CN105816337A - Composite polyphenol active materials-loaded solid lipid particle and preparation method thereof - Google Patents
Composite polyphenol active materials-loaded solid lipid particle and preparation method thereof Download PDFInfo
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- CN105816337A CN105816337A CN201610244694.2A CN201610244694A CN105816337A CN 105816337 A CN105816337 A CN 105816337A CN 201610244694 A CN201610244694 A CN 201610244694A CN 105816337 A CN105816337 A CN 105816337A
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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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- 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
- A61K8/342—Alcohols having more than seven atoms in an unbroken chain
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
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- 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
- A61K8/347—Phenols
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- 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
- A61K8/37—Esters of carboxylic acids
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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
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
- A61K8/4973—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom
- A61K8/498—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom having 6-membered rings or their condensed derivatives, e.g. coumarin
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- 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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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
- A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
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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
- A61Q19/08—Anti-ageing preparations
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Abstract
The invention discloses a composite polyphenol active materials-loaded solid lipid particle and a preparation method thereof. The solid lipid particle is prepared from the following components by mass percent: 1%-4% of tea polyphenol, 1%-3% of resveratrol, 30%-37% of 1,3-butanediol, 25%-30% of lipid materials, 20%-25% of an emulsifier and the balance of deionized water. Water-soluble and lipid-soluble polyphenol materials are simultaneously loaded by the novel solid lipid particle; the solid lipid particle has good stability and water solubility; the preparation method is simple, controllable and good in repeatability; and the prepared solid lipid particle can be applied to household chemicals, health care products, food and the like as a raw material.
Description
Technical field
The invention belongs to the carrier system preparation field in cosmetics technology of preparing, relate to a kind of micro/nano level
The preparation method of carrier, particularly to a kind of micro-nano solid with two kinds of polyphenols as active component
Body lipid particles and preparation method thereof.
Background technology
Polyphenols active matter has non-oxidizability, in the diet being present in us that they are abundant, to the mankind
Health have potential benefit.As antioxidant, polyphenol can protect cellular component from oxidation
Damage, therefore, they are to the various diseases relevant to oxidative stress, as cancer, cardiovascular disease and
Neurodegenerative diseases etc., all have preventive effect.
Tea polyphenols is the general name of Polyphenols of Tea, has the effects such as anticancer, defying age, antiinflammatory,
Cosmetics, food and field of medicaments have broad application prospects.But tea polyphenols is the most oxidizable
Polymerization, in the alkalescence oxidizable brown stain of condition, is the most easily oxidized by oxygen, at water and polyphenol oxidase
In the environment that enzyme exists, phenolic hydroxyl group can generate o-quinone by dissociation etc., and o-quinone polymerization forms rufous and gathers
Compound.
Resveratrol is the plant polyphenol compounds of a kind of non-flavonoid, and its chemical name is 3,4', 5-tri-
Hydroxy stibene, has protection cardiovascular, defying age, the effect such as anticancer, at cosmetics, food
And the application prospect of field of medicaments is boundless.But resveratrol is practically insoluble in water, it is oxidized easily
Degraded, limits its application to physicochemical properties such as light are very sensitive.
As the compound use of Polyphenols active matter, tea polyphenols and resveratrol, there is synergism, energy
Enough strengthen antioxidation efficiency etc..
Micro-nano carrier technique is as a kind of resist technology, it is possible to protect some to have volatility, sensitivity
Or the active matter of the physicochemical property such as degradable, make their application preferably be played.Micro-nano load
Target, by having the material of good biocompatibility, is lived by body technique by methods such as dissolving, absorption
Property thing parcel or be attached to micron or the inside of submicron carrier particle or the surface formed, it is achieved dissolve
The purposes such as degree and bioavailability raising, stability enhancing and targeted.
Liposome, water-in-oil emulsion and multiple emulsion can simultaneously load water soluble and liposoluble active
Thing.But the structure of liposome is relatively unstable；The foreign minister of water-in-oil emulsion is oils and fats, limits it
Application, and multiple emulsion is a kind of thermodynamic unstable system, and the situation such as breakdown of emulsion, flocculation easily occurs.
Summary of the invention
It is an object of the invention to provide a kind of solid lipid microgranule loading compound Polyphenols active matter and
Preparation method, is a kind of thermodynamic unstable system to solve multiple emulsion present in prior art,
The problem that breakdown of emulsion, flocculation easily occur.
For achieving the above object, the technical solution used in the present invention is:
A kind of solid lipid microgranule loading compound Polyphenols active matter, according to mass percent, its raw material
Composed of the following components: tea polyphenols 1-4%；Resveratrol 1-3%；1,3 butylene glycol 30-37%；Fat
Material 25-30%；Emulsifying agent 20-25%；Surplus is deionized water.
Further, described matrix material is the mixture of liquid fatty substance and Solid lipid.
Further, described liquid fatty substance material be decanoyl/octanoyl glycerides, Semen Maydis oil, macadimia nut oil,
One or both in soybean oil, described Solid lipid material is cetostearyl alcohol, glycerol monostearate
One or both in ester.
Further, in described matrix material, liquid fatty substance material accounts for solid lipid weight percentage of fines
20-23%；Solid lipid material accounts for the 5-7% of solid lipid weight percentage of fines.
Further, described emulsifying agent is made up of lipophilic emulsifier and hydrophilic emulsifier.
Further, described lipophilic emulsifier is polyglycerol polyricinoleate, Polyethylene Glycol-30-dimerization hydroxyl
One or both in base stearate；Described hydrophilic emulsifier is Polyethylene Glycol-23-Laurel acid alcohol
One or both in ether, polyoxyethylene sorbitan fatty acid ester.
Further, described lipophilic emulsifier accounts for the 9-12% of solid lipid weight percentage of fines；Institute
State hydrophilic emulsifier and account for the 11-13% of solid lipid weight percentage of fines.
The preparation method of a kind of solid lipid microgranule loading compound Polyphenols active matter, including following step
Rapid:
Step one, adds tea polyphenols and resveratrol in solvent, and 60-70 DEG C stirs, as interior water
Phase；Weigh matrix material and lipophilic emulsifier, melt in 60-70 DEG C and stir, as oil phase；
Step 2, interior aqueous phase step one obtained adds in oil phase, after pre-emulsification, high shear, high pressure
Homogenizing or ultrasonic；
Step 3, adds hydrophilic emulsifier, after stirring in 50-60 DEG C, is cooled to cold curing,
Prepare the solid lipid microgranule of the compound Polyphenols active matter of load.
On the basis of such scheme, described compound Polyphenols active matter is in solid lipid microgranule
Weight percentage is 2-7%.
The invention has the beneficial effects as follows: the present invention, as a kind of new carrier technique, is used in combination multiple
Oil phase in emulsion and lipid nanoparticle technology, i.e. multiple emulsion selects mushy stage mixing lipid, will
Water solublity and fat-soluble Polyphenols active matter are concurrently placed in interior aqueous phase, more traditional multiple of this structure
Emulsion is more stable, and the solid lipid microgranule of the compound Polyphenols active matter of load prepared can conduct
Raw material, adds to cosmetics, health product and food etc., effectively solves defect present on application.
Accompanying drawing explanation
Fig. 1 is the preparation method flow chart of the solid lipid microgranule containing the compound Polyphenols active matter of load.
Detailed description of the invention
Below in conjunction with specific embodiment, such scheme is described further.These embodiments are for saying
The bright present invention and be not limited to limit the scope of the present invention.The implementation condition used in embodiment can basis
The condition of concrete producer does adjustment further, and not marked implementation condition is usually the bar in normal experiment
Part.
Embodiment 1
It is combined as formula:
The preparation method of the solid lipid microgranule of the compound Polyphenols active matter of load:
The first step: weigh 4g tea polyphenols, 1g resveratrol, 35g 1,3 butylene glycol and 11g deionization
Water, 70 DEG C of waters bath with thermostatic control are heated and stirred to be made it be completely dissolved and stirs, and is formed containing compound polyphenol
The solution of class active matter, as interior aqueous phase；
Weigh 22g decanoyl/octanoyl glycerides, 10g polyglycereol Semen Ricini alcohol ester, 6g cetostearyl alcohol, 70 DEG C
Water bath with thermostatic control is heated and stirred to be made it be completely dissolved and stirs, as oil phase；
Second step: be slowly added in oil phase by interior aqueous phase, is stirred 5 minutes, after mix homogeneously simultaneously,
10000rpm high shear 3 minutes；
3rd step: add 11g Polyethylene Glycol-23-lauric acid alcohol ether, 50 DEG C of waters bath with thermostatic control in mixture
Heat, and stirring makes its mix homogeneously, be cooled to room temperature solidification, obtain loading compound Polyphenols activity
The solid lipid microgranule of thing.
Being disperseed in deionized water by solid lipid microgranule, this dispersion liquid records its mean diameter by particle size analyzer
It is 1.17 μm.
Embodiment 2
It is combined as formula:
The preparation method of the solid lipid microgranule of the compound Polyphenols active matter of load:
The first step: weigh 3g tea polyphenols, 2g resveratrol, 36g 1,3 butylene glycol and 10g deionization
Water, 70 DEG C of waters bath with thermostatic control are heated and stirred to be made it be completely dissolved and stirs, and is formed containing compound polyphenol
The solution of class active matter, as interior aqueous phase；
Weigh 23g Semen Maydis oil, 10g Polyethylene Glycol-30-dimerization hydroxy stearic acid ester, 5g monostearate
Glyceride, 70 DEG C of waters bath with thermostatic control are heated and stirred to be made it be completely dissolved and stirs, as oil phase；
Second step: be slowly added in oil phase by interior aqueous phase, is stirred 5 minutes, after mix homogeneously simultaneously,
600bar high pressure homogenize 3 circulation；
3rd step: add 11g polyoxyethylene sorbitan monooleate dehydration, 50 DEG C of water-baths in mixture
Heating, and stirring makes its mix homogeneously, be cooled to room temperature solidification, it is active that prepared load is combined Polyphenols
The solid lipid microgranule of thing.
Being disperseed in deionized water by solid lipid microgranule, this dispersion liquid records its mean diameter by particle size analyzer
It it is 0.91 μm.
Embodiment 3
It is combined as formula:
The preparation method of the solid lipid microgranule of the compound Polyphenols active matter of load:
The first step: weigh 1g tea polyphenols, 3g resveratrol, 37g 1,3 butylene glycol and 10g deionization
Water, 70 DEG C of waters bath with thermostatic control are heated and stirred to be made it be completely dissolved and stirs, and is formed containing compound polyphenol
The solution of class active matter, as interior aqueous phase；
Weigh 22g soybean oil, 10g Polyethylene Glycol-30-dimerization hydroxy stearic acid ester, 6g 16
Alcohol, 70 DEG C of waters bath with thermostatic control are heated and stirred to be made it be completely dissolved and stirs, as oil phase；
Second step: be slowly added in oil phase by interior aqueous phase, is stirred 5 minutes, after mix homogeneously simultaneously,
Ultrasonic 7 minutes；
3rd step: addition 11g Polyethylene Glycol-23-lauric acid alcohol ether in mixture, 50 DEG C of heating in water bath,
And stirring makes its mix homogeneously, it is cooled to room temperature solidification, prepares consolidating of the compound Polyphenols active matter of load
Body lipid particles.
Being disperseed in deionized water by lipid particles, it is 2.39 that this dispersion liquid records its particle diameter by particle size analyzer
μm。
Embodiment 4
It is combined as formula:
The preparation method of the solid lipid microgranule of the compound Polyphenols active matter of load:
The first step: weigh 1g tea polyphenols, 3g resveratrol, 30g 1,3 butylene glycol and 16g deionization
Water, 70 DEG C of waters bath with thermostatic control are heated and stirred to be made it be completely dissolved and stirs, and is formed containing compound polyphenol
The solution of class active matter, as interior aqueous phase；
Weigh 23g macadimia nut oil, 9g Polyethylene Glycol-30-dimerization hydroxy stearic acid ester, 7g 16
Eight alcohol and the mixture of glyceryl monostearate, 70 DEG C of waters bath with thermostatic control are heated and stirred makes it be completely dissolved
And stir, as oil phase；
Second step: be slowly added in oil phase by interior aqueous phase, is stirred 5 minutes, after mix homogeneously simultaneously,
Ultrasonic 7 minutes；
3rd step: add 11g Polyethylene Glycol-23-lauric acid alcohol ether and polyoxyethylene sorbitan in mixture
The mixture of Span, 50 DEG C of heating in water bath, and stirring make its mix homogeneously, are cooled to
Room temperature solidifies, and prepares the solid lipid microgranule of the compound Polyphenols active matter of load.
Being disperseed in deionized water by solid lipid microgranule, this dispersion liquid records its particle diameter by particle size analyzer and is
1.42μm。
Embodiment 5
It is combined as formula:
The preparation method of the solid lipid microgranule of the compound Polyphenols active matter of load:
The first step: weigh 2g tea polyphenols, 3g resveratrol, 33g 1,3 butylene glycol and 12g deionization
Water, 70 DEG C of waters bath with thermostatic control are heated and stirred to be made it be completely dissolved and stirs, and is formed containing compound polyphenol
The solution of class active matter, as interior aqueous phase；
Weigh the mixture of 20g soybean oil and Semen Maydis oil, 12g polyglycerol polyricinoleate and Polyethylene Glycol
The mixture of-30-dimerization hydroxy stearic acid ester, 5g cetostearyl alcohol, 70 DEG C of waters bath with thermostatic control are heated and stir
Mix and make it be completely dissolved and stir, as oil phase；
Second step: be slowly added in oil phase by interior aqueous phase, is stirred 5 minutes, after mix homogeneously simultaneously,
600bar high pressure homogenize 3 circulation；
3rd step: addition 13g Polyethylene Glycol-23-lauric acid alcohol ether in mixture, 50 DEG C of heating in water bath,
And stirring makes its mix homogeneously, it is cooled to room temperature solidification, prepares consolidating of the compound Polyphenols active matter of load
Body lipid particles.
Being disperseed in deionized water by solid lipid microgranule, this dispersion liquid records its particle diameter by particle size analyzer and is
1.61μm。
Claims (9)
1. the solid lipid microgranule of the compound Polyphenols active matter of load, it is characterised in that: according to quality hundred
Proportion by subtraction, its raw material is composed of the following components: tea polyphenols 1-4%；Resveratrol 1-3%；1,3 butylene glycol
30-37%；Matrix material 25-30%；Emulsifying agent 20-25%；Surplus is deionized water.
Load the most according to claim 1 is combined the solid lipid microgranule of Polyphenols active matter, its feature
It is: described matrix material is the mixture of liquid fatty substance and Solid lipid.
Load the most according to claim 2 is combined the solid lipid microgranule of Polyphenols active matter, its feature
It is: described liquid fatty substance material is decanoyl/octanoyl glycerides, Semen Maydis oil, macadimia nut oil, soybean oil
In one or both, described Solid lipid material is in cetostearyl alcohol, glyceryl monostearate
One or both.
Load the most according to claim 3 is combined the solid lipid microgranule of Polyphenols active matter, its feature
Being: in described matrix material, liquid fatty substance material accounts for solid lipid weight percentage of fines
20-23%；Solid lipid material accounts for the 5-7% of solid lipid weight percentage of fines.
Load the most according to claim 1 is combined the solid lipid microgranule of Polyphenols active matter, its feature
It is: described emulsifying agent is made up of lipophilic emulsifier and hydrophilic emulsifier.
Load the most according to claim 5 is combined the solid lipid microgranule of Polyphenols active matter, its feature
It is: described lipophilic emulsifier is polyglycerol polyricinoleate, Polyethylene Glycol-30-dimerization hydroxy stearic acid
One or both in ester；Described hydrophilic emulsifier is Polyethylene Glycol-23-lauric acid alcohol ether, polyoxy second
One or both in alkene sorbitan fatty acid ester.
Load the most according to claim 6 is combined the solid lipid microgranule of Polyphenols active matter, its feature
It is: described lipophilic emulsifier accounts for the 9-12% of solid lipid weight percentage of fines；Described hydrophilic
Property emulsifying agent accounts for the 11-13% of solid lipid weight percentage of fines.
Load the most according to claim 1 is combined the solid lipid microgranule of Polyphenols active matter, its feature
It is: described compound Polyphenols active matter weight percentage in solid lipid microgranule is 2-7%.
9. the solid lipid microgranule of the compound Polyphenols active matter of the arbitrary described load of claim 1-8
Preparation method, it is characterised in that: comprise the following steps:
Step one, adds tea polyphenols and resveratrol in solvent, and 60-70 DEG C stirs, as interior water
Phase；Weigh matrix material and lipophilic emulsifier, melt in 60-70 DEG C and stir, as oil phase；
Step 2, interior aqueous phase step one obtained adds in oil phase, after pre-emulsification, high shear, high pressure
Homogenizing or ultrasonic；
Step 3, adds hydrophilic emulsifier, after stirring in 50-60 DEG C, is cooled to cold curing,
Prepare the solid lipid microgranule of the compound Polyphenols active matter of load.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110409174A (en) * | 2019-08-07 | 2019-11-05 | 苏州经贸职业技术学院 | A kind of phenols environmental protection finishing agent and preparation method thereof |
| CN113907355A (en) * | 2021-10-19 | 2022-01-11 | 南昌大学 | Water-phase crystallization type water-in-oil emulsion and preparation method thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010051918A2 (en) * | 2008-11-04 | 2010-05-14 | Pharmasol Gmbh | Compositions containing lipid micro- or nanoparticles for the enhancement of the dermal action of solid particles |
| CN103976901A (en) * | 2014-05-22 | 2014-08-13 | 东南大学 | Coenzyme Q10 and tea polyphenol loaded micro-nano carrier, as well as preparation and application methods thereof |
-
2016
- 2016-04-19 CN CN201610244694.2A patent/CN105816337A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010051918A2 (en) * | 2008-11-04 | 2010-05-14 | Pharmasol Gmbh | Compositions containing lipid micro- or nanoparticles for the enhancement of the dermal action of solid particles |
| CN103976901A (en) * | 2014-05-22 | 2014-08-13 | 东南大学 | Coenzyme Q10 and tea polyphenol loaded micro-nano carrier, as well as preparation and application methods thereof |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110409174A (en) * | 2019-08-07 | 2019-11-05 | 苏州经贸职业技术学院 | A kind of phenols environmental protection finishing agent and preparation method thereof |
| CN113907355A (en) * | 2021-10-19 | 2022-01-11 | 南昌大学 | Water-phase crystallization type water-in-oil emulsion and preparation method thereof |
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Application publication date: 20160803 |
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