CN110151603A - A kind of nano-encapsulated leonurine liposome and the preparation method and application thereof - Google Patents
A kind of nano-encapsulated leonurine liposome and the preparation method and application thereof Download PDFInfo
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- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
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- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
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Abstract
The invention discloses a kind of nano-encapsulated leonurine liposome and the preparation method and application thereof, the raw material for preparing of the nano-encapsulated leonurine liposome is comprised the following components in parts by weight: leonurine: 0.1-5;Raw element C:1-4;Lecithin: 5-40;Cholesterol: 10-20;Glycerol: 1-100.The preparation method includes above step: S1, being heated to carrying out sterilization treatment after being completely dissolved after mixing lecithin, cholesterol and glycerol, and ethyl alcohol is added into the solution after sterilization treatment, obtain mixed solution;S2, injection leonurine and vitamin C, insulated and stirred;S3, it is placed in high-pressure homogeneous middle processing, obtains the leonurine liposome of the nano-encapsulated after dry.Nano-encapsulated leonurine liposome has slow releasing function, can discharge slowly and for a long time active principle in lesion, play significant biological action, while avoiding skin adverse reaction caused by the leonurine of bolus.
Description
Technical field
The present invention relates to cosmetic technical fields, and in particular to a kind of nano-encapsulated leonurine liposome and its preparation side
Method and application.
Background technique
Leonurine is that isolated alkaloid is extracted from Chinese medicine motherwort, and clinically there are many motherworts at present
Preparation, such as capsule, tablet, paste, granule and injection.In recent years, correlative study discovery leonurine also has antioxygen
The properties such as change, anti-apoptotic, antibacterial, anti-acne, it is therefore, more and more for research of the leonurine in cosmetics.However, due to
The phenolic hydroxyl group and guanidino group polarity contained in leonurine structure is larger, cause leonurine it is fat-soluble it is poor, cross-film ability is weak,
Bioavilability is low.And leonurine is more toxic, and is directly acted on skin and is had stimulation.This makes answering for leonurine
With by certain obstruction.
Nano structured lipid carrier is that partial size is made using spatially incompatible Solid lipid and liquid fatty substance as carrier
Liquid fatty substance is added into Solid lipid at a certain temperature for nano novel drug delivery system within the scope of 100~1000nm,
Make the reduction of its ordered arrangement degree, form the lipid carrier skeleton containing special lar nanometric cavities, drugloading rate and encapsulating both can be improved
Rate reduces and is encapsulated drug and leaks, and can preferably adjust drug release effect, is a kind of the novel of great development prospect
Medicament carrier system has been obtained as the carrier through epidermis, oral or intravenous administration and is widely applied.
Therefore, if being expected to overcome motherwort in cosmetics by being applied to after the liposome of leonurine nanostructure
Application limitation caused by alkali structure itself, however, there has been no relevant reports in the prior art.
Summary of the invention
The first technical problem to be solved by the present invention is: providing one kind, can to slow down leonurine bad to skin anti-
The nano-encapsulated leonurine liposome answered.
Second technical problem to be solved by this invention is: providing a kind of above-mentioned nano-encapsulated leonurine liposome
Preparation method.
Third technical problem to be solved by this invention is: providing a kind of above-mentioned nano-encapsulated leonurine liposome
Using.
In order to solve above-mentioned first technical problem, the technical solution adopted by the present invention are as follows: a kind of nano-encapsulated motherwort
The raw material for preparing of alkali liposome, the nano-encapsulated leonurine liposome comprises the following components in parts by weight:
Leonurine: 0.1-5;
Vitamin C: 1-4;
Lecithin: 5-40;
Cholesterol: 10-20;
Glycerol: 1-100.
Preferably, the raw material for preparing comprises the following components in parts by weight:
Leonurine: 1.5-4;
Vitamin C: 2-3;
Lecithin: 30-35;
Cholesterol: 15-25;
Glycerol: 30-50.
In order to solve above-mentioned second technical problem, the technical solution adopted by the present invention are as follows: a kind of nano-encapsulated motherwort
The preparation method of alkali liposome, including above step:
S1, each component prepared in raw material is weighed, is carried out after dissolution is heated to after lecithin, cholesterol and glycerol are mixed
Sterilization treatment, and ethyl alcohol is added into the solution after sterilization treatment, obtain mixed solution;
S2, leonurine and vitamin C are injected into mixed solution obtained in step S1, be kept stirring and maintain to react
The constant 50-80min at 55~70 DEG C of the temperature of system;
S3, by above-mentioned steps S2 treated solution is placed in high-pressure homogeneous middle processing, obtain the nano-encapsulated after dry
Leonurine liposome.
Further, the disinfecting action in the step S1 is that 15~25min of isothermal holding is (preferably at 80~100 DEG C
For 20min).
Further, the high pressure in the step S3 is 3~5MPa.
The invention has the benefit that leonurine is a kind of traditional Chinese medicine ingredients with anti-inflammatory, anti-acne, but when large dosage
When leonurine acts on skin, it will lead to the adverse reactions such as stimulation skin.Therefore, the nano-encapsulated benefit obtained after treatment
Brittle Falsepimpernel Herb alkali liposome has slow releasing function, can discharge slowly and for a long time active principle in lesion, play significant biology
Effect, while avoiding skin adverse reaction caused by the leonurine of bolus.
To solve above-mentioned third technical problem, the solution of the present invention are as follows: one kind contains above-mentioned nano-encapsulated leonurine
The face cream of liposome.
Further, the weight accounting for preparing nano-encapsulated leonurine liposome in raw material of the face cream be (1~
10) %.
Further, the face cream prepares the component that raw material further includes following parts by weight:
Hyaluronic acid: (0.03-0.07) wt%;
Glycerol: (4-6) wt%;
Cyclic dimethylsiloxane: (1-3) wt%;
Dimethicone: (1-4) wt%;
Tocopherol: (2-4) wt%;
Saualane: (1-3) wt%;
GTCC:(1-3) wt%;
Shea butter: (1-2) wt%;
Emulsifing thickener 305:(1-4) wt%;
A631:(0.1-1) wt%;
Deionized water: surplus.
To solve above-mentioned third technical problem, the solution of the present invention may also is that a kind of nano-encapsulated leonurine rouge
Application of the anti-inflammatory anti-acne of plastid in the preparation of face cream, includes the following steps:
(1) A phase is prepared: high-speed stirred is warming up under stirring to dispersion after deionized water, glycerol, hyaluronic acid are mixed
At the uniform velocity A phase materials are made after stirring insulated sterilizing in (85~95) DEG C;
(2) B phase is prepared: by cyclic dimethylsiloxane, cyclic dimethylsiloxane, tocopherol, saualane, the octanoic acid/last of the ten Heavenly stems
(80~90) are heated to after acid glycerol three ester (CAPRYLIC/CAPRIC TRIGLYCERIDE, GTCC) and shea butter mixing
DEG C, it is added after dissolution into A phase materials and B phase materials is made;
(3) B phase materials obtained are cooled to after (55~65) DEG C under stiring, emulsifing thickener 305 are added, and carry out
Homogeneous operates to obtain finely dispersed mixture;
(4) continue stirring and be cooled to 45 DEG C, and A631 and nano-encapsulated leonurine liposome are added to above-mentioned steps
(3) in mixture made from, and continue stirring to being uniformly dispersed, stop stirring, obtaining after cooling is female containing nano-encapsulated benefit
The face cream of potash liposome.
Further, in the step (1), the mixing speed is 500-800r/min.
Further, in the step (3), homogeneous revolving speed is 3000-5000r/min, and the homogenizing time is 20-60 points
Clock.
The beneficial effects of the present invention are: glycerol and shea butter all have moisture-keeping function, face made from the present invention program
Frost not only has the function of anti-inflammatory anti-acne, while can also keep skin moisture, reaches moisturizing effect.Vitamin C has whitening
Effect, leonurine solubility is low, if being simply added in face cream system, can be difficult to dissolve, and the present invention program is logical
It crosses and is prepared into after the liposome of nano-encapsulated, increase it in the solubility of face cream system, final nanometer packet obtained
It wraps up in the anti-inflammatory Pimple removing scream of leonurine and is free of any toxic component, it is safe and non-stimulating, it can be applied in daily skin care, and there is length
Long stability, is with a wide range of applications.
Specific embodiment
To explain the technical content, the achieved purpose and the effect of the present invention in detail, it is explained below in conjunction with embodiment.
The embodiment of the present invention 1 are as follows: a kind of nano-encapsulated leonurine liposome, the liposome are by following mass component
Raw material is made, leonurine: 1.5wt%, vitamin C: 2wt%, lecithin: 35wt%, cholesterol: 15wt%, glycerol:
46.5wt%.
Specific preparation process is as follows:
A, each component is weighed, lecithin, cholesterol and glycerol water-bath are added into beaker and is heated to being completely dissolved, and 90
20min is kept the temperature at DEG C to reach sterilization effect, and 50mL ethyl alcohol, solution after being mixed are added into solution;
B, 60 DEG C of waters bath with thermostatic control heating and under stiring, will be slowly injected into solution obtained in step A leonurine and
Vitamin C, mixing speed 200r/min, heating water bath constant temperature time are 60min.
The solution that C obtains above-mentioned step B is placed in high-pressure homogeneous middle processing 30min, so that partial size is reached requirement, high pressure is equal
Matter pressure is 3MPa, and freeze-drying obtains the leonurine liposome of nano-encapsulated.
The embodiment of the present invention 2 are as follows: a kind of nano-encapsulated leonurine liposome, the liposome are by following mass component
Raw material is made, leonurine: 2wt%, vitamin C: 3wt%, lecithin: 30wt%, cholesterol: 20wt%, glycerol:
45wt%.
Specific preparation process is as follows:
A, each component is weighed, lecithin, cholesterol and glycerol water-bath are added into beaker and is heated to being completely dissolved, and 90
20min is kept the temperature at DEG C to reach sterilization effect, and 50mL ethyl alcohol, solution after being mixed are added into solution;
B, 60 DEG C of waters bath with thermostatic control heating and under agitation, will be slowly injected into motherwort in solution obtained in step A
Alkali and vitamin C, mixing speed 250r/min, constant temperature water bath time are 60min.
C, the solution for obtaining above-mentioned step B is placed in high-pressure homogeneous middle processing 40min, so that partial size is reached requirement, high pressure is equal
Matter pressure is 4MPa, and freeze-drying obtains the leonurine liposome of nano-encapsulated.
The embodiment of the present invention 3 are as follows: a kind of nano-encapsulated leonurine liposome, the liposome are by following mass component
Raw material is made, leonurine: 4wt%, vitamin C: 3.5wt%, lecithin: 35wt%, cholesterol: 25wt%, glycerol:
32.5wt%
A weighs each component, and into beaker, addition lecithin, cholesterol, glycerol water-bath are heated to being completely dissolved, and at 90 DEG C
40mL ethyl alcohol, solution after being mixed are added into solution to reach sterilization effect by lower holding 20min;
60 DEG C of waters bath with thermostatic control of B heating and under agitation, will be slowly injected into motherwort in solution obtained in step A
Alkali and vitamin C, mixing speed 250r/min, water bath with thermostatic control heating time are 70min.
The solution that C obtains above-mentioned step B is placed in high-pressure homogeneous middle processing 50min, so that partial size is reached requirement, high pressure is equal
Matter pressure is 5MPa, and freeze-drying obtains the leonurine liposome of nano-encapsulated.
The embodiment of the present invention 4 are as follows: a kind of preparation method of the anti-inflammatory Pimple removing scream of nano-encapsulated leonurine liposome, the face
Frost is made of the raw material of following mass component, nano-encapsulated leonurine liposome (above-described embodiment 1 is prepared)
2.6wt%;Deionized water: 75.43wt%;Hyaluronic acid: 0.07wt%;Glycerol: 6wt%;Cyclic dimethylsiloxane
(DC345): 2wt%;Dimethicone (DC200/100): 2wt%;Tocopherol: 3wt%;Saualane: 2wt%;GTCC:
2wt%;Shea butter: 1.8wt%;Emulsifing thickener 305:2.5wt%;A631:0.60wt%.
Detailed process is as follows:
(1) A phase is prepared: deionized water, glycerol, hyaluronic acid being once added in beaker, high-speed stirred is to uniform point
It clears complete, mixing speed 500r/min;
(2) 90 DEG C are warming up under lasting stirring, at the uniform velocity stirring heat preservation 20 minutes with sterilizing;
(3) B phase is prepared: separately taking a beaker, DC345, DC200/100, tocopherol, saualane, GTCC, cream is once added
The wooden fruit oil, is heated to 85 DEG C, is added after dissolution into A phase, starts to cool down;
(4) it is cooled to after 60 DEG C under stiring, emulsifing thickener 305 is added, and so that it is uniformly dispersed using homogenizer,
Matter speed of agitator is 3000r/min, and homogenizing time is 20 minutes.
(5) continue stirring and be cooled to 45 DEG C, A631 and nano-encapsulated leonurine liposome are added to said mixture
In, and continue stir about 10 minutes to being uniformly dispersed, stop stirring, obtains nano-encapsulated leonurine lipid dignity after cooling
Frost is named as face cream 1.
The embodiment of the present invention 5 are as follows: a kind of preparation method of the anti-inflammatory Pimple removing scream of nano-encapsulated leonurine liposome, the face
Frost is made of the raw material of following mass component, nano-encapsulated leonurine liposome (above-described embodiment 2 is prepared)
4.5wt%;Deionized water: 74.18wt%;Hyaluronic acid: 0.05wt%;Glycerol: 4wt%;Cyclic dimethylsiloxane
(DC345): 2.3wt%;Dimethicone (DC200/100): 3.1wt%;Tocopherol: 2.6wt%;Saualane: 2.5wt%;
GTCC:2.1wt%;Shea butter: 2.3wt%;Emulsifing thickener 305:2.1wt%;A631:0.09wt%.
Include the following steps:
(1) A phase is prepared: deionized water, glycerol, hyaluronic acid being once added in beaker, high-speed stirred is to uniform point
It clears complete, mixing speed 700r/min;
(2) 90 DEG C are warming up under uniform stirring, at the uniform velocity stirring heat preservation 20 minutes with sterilizing;
(3) B phase is prepared: separately taking a beaker, DC345, DC200/100, tocopherol, saualane, GTCC, cream is once added
The wooden fruit oil, is heated to 85 DEG C, is added after dissolution into A phase, starts to cool down;
(4) it is cooled to after 60 DEG C under stiring, emulsifing thickener 305 is added, and so that it is uniformly dispersed using homogenizer,
Matter speed of agitator is 4000r/min, and homogenizing time is 50 minutes.
(5) continue stirring and be cooled to 45 DEG C, A631 and nano-encapsulated leonurine liposome are added to said mixture
In, and continue stir about 10 minutes to being uniformly dispersed, stop stirring, obtains nano-encapsulated leonurine lipid dignity after cooling
Frost is named as face cream 2.
The embodiment of the present invention 6 are as follows: a kind of preparation method of the anti-inflammatory Pimple removing scream of nano-encapsulated leonurine liposome, the face
Frost is made of the raw material of following mass component, nano-encapsulated leonurine liposome (above-described embodiment 3 is prepared)
5wt%;Deionized water: 73.77wt%;Hyaluronic acid: 0.03wt%;Glycerol: 4wt%;Cyclic dimethylsiloxane
(DC345): 2.5wt%;Dimethicone (DC200/100): 1.5wt%;Tocopherol: 2.9wt%;Saualane: 1.5wt%;
GTCC:3wt%;Shea butter: 2.3wt%;Emulsifing thickener 305:3wt%;A631:0.5wt%.
Include the following steps:
(1) A phase is prepared: deionized water, glycerol, hyaluronic acid being once added in beaker, high-speed stirred is to uniform point
It clears complete, mixing speed 800r/min;
(2) 90 DEG C are warming up under uniform stirring, at the uniform velocity stirring heat preservation 20 minutes with sterilizing;
(3) B phase is prepared: separately taking a beaker, DC345, DC200/100, tocopherol, saualane, GTCC, cream is once added
The wooden fruit oil, is heated to 85 DEG C, is added after dissolution into A phase, starts to cool down;
(4) it is cooled to after 60 DEG C under stiring, emulsifing thickener 305 is added, and so that it is uniformly dispersed using homogenizer,
Matter speed of agitator is 5000r/min, and homogenizing time is 60 minutes.
(5) continue stirring and be cooled to 45 DEG C, A631 and nano-encapsulated leonurine liposome are added to said mixture
In, and continue stir about 10 minutes to being uniformly dispersed, stop stirring, obtains nano-encapsulated leonurine lipid dignity after cooling
Frost is named as face cream 3.
Reference examples 1 of the present invention are as follows: a kind of preparation method of the anti-inflammatory Pimple removing scream of leonurine, it is by following mass component
Raw material be made: leonurine 2.6wt%;Deionized water: 75.43wt%;Hyaluronic acid: 0.07wt%;Glycerol: 6wt%;Ring
Shape dimethyl siloxane (DC345): 2wt%;Dimethicone (DC200/100): 2wt%;Tocopherol: 3wt%;Saualane:
2wt%;GTCC:2wt%;Shea butter: 1.8wt%;Emulsifing thickener 305:2.5wt%;A631:0.60wt%.
Include the following steps:
(1) A phase is prepared: deionized water, glycerol, hyaluronic acid being once added in beaker, high-speed stirred is to uniform point
It clears complete, mixing speed 500r/min;
(2) 90 DEG C are warming up under uniform stirring, at the uniform velocity stirring heat preservation 20 minutes with sterilizing;
(3) B phase is prepared: separately taking a beaker, DC345, DC200/100, tocopherol, saualane, GTCC, cream is once added
The wooden fruit oil, is heated to 85 DEG C, is added after dissolution into A phase, starts to cool down;
(4) it is cooled to after 60 DEG C under stiring, emulsifing thickener 305 is added, and so that it is uniformly dispersed using homogenizer,
Matter speed of agitator is 3000r/min, and homogenizing time is 20 minutes.
(5) continue stirring and be cooled to 45 DEG C, A631 and leonurine are added in said mixture, and continue stir about
To being uniformly dispersed, stop stirring, obtain leonurine face cream after cooling, be named as face cream 4 within 10 minutes.
Comparative example 1 and the difference of embodiment 4 are that the form of leonurine is different, and comparative example is leonurine solid, real
Applying example 4 is nano-encapsulated leonurine liposome.
100 volunteers are collected, treatment group 50 and control group 50 is equally divided into.Treatment group course of disease 1-10, average 6
Year, the age 12-36 years old, average age was 25 years old;Control group course of disease 1-10, average 7 years, the age 12-36 years old, average age was
24 years old.
Therapeutic scheme: two groups after daily with clear water by face wash clean, face cream 1 that treatment group will give embodiment 4 and prepare
Affected part is smeared, control group gives the face cream 4 prepared in comparative example 1 and is applied to affected part, adheres to using 1 month, owns during observation
Patient deactivates other any drugs.
Curative effect judgement: 1. cure: skin affected part cures completely, does not occur new acne or fash;2. effectively: skin injury is repaired
Multiple 70% or more;3. improving: skin injury repairs 20% or more;4. invalid: skin injury repairs 20% or less.
As the result is shown: treatment group's total effective rate is 95%, and control group effective percentage is 50%, two groups of therapeutic effects comparisons such as table
Shown in 1:
Influence of the different face creams of table 1 to patient outcomes
Conclusion: the face cream by nano-encapsulated leonurine liposome preparation has more preferably anti-acne than leonurine face cream
Anti-inflammatory effects.Similarly, face cream 2 made from Example 5 and 6 and face cream 3 carry out anti-acne experiment, as the result is shown its cure rate point
It Wei 96% and 94%.
The above description is only an embodiment of the present invention, is not intended to limit the scope of the invention, all to utilize this hair
Equivalents made by bright description are applied directly or indirectly in relevant technical field, are similarly included in this hair
In bright scope of patent protection.
Claims (10)
1. a kind of nano-encapsulated leonurine liposome, it is characterised in that: the preparation of the nano-encapsulated leonurine liposome
Raw material comprises the following components in parts by weight:
Leonurine: 0.1-5;
Vitamin C: 1-4;
Lecithin: 5-40;
Cholesterol: 10-20;
Glycerol: 1-100.
2. nano-encapsulated leonurine liposome according to claim 1, it is characterised in that: it is described prepare raw material include with
The component of lower parts by weight:
Leonurine: 1.5-4;
Vitamin C: 2-3;
Lecithin: 30-35;
Cholesterol: 15-25;
Glycerol: 30-50.
3. a kind of preparation method of nano-encapsulated leonurine liposome as claimed in claim 1 or 2, it is characterised in that: packet
Include above step:
S1, each component prepared in raw material is weighed, sterilized after dissolution is heated to after lecithin, cholesterol and glycerol are mixed
Processing, and ethyl alcohol is added into the solution after sterilization treatment, obtain mixed solution;
S2, leonurine and vitamin C are injected into mixed solution obtained in step S1, be kept stirring and maintain reaction system
The constant 50-80min at 55~70 DEG C of temperature;
S3, by above-mentioned steps S2 treated solution is placed in high-pressure homogeneous middle processing, obtain the benefit of the nano-encapsulated after dry
Brittle Falsepimpernel Herb alkali liposome.
4. the preparation method of nano-encapsulated leonurine liposome according to claim 3, it is characterised in that: the step
High pressure in S3 is 3~5MPa.
5. a kind of face cream containing nano-encapsulated leonurine liposome as claimed in claim 1 or 2.
6. face cream according to claim 5, it is characterised in that: the face cream prepares nano-encapsulated leonurine in raw material
The weight accounting of liposome is (1~10) %.
7. face cream according to claim 6, it is characterised in that: the raw material for preparing of the face cream further includes following parts by weight
Component:
Hyaluronic acid: (0.03-0.07) wt%;
Glycerol: (4-6) wt%;
Cyclic dimethylsiloxane: (1-3) wt%;
Dimethicone: (1-4) wt%;
Tocopherol: (2-4) wt%;
Saualane: (1-3) wt%;
GTCC:(1-3) wt%;
Shea butter: (1-2) wt%;
Emulsifing thickener 305:(1-4) wt%;
A631:(0.1-1) wt%;
Deionized water: surplus.
8. a kind of anti-inflammatory anti-acne of nano-encapsulated leonurine liposome as claimed in claim 1 or 2 is in the preparation of face cream
Using, characterized by the following steps:
(1) A phase is prepared: high-speed stirred is extremely dispersed after deionized water, glycerol, hyaluronic acid are mixed, be warming up under stirring (85~
95) A phase materials at the uniform velocity DEG C, are made after stirring insulated sterilizing;
(2) B phase is prepared: cyclic dimethylsiloxane, dimethicone, tocopherol, saualane, GTCC and shea butter are mixed
After be heated to (80~90) DEG C, after dissolution be added into A phase materials be made B phase materials;
(3) B phase materials obtained are cooled to after (55~65) DEG C under stiring, emulsifing thickener 305 are added, and carry out homogeneous
Operation obtains finely dispersed mixture;
(4) continue stirring and be cooled to 45 DEG C, and A631 and nano-encapsulated leonurine liposome are added to above-mentioned steps (3) system
In the mixture obtained, and continue stirring to being uniformly dispersed, stops stirring, obtain after cooling containing nano-encapsulated leonurine rouge
The face cream of plastid.
9. application according to claim 8, it is characterised in that: in the step (1), the mixing speed is 500-
800r/min。
10. application according to claim 8, it is characterised in that: in the step (3), homogeneous revolving speed is 3000-5000r/
Min, the homogenizing time are 20-60 minutes.
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