CN114569486B - Easily-absorbed skin repair liposome and preparation method thereof - Google Patents
Easily-absorbed skin repair liposome and preparation method thereof Download PDFInfo
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- CN114569486B CN114569486B CN202111340625.9A CN202111340625A CN114569486B CN 114569486 B CN114569486 B CN 114569486B CN 202111340625 A CN202111340625 A CN 202111340625A CN 114569486 B CN114569486 B CN 114569486B
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- 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
- A61K8/68—Sphingolipids, e.g. ceramides, cerebrosides, gangliosides
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- 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
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- 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
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- 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
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- 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
- A61K8/67—Vitamins
- A61K8/678—Tocopherol, i.e. vitamin E
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- 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
- A61K8/92—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
- A61K8/922—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- 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
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- 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
- A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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Abstract
The application provides an absorbable skin repair liposome and a preparation method thereof, wherein the skin repair liposome comprises, by mass, 20% of deionized water, 1-15% of octyldodecanol, 0.5% of tocopherol, 0.5% of sunflower seed oil, 1-5% of ceramide, 1-5% of phospholipid, 1-2% of hydrogenated phosphatidylcholine, 1-2% of cholesterol and the balance of glycerol. The liposome prepared by the application does not contain emulsifier components such as surfactant, so that the stability of the mixed liquid formed by the liposome and deionized water is improved, and the defoaming effect of the mixed liquid is also improved. The liposome prepared by the application has good compatibility with skin, is easy to be absorbed by the skin, and has the effects of moisturizing, whitening, diminishing inflammation and repairing the skin.
Description
Technical Field
The application relates to the technical field of A61K8/68, in particular to an absorbable skin repair liposome and a preparation method thereof.
Background
Ceramide is one of hot raw materials in the fields of skin care products and cosmetics in recent years, and has excellent moisturizing, repairing and anti-allergic effects. However, ceramide, which is an oil-soluble substance, is difficult to disperse uniformly in water-based cosmetics or skin care products and difficult to apply.
Chinese patent CN109106611a discloses a ceramide liposome, in which an emulsifier such as stearyl alcohol polyether, tween, glycerin fatty acid ester, etc. is added in order to improve dispersibility and stability of the liposome in an aqueous system. Chinese patent CN108272652B discloses a ceramide liposome, to which tween, alkyl glycoside, sugar ester, sucrose fatty acid ester, etc. are added as auxiliary emulsifying agents. However, the ceramide liposome added with the emulsifier has the phenomenon of difficult hydration due to the existence of the emulsifier in the use process.
Based on the above, the application provides an absorbable skin repair liposome and a preparation method thereof, wherein the preparation raw material does not contain emulsifying agent components such as surfactant and the like.
Disclosure of Invention
In a first aspect, the application provides an absorbable skin repair liposome, wherein the liposome is prepared from liposome membrane components and ceramide.
In a preferred embodiment, the ceramide is selected from at least one of ceramide EOS, ceramide NS, ceramide NP, ceramide AS, ceramide 6II, ceramide AH, ceramide NH, ceramide E.
In a preferred embodiment, the ceramide is a ceramide NP.
In a preferred embodiment, the liposome membrane component comprises at least one of a phospholipid, a hydrogenated phosphatidylcholine, cholesterol, lecithin, a hydrogenated phospholipid.
In a preferred embodiment, the liposome membrane component is a phospholipid, hydrogenated phosphatidylcholine, cholesterol.
In a preferred embodiment, the mass ratio of the ceramide to the liposome membrane component is (1-5): (1-20).
In a preferred embodiment, the mass ratio of ceramide to liposome membrane components is 1: (3-5).
In a preferred embodiment, the mass ratio of the phospholipid, hydrogenated phosphatidylcholine and cholesterol is (2-3): 1:1.
in a preferred embodiment, the liposome preparation raw material further comprises a moisturizing component, a penetration promoting component, glycerol and deionized water.
In a preferred embodiment, the moisturizing component is selected from at least one of tocopherol, squalane, sunflower seed oil, allantoin, caprylic/capric triglyceride, hyaluronic acid, tremella polysaccharide.
In a preferred embodiment, the moisturizing component is tocopherol and sunflower seed oil.
In the experimental process, the applicant finds that although the liposome prepared by taking the ceramide NP as the raw material can improve the moisturizing and repairing capabilities of the liposome prepared by taking the ceramide NP as the raw material, compared with other ceramides, the ceramide NP lacks unsaturated bonds and replaces more hydrophilic groups, so that the cohesive force of the liposome containing the ceramide NP is smaller, the particle size of the liposome is enlarged, and the stability of the liposome is reduced.
However, the applicant found that adding sunflower seed oil and tocopherol together with ceramide NP as the inclusion substances of the liposome can improve the aggregation capability of liposome membrane components and inclusion substances, improve the stability of the liposome, and reduce the particle size of the liposome, and the applicant speculates that the possible reasons are that the hydrophilic groups carried on the tocopherol are combined with the hydrophilic groups of the ceramide NP through acting forces such as hydrogen bonds, and the long carbon chains on the tocopherol form a package structure at the periphery of the hydrophilic groups, so that the binding capability of the inclusion and the liposome membrane components is improved, and meanwhile, the hydrophobic groups of the sunflower seed oil are further combined with the liposome membrane layer, so that the stability of the liposome is improved, the cohesion of the liposome is improved, and the particle size of the liposome is reduced.
In a preferred embodiment, the mass ratio of sunflower seed oil to tocopherol is 1:1.
In a preferred embodiment, the penetration enhancing component is selected from at least one of an alcohol compound, a fatty acid ester compound, a azone compound, pyrrolidone and derivatives thereof.
In a preferred embodiment, the penetration enhancer is an alcohol compound, preferably at least one selected from octyldodecanol, propylene glycol, pentanediol, menthol.
In a preferred embodiment, the permeation enhancer is octyldodecanol.
In a preferred embodiment, the liposome comprises, by mass, 10-30% of deionized water, 1-30% of a penetration promoting component, 0.1-1% of tocopherol, 0.1-1% of sunflower seed oil, 1-5% of ceramide, 1-20% of a liposome membrane component, and the balance of glycerol.
In a preferred embodiment, the liposome is prepared from 15-25% of deionized water, 1-15% of octyl dodecanol, 0.1-1% of tocopherol, 0.1-1% of sunflower seed oil, 1-5% of ceramide, 1-10% of phospholipid, 1-5% of hydrogenated phosphatidylcholine, 1-5% of cholesterol and the balance of glycerol.
In a preferred embodiment, the liposome is prepared from, by mass, 20% of deionized water, 1-15% of octyldodecanol, 0.5% of tocopherol, 0.5% of sunflower seed oil, 1-5% of ceramide, 1-5% of phospholipid, 1-2% of hydrogenated phosphatidylcholine, 1-2% of cholesterol and the balance of glycerol.
The second aspect of the present application provides a method for preparing an absorbable skin repair liposome, comprising the steps of:
(1) Adding ceramide, tocopherol, liposome membrane components and sunflower seed oil into a stirring container, and uniformly stirring to obtain a solution A;
(2) Adding glycerol, deionized water and permeation promoting components into a stirring container, and uniformly stirring to obtain a solution B;
(3) Slowly adding the solution A into the solution B, and homogenizing to obtain the liposome composition;
(4) And extruding the prepared liposome composition by using a nano-lipid extruder to obtain the liposome.
In a preferred embodiment, the temperature during the stirring in step (1) and step (2) is 60 ℃.
In a preferred embodiment, the specific operating conditions for the homogenization in step (3) are as follows: homogenizing under normal pressure at 60deg.C for 1-3 times for 10-15min at 5000-7000rpm.
In a preferred embodiment, the specific operation method of step (4) is as follows: extruding the liposome composition through an extrusion film by using a nano lipid extruder for 5-8 times.
In a preferred embodiment, the extruded film is a polyurethane film, the extruded film having a film diameter of 0.08 to 0.2 μm.
Compared with the prior art, the application has the beneficial effects that:
1. the ceramide liposome composition prepared by the application does not add a surfactant as an emulsifying agent, and forms a water dispersion system with deionized water, so that the ceramide liposome composition is not easy to foam and cannot stabilize foam. Meanwhile, sunflower seed oil and tocopherol are added, and the stability of the liposome is improved, the particle size of the liposome is reduced, and the dispersion performance of the liposome is also improved through the interaction of molecular groups.
2. The ceramide liposome composition prepared by the application has good compatibility with skin, is easy to be absorbed by the skin, and has the effects of moisturizing, whitening, diminishing inflammation and repairing the skin.
Detailed Description
Example 1
The first aspect of the embodiment provides an absorbable skin repair liposome, which is prepared from, by mass, 20% of deionized water, 12% of octyldodecanol, 0.5% of tocopherol, 0.5% of sunflower seed oil, 3% of ceramide NP, 5% of phospholipid, 2% of hydrogenated phosphatidylcholine, 2% of cholesterol and the balance of glycerol.
The octyl dodecanol is purchased from Basoff corporation under the trade designationG。
The tocopherol is purchased from imperial craftsman.
The sunflower seed oil is purchased from Hallstar Inc., USA under the trade designationSunflower Oil REF。
The ceramide NP was purchased from Korean Fangshan group under the model DS-CERAMIDE Y O.
The phospholipids were purchased from Korean Fangshan group under the model DS-SUN PC65.
The hydrogenated phosphatidylcholine was purchased from the Korean Fangshan group under the model DS-Soya HPC90.
The cholesterol was purchased from japan refinement.
The second aspect of the present embodiment provides a method for preparing an absorbable skin repair liposome, comprising the following steps:
(1) Adding ceramide NP, tocopherol (vitamin E), phospholipid, hydrogenated phosphatidylcholine, cholesterol and sunflower seed oil into a stirring container, and stirring at 60 ℃ to obtain a solution A;
(2) Adding glycerol, water and octyl dodecanol into a stirring container, and uniformly stirring at 60 ℃ to obtain a solution B;
(3) Slowly adding the solution A into the solution B, homogenizing under normal pressure at 60deg.C for 1 times for 13min at 5500rpm to obtain liposome composition;
(4) The liposome composition thus obtained was extruded 6 times using a nanolipid extruder to give a film polyurethane film having a film diameter of 0.08. Mu.m.
Example 2
The first aspect of the embodiment provides an absorbable skin repair liposome, which is prepared from, by mass, 20% of deionized water, 4% of octyldodecanol, 0.5% of tocopherol, 0.5% of sunflower seed oil, 1% of ceramide NP, 3% of phospholipid, 1% of hydrogenated phosphatidylcholine, 1% of cholesterol and the balance of glycerol.
The octyl dodecanol is purchased from Basoff corporation under the trade designationG。
The tocopherol is purchased from imperial craftsman.
The sunflower seed oil is purchased from Hallstar Inc., USA under the trade designationSunflower Oil REF。
The ceramide NP was purchased from Korean Fangshan group under the model DS-CERAMIDE Y O.
The phospholipids were purchased from Korean Fangshan group under the model DS-SUN PC65.
The hydrogenated phosphatidylcholine was purchased from the Korean Fangshan group under the model DS-Soya HPC90.
The cholesterol was purchased from japan refinement.
The second aspect of the present embodiment provides a method for preparing an absorbable skin repair liposome, comprising the following steps:
(1) Adding ceramide NP, tocopherol (vitamin E), phospholipid, hydrogenated phosphatidylcholine, cholesterol and sunflower seed oil into a stirring container, and stirring at 60 ℃ to obtain a solution A;
(2) Adding glycerol, water and octyl dodecanol into a stirring container, and uniformly stirring at 60 ℃ to obtain a solution B;
(3) Slowly adding the solution A into the solution B, homogenizing under normal pressure at 60deg.C for 1 times for 13min at 5500rpm to obtain liposome composition;
(4) The liposome composition thus obtained was extruded 6 times using a nanolipid extruder to give a film polyurethane film having a film diameter of 0.08. Mu.m.
Example 3
The first aspect of this example provides an absorbable skin repair liposome, and the second aspect of this example provides a method for preparing an absorbable skin repair liposome, wherein the raw materials and embodiments for the preparation are the same as those of example 1, except that no tocopherol or sunflower seed oil is added.
Example 4
The first aspect of the present embodiment provides an absorbable skin repair liposome, and the second aspect of the present embodiment provides a method for preparing an absorbable skin repair liposome, wherein the specific raw materials and embodiments for preparing the absorbable skin repair liposome are the same as those of embodiment 1, except that tween 60 with a mass percentage of 5% is added.
Performance testing
1. The liposome prepared in the example was tested for stability and defoaming effect. And mixing the prepared liposome with deionized water, wherein the volume ratio of the liposome to the deionized water is 1:19.
2. The liposomes prepared in example 1 and example 2 were subjected to zeta potential and liposome average particle size detection. The detection results are recorded in table 2.
TABLE 1
Stability of | Defoaming effect | |
Example 1 | 58 days | 35min |
Example 2 | 51 days | 32min |
Example 3 | For 24 days | 155min |
Example 4 | For 10 days | 49h |
TABLE 2
zeta potential (mV) | Average particle size of liposome (nm) | |
Example 1 | -35.93 | 125.51 |
Example 2 | -47.70 | 117.83 |
Claims (2)
1. An absorbable skin repair liposome, which is characterized by comprising the following preparation raw materials in percentage by mass: deionized water 20%, octyl dodecanol 1-15%, tocopherol 0.5%, sunflower seed oil 0.5%, ceramide 1-5%, phospholipid 1-5%, hydrogenated phosphatidylcholine 1-2%, cholesterol 1-2%, and glycerol for the balance;
the ceramide is ceramide NP.
2. A method of preparing a liposome according to claim 1, comprising the steps of:
(1) Adding ceramide, tocopherol, phospholipid, hydrogenated phosphatidylcholine, cholesterol and sunflower seed oil into a stirring container, and uniformly stirring to obtain a solution A;
(2) Adding glycerol, deionized water and octyl dodecanol into a stirring container, and uniformly stirring to obtain a solution B;
(3) Slowly adding the solution A into the solution B, and homogenizing to obtain a liposome composition;
(4) And extruding the prepared liposome composition by using a nano-lipid extruder to obtain the liposome.
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Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
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JP2012206948A (en) * | 2011-03-29 | 2012-10-25 | Kose Corp | Liposome composition, cosmetic and skin external preparation using the same, and method for producing the same |
CN104546516A (en) * | 2014-12-09 | 2015-04-29 | 美嘉乐(上海)生物科技有限公司 | Preparation process and application of compound ceramide liposome |
CN110638696A (en) * | 2019-10-25 | 2020-01-03 | 中南大学湘雅医院 | Composition for repairing skin barrier and preparation method and application thereof |
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Publication number | Priority date | Publication date | Assignee | Title |
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JP2012206948A (en) * | 2011-03-29 | 2012-10-25 | Kose Corp | Liposome composition, cosmetic and skin external preparation using the same, and method for producing the same |
CN104546516A (en) * | 2014-12-09 | 2015-04-29 | 美嘉乐(上海)生物科技有限公司 | Preparation process and application of compound ceramide liposome |
CN110638696A (en) * | 2019-10-25 | 2020-01-03 | 中南大学湘雅医院 | Composition for repairing skin barrier and preparation method and application thereof |
Non-Patent Citations (1)
Title |
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含有神经酰胺脂质体的研究进展;郑琪瑶;王士斌;刘源岗;;日用化学工业(01);50-54 * |
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