio of the weight average molecular weight to the number average molecular weight characterizes a parameter of the molecular weight inhomogeneity of the polymer. The larger the number, the wider the molecular weight distribution of the liposome, and the more nonuniform the size.
ZETA potential: the important meaning of the ZETA potential is that its value is related to the stability of the colloidal dispersion. The ZETA potential is a measure of the strength of the mutual repulsion or attraction between particles. The smaller the molecule or dispersed particle, the higher the absolute value of the ZETA potential (positive or negative), the more stable the system, i.e., the dissolution or dispersion can resist aggregation.
Coating rate: refers to the ability of liposomes to encapsulate water-soluble active ingredients.
Deformation index: i.e. the elasticity index, the larger the number the greater the elasticity and the higher the deformability.
Examples 4 to 5 and comparative examples 4 to 6
The cosmetic compositions of examples 4 to 5 were obtained by preparing the cosmetic compositions of examples 1 to 2 above, and the elastic liposome compositions of comparative examples 4 to 6 were replaced with nicotinamide, respectively, based on example 4, in the amounts of 2%, 5%, 10% by weight, respectively, as shown in Table 3 below.
TABLE 3 Table 3
Note that: the ammonium acryloyldimethyl taurate/VP copolymer is available from CLARIANT under the trademark ARISTOFLEX AVC;
cetostearyl alcohol is available from BASF under the trademark
Polyglycerol-10 distearate was purchased from ILSHINWELLS under the trade designation ALMAX-9062;
caprylic/capric triglyceride is available from EVONIK under the trademark
The preparation method of the cosmetic composition comprises the following steps:
(1) Uniformly mixing and dispersing the first component, and heating to 75-78 ℃;
(2) Uniformly mixing the second component, heating to 75-78 ℃ and completely dissolving;
(3) Slowly pouring the second component of the treated step (2) into the first component of the treated step (1), homogenizing and emulsifying (3000 rpm) in vacuum at 75-78 ℃, cooling to 45 ℃, performing secondary emulsification (3000 rpm), and cooling to 35 ℃ to obtain the cosmetic composition.
Performance test (II)
The cosmetic compositions obtained in examples 4 to 5 and comparative examples 4 to 6 were evaluated for efficacy.
The testing method comprises the following steps: a Japanese American CM-2500D color difference meter [ KONICA MINOLTA ] was used. The values of L, a, b at each observation time point were measured for the test and control areas, respectively, and each area was tested 3 times and recorded. Calculating individual skin tone type angle (individule type angle, ITA °) parameters:
l: white chromaticity;
a: red chromaticity;
b: yellow chromaticity;
the greater the ITA DEG value, the lighter the skin tone, and conversely the darker the skin tone.
1. Skin whitening effect
The test part (face) stands for 30 minutes under the constant temperature and humidity environment;
determination of skin Brightness L before use, after 2 weeks of use, after 4 weeks of use *
According to the method of using the product, a proper amount of sample is taken and uniformly smeared on the face once in the morning and at night, and the sample is gently and completely absorbed.
Evaluation criteria: skin lightening improvement rate = (skin lightening after use-skin lightening before use)/skin lightening before use 100%.
The results are shown in Table 4 below.
TABLE 4 skin lightening L *
Test results: by data analysis, the skin lightening effect of examples 4 and 5, in which niacinamide was added after coating the elastic liposome of the present invention, was significantly increased compared to that of comparative examples 4 and 5, in which niacinamide was directly applied to dosage forms, in the case of adding the same amount of niacinamide. Illustrating that the elastic liposomes of the present invention help to increase the skin penetration of the water-soluble active ingredient.
The skin lightening effect of example 5 (total nicotinamide content 5%) in the present invention is not significantly different from that of comparative example 6 (total nicotinamide content 10%), but the addition ratio of nicotinamide may indicate that the inventive elastic liposome coated with a low concentration of active ingredient may achieve a similar effect as the high content of active ingredient.
2. Skin color improving effect
The test part (face) stands for 30 minutes under the constant temperature and humidity environment;
determining skin chromaticity ITA DEG before use, after use for 2 weeks and after use for 4 weeks;
according to the method of using the product, a proper amount of sample is taken and uniformly smeared on the face once in the morning and at night, and the sample is gently and completely absorbed.
Evaluation criteria: skin chromaticity improvement rate= (skin chromaticity after use-skin chromaticity before use)/skin chromaticity before use 100%.
The results are shown in Table 5 below.
TABLE 5 skin chromaticity ITA DEG
Test results: by data analysis, the skin tone improving effect of the example 4 and the example 5, in which the niacinamide is added after the coating of the elastic liposome of the present invention, is significantly increased compared with the skin tone improving effect of the comparative example 4 and the comparative example 5, in which the niacinamide is directly applied to the dosage form. Illustrating that the elastic liposomes of the present invention help to increase the skin penetration of the water-soluble active ingredient.
The skin lightening effect of example 5 (total nicotinamide content 5%) in the present invention is not significantly different from that of comparative example 6 (total nicotinamide content 10%), but the addition ratio of nicotinamide may indicate that the inventive elastic liposome coated with a low concentration of active ingredient may achieve a similar effect as the high content of active ingredient.
The above embodiments are provided to illustrate the technical concept and features of the present invention and are intended to enable those skilled in the art to understand the content of the present invention and implement the same, and are not intended to limit the scope of the present invention. All equivalent changes or modifications made in accordance with the spirit of the present invention should be construed to be included in the scope of the present invention.
The endpoints and any values of the ranges disclosed herein are not limited to the precise range or value, and are understood to encompass values approaching those ranges or values. For numerical ranges, one or more new numerical ranges may be found between the endpoints of each range, between the endpoint of each range and the individual point value, and between the individual point value, in combination with each other, and are to be considered as specifically disclosed herein.

Claims (9)

1. An elastic liposome composition is characterized in that the raw materials of the elastic liposome composition comprise the following components: an aqueous phase component, a polyol component and a lipid component;
wherein the aqueous phase component comprises water, a water-soluble active ingredient;
the lipid component consists of lecithin and polyglycerol ester, wherein the mass ratio of the lecithin to the polyglycerol ester is 1:0.01-0.3, and the polyglycerol ester is obtained through esterification reaction of polyglycerol and stearic acid; wherein the polyglycerol ester is polyglycerol-10 stearate and/or polyglycerol-10 distearate, and the lecithin is hydrogenated lecithin;
the water-soluble active ingredient comprises nicotinamide, wherein the nicotinamide accounts for 0.1-10.0% of the elastic liposome composition in percentage by mass;
the preparation method of the elastic liposome composition comprises the following steps:
(1) Mixing and dispersing the components in the water phase component, and heating to 72-85 ℃;
(2) Mixing and dispersing the components in the polyol component, and heating to 72-85 ℃;
(3) Adding the lipid component into the polyol component treated in the step (2), and uniformly mixing;
(4) Adding the mixture obtained after the treatment in the step (3) into the water phase component obtained after the treatment in the step (1) under the stirring condition, and uniformly mixing;
(5) Cooling the mixture obtained after the treatment in the step (4) to 50-65 ℃, and homogenizing after cooling to prepare the elastic liposome composition.
2. The elastic liposome composition according to claim 1, wherein the ratio of the lipid component to the water-soluble active ingredient is 1:0.0001-2.5 by mass.
3. The elastic liposome composition of claim 2, wherein the ratio of the lipid component to the water-soluble active ingredient is 1:0.1-2.5 by mass.
4. The elastic liposome composition of claim 1, wherein the mass ratio of lecithin to polyglycerol ester is 1:0.01-0.15.
5. The elastic liposome composition of claim 1, wherein the polyol component comprises 1% -20% by mass of the elastic liposome composition, and the polyol component is one or a combination of more selected from the group consisting of glycerin, butylene glycol, 1, 3-propanediol, 1, 2-hexanediol, methyl propanediol and dipropylene glycol.
6. The elastic liposome composition of claim 1, wherein the elastic liposome in the elastic liposome composition has an average particle size of 70-200nm.
7. A method of preparing the elastic liposome composition of any one of claims 1-6, comprising:
(1) Mixing and dispersing the components in the water phase component, and heating to 72-85 ℃;
(2) Mixing and dispersing the components in the polyol component, and heating to 72-85 ℃;
(3) Adding the lipid component into the polyol component treated in the step (2), and uniformly mixing;
(4) Adding the mixture obtained after the treatment in the step (3) into the water phase component obtained after the treatment in the step (1) under the stirring condition, and uniformly mixing;
(5) Cooling the mixture obtained after the treatment in the step (4) to 50-65 ℃, and homogenizing after cooling to prepare the elastic liposome composition.
8. An elastic liposome, wherein the elastic liposome is an elastic liposome in the elastic liposome composition of any one of claims 1 to 6.
9. A cosmetic composition comprising, in mass%, from 0.0001% to 50% of the elastic liposome composition of any one of claims 1 to 6.
CN202210577130.6A 2022-05-25 2022-05-25 Elastic liposome composition and preparation method and application thereof Active CN114886786B (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202210577130.6A CN114886786B (en) 2022-05-25 2022-05-25 Elastic liposome composition and preparation method and application thereof

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN202210577130.6A CN114886786B (en) 2022-05-25 2022-05-25 Elastic liposome composition and preparation method and application thereof

Publications (2)

Publication Number Publication Date
CN114886786A CN114886786A (en) 2022-08-12
CN114886786B true CN114886786B (en) 2024-04-12

Family

ID=82725613

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202210577130.6A Active CN114886786B (en) 2022-05-25 2022-05-25 Elastic liposome composition and preparation method and application thereof

Country Status (1)

Country Link
CN (1) CN114886786B (en)

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20100043748A (en) * 2008-10-21 2010-04-29 (주)네오팜 Elastic liposome and composition of skin external application containing the same
CN109700671A (en) * 2018-02-13 2019-05-03 深圳高尚科美生物科技有限公司 Flexible lipidosome cosmetics and preparation method thereof comprising active small molecular substance
CN111195230A (en) * 2018-11-19 2020-05-26 奥维嘉生物科技(北京)有限公司 Method for preparing flexible liposome
KR20200095244A (en) * 2019-01-31 2020-08-10 서울과학기술대학교 산학협력단 A deformable liposome prepared with natural surfactants and use of the same
KR20210095352A (en) * 2020-01-23 2021-08-02 (주)에이티 랩 Manufacturing method of liposome with enhanced skin permeation
WO2021235767A1 (en) * 2020-05-19 2021-11-25 주식회사 스타스테크 Method for obtaining collagen peptide from starfish, elastic liposome comprising starfish-derived collagen peptide, and cosmetic composition comprising same
CN114080215A (en) * 2019-08-14 2022-02-22 韩国科玛株式会社 Elastomeric liposome composition comprising sucrose-based surfactant and cosmetic composition containing the same
CN114366679A (en) * 2022-01-13 2022-04-19 拉芳家化股份有限公司 Liposome containing organic acid microparticles and preparation method thereof
KR20220052560A (en) * 2020-10-21 2022-04-28 주식회사 코리아나화장품 Cosmetic composition comprising deformable liposome with effects of alleviating skin irritation and promoting skin absorption

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20100043748A (en) * 2008-10-21 2010-04-29 (주)네오팜 Elastic liposome and composition of skin external application containing the same
CN109700671A (en) * 2018-02-13 2019-05-03 深圳高尚科美生物科技有限公司 Flexible lipidosome cosmetics and preparation method thereof comprising active small molecular substance
CN111195230A (en) * 2018-11-19 2020-05-26 奥维嘉生物科技(北京)有限公司 Method for preparing flexible liposome
KR20200095244A (en) * 2019-01-31 2020-08-10 서울과학기술대학교 산학협력단 A deformable liposome prepared with natural surfactants and use of the same
CN114080215A (en) * 2019-08-14 2022-02-22 韩国科玛株式会社 Elastomeric liposome composition comprising sucrose-based surfactant and cosmetic composition containing the same
KR20210095352A (en) * 2020-01-23 2021-08-02 (주)에이티 랩 Manufacturing method of liposome with enhanced skin permeation
WO2021235767A1 (en) * 2020-05-19 2021-11-25 주식회사 스타스테크 Method for obtaining collagen peptide from starfish, elastic liposome comprising starfish-derived collagen peptide, and cosmetic composition comprising same
KR20220052560A (en) * 2020-10-21 2022-04-28 주식회사 코리아나화장품 Cosmetic composition comprising deformable liposome with effects of alleviating skin irritation and promoting skin absorption
CN114366679A (en) * 2022-01-13 2022-04-19 拉芳家化股份有限公司 Liposome containing organic acid microparticles and preparation method thereof

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Physical Characterizations and In Vitro Skin Permeation of Elastic Liposomes for Transdermal Delivery of Polygonum aviculare L. Extract;Saet Byeol Han,等;Polymer(Korea);第38卷(第6期);694-701 *
醇传递体在透皮给药系统中的研究进展;赵丹丹;于莲;冯幸福;戚映丹;应晓英;高建青;;中国现代应用药学;第36卷(第09期);1166-1171 *

Also Published As

Publication number Publication date
CN114886786A (en) 2022-08-12

Similar Documents

Publication Publication Date Title
JP3687277B2 (en) Whitening cosmetics
EP1267830B1 (en) Method for preparing high pressure/high shear dispersions containing physiologically active ingredients
AU668186B2 (en) Cosmetic containing phospholipids and fluorocarbon compounds
KR101762416B1 (en) Micelle composition for cosmetic
KR101116899B1 (en) Concentrated and diluted stable oil/water emulsions
KR20130011800A (en) O/w emulsion having skin lipid and cosmetic composition comprising the same
CN111544317A (en) Anti-aging composition cationic nano-liposome and preparation method and application thereof
KR102004147B1 (en) Cosmetic composition contaning lioosome idebenone
DE19922193B4 (en) Water-soluble concentrate consisting of essential oils microencapsulated in a liposome system, a process for its preparation and its use
KR101176523B1 (en) A Cosmetic Composition having phase transformation
CN101773452B (en) Structured lotions
KR20190079201A (en) High natural oil content nano emulsion composition improved clarity, and cosmetic composition comprising the same, and method for preparing same
KR102078667B1 (en) Cosmetic composition containg nanoemulsion encapsulated with 7-dehydrocholesterol, cholesterol and stearic acid in inner phase of hyaluronate-ceramide NP complex and manufacturing method thereof
CN114886786B (en) Elastic liposome composition and preparation method and application thereof
AU2018272337B2 (en) Emulsified liposome composition and preparation method therefor
JP6752057B2 (en) Stable composition for skin quality improver
KR100501728B1 (en) Cosmetic composition having the capsule structure of multiple-liquid crystalline membrane with nano size and manufacturing method thereof
JP2002226342A (en) Ammonia-containing emulsified composition as hair decolorant or hair dye, and method for hair decoloring or dyeing using the same
KR20210051522A (en) Oil-in-water nano emulsion cosmetic composition containing high content oil
JP4592347B2 (en) External preparation composition
KR102653968B1 (en) Method for manufacturing cosmetic composition with improved stability comprising high content of ceramide
KR102622315B1 (en) Method for manufacturing nanovesicles stably capturing high content of high-molecular Polysaccharide
KR102248265B1 (en) Method for producing ceramide ball with excellent stability and ceramide ball with excellent stability produced by the same method
CN114159332B (en) Liposome composition and preparation method thereof
US20210169805A1 (en) Emulsified liposome composition and preparation process thereof

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant