CN113425620A

CN113425620A - Liposome for wrapping active component, preparation method and application thereof

Info

Publication number: CN113425620A
Application number: CN202110672959.XA
Authority: CN
Inventors: 陈晗俊; 庄洁; 安冬; 唐毓萍; 孙晓梅; 赵毅; 龚颖; 吴瑶瑶; 瞿怡宁; 吴旭; 段国兰
Original assignee: Bloomage Biotech Co Ltd
Current assignee: Bloomage Biotech Co Ltd
Priority date: 2021-06-17
Filing date: 2021-06-17
Publication date: 2021-09-24
Anticipated expiration: 2041-06-17
Also published as: CN113425620B

Abstract

The invention discloses a liposome for wrapping active ingredients, a preparation method and application thereof. The liposome comprises an alcohol phase, water and an active ingredient, wherein the alcohol phase comprises hydrogenated lecithin, sodium surfactin and a polyol. The active ingredients are added in the preparation process, so that the active ingredients can be stably and efficiently wrapped, the obtained liposome has better stability, the active substances can be kept more stable at high temperature, and better skin permeability is realized. And in addition, water is added in the preparation process, so that the obtained liposome has good dispersibility in an aqueous solution, reduced viscosity and increased fluidity, can be quickly dissolved in water, improves the convenience of the liposome in use, and is easy to add into various dosage forms.

Description

Liposome for wrapping active component, preparation method and application thereof

Technical Field

The invention relates to the technical field of medicines, in particular to a liposome for wrapping active ingredients, a preparation method and application thereof.

Background

"anti-aging" is a permanent goal pursued by people and is also a research hotspot of scientific researchers. Retinoids, which have been proven to be one of the effective anti-aging actives by many human tests, are increasingly used in cosmetics. However, retinoids are very unstable compounds, which are gradually decomposed and inactivated by high temperature and light.

In the prior art, the stability and the transdermal property of unstable active ingredients are improved by coating active substances such as retinol and the like which lack stability through liposome. The Liposome (Liposome) is a medicament delivery dosage form, is a spheroidal, is an artificial synthetic membrane taking phospholipid as a wall material, is an ultramicro spherical particle with a bilayer structure formed by self-aggregation in water, is very close to a plasma membrane structure of human cells, and has good physiological compatibility with a human body, so that the Liposome is used as a medicament carrying system and has the advantages of low toxicity, targeted medicament delivery, long-acting and slow-release of medicaments, improved stability and the like.

Traditional liposome membrane structures are composed primarily of phospholipids and cholesterol. Phospholipid is used as the base of a liposome membrane structure and has amphipathy, the hydrophilic head part is gathered to one side, the hydrophobic tail part is gathered to the other side, and a stable closed vesicle structure with a bilayer is formed. Cholesterol plays a stabilizing role in the structure of liposomes. Novel flexible liposomes have been studied extensively in recent years. The flexible liposome is a deformable vesicle carrier with wide application, consists of lipid with good biocompatibility and surfactant, and is used for wrapping various micromolecule and macromolecule medicines with different functions at the beginning of research and development, so that the transdermal and skin retention rates of the micromolecule and macromolecule medicines are improved, and the local curative effect and the administration compliance of the micromolecule and macromolecule medicines are improved.

In recent years, the demand of consumers for the efficacy of cosmetics is increasing, and the soft body can also wrap and deliver a plurality of active substances which are difficult to be applied to the conventional dosage form in the cosmetics, and has obvious advantages compared with the conventional dosage form in the penetration effect of the active substances: the rigidity of the phospholipid membrane in the flexible liposome is reduced and the fluidity and deformability of the membrane are increased compared to the conventional liposome, and thus, the flexible liposome has high permeability, hydrophilicity and high flexibility.

Disclosure of Invention

The liposome can stably and efficiently wrap active ingredients, has better stability, can keep the active ingredients more stable at high temperature, has better skin permeability, and is added with water in the process of preparing the liposome, so that the obtained liposome has good dispersibility in aqueous solution, reduced viscosity and increased fluidity, can be quickly dissolved in water, improves the convenience of the liposome in use, and is easy to add into various dosage forms.

The specific technical scheme of the invention is as follows:

1. a liposome encapsulating an active ingredient, the liposome comprising an alcohol phase, water and the active ingredient, the alcohol phase comprising hydrogenated lecithin, sodium surfactin and a polyol.

2. The liposome according to item 1, wherein the hydrogenated lecithin is 1 to 10%, preferably 2 to 8%, and more preferably 2 to 5% by mass of the liposome;

the content of the sodium surfactin is 0.01-0.5%, preferably 0.2-0.5%;

the polyol is 40-80%;

the water accounts for 5-20%; and

the active ingredient is 0.1-10%.

3. The liposome according to item 1 or 2, wherein the mass ratio of the hydrogenated lecithin to the sodium surfactin is 1:0.01-0.25, preferably 1: 0.05-0.2.

4. The liposome according to any one of claims 1 to 3, wherein the polyhydric alcohol is one or more selected from glycerol, butylene glycol and propylene glycol.

5. The liposome according to any one of claims 1 to 4, wherein the active ingredient is an oil-soluble active ingredient, preferably the active ingredient is a vitamin, a vitamin derivative, idebenone, coenzyme Q10, ceramide or an analogue thereof.

6. The liposome according to any one of items 1 to 5, wherein the liposome further comprises an oil phase, preferably, the oil phase is 10 to 30% by mass of the liposome.

7. The liposome of claim 6, wherein the oil phase is selected from caprylic capric triglyceride, squalane, microalgal oil or silicone oil.

8. A method for preparing liposomes encapsulating an active ingredient comprising the steps of:

mixing hydrogenated lecithin, sodium surfactin and polyhydric alcohol to obtain an alcohol phase;

mixing the oil phase and the active ingredient, adding into the alcohol phase, mixing, and adding water for homogenizing to obtain liposome.

9. The method according to item 8, wherein the hydrogenated lecithin is 1 to 10%, preferably 2 to 8%, and more preferably 2 to 5% by mass of the liposome;

the content of the sodium surfactin is 0.01-0.5%, preferably 0.2-0.5%;

the polyol is 40-80%;

the water accounts for 5-20%;

the active ingredient is 0.1-10%; and

the oil phase is 10-30%.

10. The method according to item 8 or 9, wherein the mass ratio of the hydrogenated lecithin to the sodium surfactin is 1:0.01 to 0.25, preferably 1:0.05 to 0.2.

11. The method of any of claims 8-10, wherein the polyol is selected from one or more of glycerol, butylene glycol, and propylene glycol.

12. The method according to any one of claims 8 to 11, wherein the active ingredient is an oil-soluble active ingredient, preferably the active ingredient is a vitamin, a vitamin derivative, idebenone, coenzyme Q10, ceramide or an analogue thereof.

13. The method of any of claims 8-12, wherein the oil phase is selected from caprylic capric triglyceride, squalane, microalgal oil, or silicone oil.

14. A cosmetic composition comprising the liposome of any one of claims 1-7 or the liposome prepared by the method of any one of claims 8-13.

15. The cosmetic composition according to item 14, wherein the liposome is 0.1 to 10% by mass in the cosmetic composition.

16. Use of a liposome according to any of claims 1 to 7 or prepared by the method according to any of claims 8 to 13 in the cosmetic field.

ADVANTAGEOUS EFFECTS OF INVENTION

The liposome provided by the invention is added with active ingredients in the preparation process, so that the active ingredients can be stably and efficiently wrapped, the obtained liposome has better stability, active substances can be kept more stable at high temperature, and better skin permeability is achieved.

The liposome is added with water in the preparation process, so that the liposome has good dispersibility in aqueous solution, reduced viscosity and increased fluidity, can be quickly dissolved in water, improves the convenience of the liposome in use, and is easy to add into various dosage forms.

The liposome diluent has good transmittance and smaller particle diameter ratio, and can be used for manufacturing products with transparent appearances.

Drawings

Figure 1 is a schematic of the total amount of liposomes and vitamin oil solution into the skin as described in example 3.

Figure 2 is a schematic of the depth of penetration of the liposomes and vitamin oil solution described in example 3 into the skin.

Detailed Description

The present invention is described in detail in the following description of embodiments with reference to the figures, in which like numbers represent like features throughout the figures. While specific embodiments of the invention are shown in the drawings, it should be understood that the invention may be embodied in various forms and should not be construed as limited to the embodiments set forth herein. Rather, these embodiments are provided so that this disclosure will be thorough and complete, and will fully convey the scope of the invention to those skilled in the art.

It should be noted that certain terms are used throughout the description and claims to refer to particular components. As one skilled in the art will appreciate, various names may be used to refer to a component. This specification and claims do not intend to distinguish between components that differ in name but not function. In the following description and in the claims, the terms "include" and "comprise" are used in an open-ended fashion, and thus should be interpreted to mean "include, but not limited to. The description which follows is a preferred embodiment of the invention, however, the description is given for the purpose of illustrating the general principles of the invention and not for the purpose of limiting the scope of the invention. The scope of the present invention is defined by the appended claims.

The invention provides a liposome for encapsulating an active ingredient, which comprises an alcohol phase, water and the active ingredient, wherein the alcohol phase comprises hydrogenated lecithin, sodium surfactin and polyalcohol.

The liposome generally refers to a liposome (hollow) made of phospholipid and cholesterol. Phospholipid is used as the base of a liposome membrane structure and has amphipathy, the hydrophilic head part is gathered to one side, the hydrophobic tail part is gathered to the other side, and a stable closed vesicle structure with a bilayer is formed.

The hydrogenated lecithin refers to a stable emulsifier and humectant formed by the hydrogenation of lecithin under the action of a catalyst, has strong hydrophilicity and moisture retention property, has strong affinity to skin and mucous membrane, and can play roles of moisture retention, emulsification, dispersion, oxidation resistance and the like when used in a formula of cosmetics.

The sodium surfactin is fermented by utilizing a bacillus subtilis high-yield strain, has biodegradability, good biocompatibility, ultralow irritation and stable physical and chemical properties, and is identified by toxicology and hygiene. The sodium surfactin is not only a surfactant and a biological emulsifier with excellent performance, but also has strong antibacterial and bacteriolytic effects and the effect of inhibiting blood cellulose coagulation, and mainly acts as a gel, a surfactant, an antibacterial agent and the like in cosmetics and skin care products.

In one embodiment, the hydrogenated lecithin is 1-10%, preferably 2-8%, and more preferably 2-5% by mass of the liposome;

the content of the sodium surfactin is 0.01-0.5%, preferably 0.2-0.5%;

the polyol is 40-80%, preferably 50-70%;

the water is 5-20%, preferably 10-15%; and

the active ingredient is 0.1-10%.

For example, the hydrogenated lecithin may be 1%, 2%, 3%, 4%, 5%, 6%, 7%, 8%, 9%, 10%, etc. in mass percentage in the liposome;

the sodium surfactin can be 0.01%, 0.1%, 0.2%, 0.3%, 0.4%, 0.5%;

the polyols may be 40%, 45%, 50%, 55%, 60%, 65%, 70%, 75%, 80%, etc.;

the water may be 5%, 10%, 15%, 20%, etc.;

the active ingredient may be 0.1%, 0.5%, 1%, 2%, 3%, 4%, 5%, 6%, 7%, 8%, 9%, 10%, etc.

In one embodiment, the mass ratio of the hydrogenated lecithin to the sodium surfactin is 1:0.01 to 0.25, preferably 1:0.05 to 0.2.

For example, the mass ratio of the hydrogenated lecithin to the sodium surfactin can be 1:0.01, 1:0.02, 1:0.03, 1:0.04, 1:0.05, 1:0.06, 1:0.07, 1:0.08, 1:0.09, 1:0.1, 1:0.15, 1:0.2, 1:0.25, and the like.

In one embodiment, the polyol is selected from one or more of glycerol, propylene glycol and butylene glycol.

In one embodiment, the active ingredient is an oil soluble active ingredient, preferably the active ingredient is a vitamin, a vitamin derivative, idebenone, coenzyme Q10, ceramide or an analogue thereof.

In one embodiment, the ceramide may be, for example, ceramide 1, ceramide 2, ceramide 3, ceramide 4, ceramide 6, or ceramide 9.

In one embodiment, the vitamin is selected from one or more of vitamin a, vitamin C and vitamin E.

In one embodiment, the Vitamin derivative is Vitamin A Palmitate (VA-pal).

In one embodiment, the liposome further comprises an oil phase, preferably, the oil phase is 10-30% by mass of the liposome.

For example, the oil phase may be 10%, 15%, 20%, 25%, 30%, etc.

The oil phase serves to dissolve the active ingredient so that the active ingredient is sufficiently dissolved, and in addition, the oil phase can improve the skin feel of the liposome and can improve the stability of the liposome.

In one embodiment, the oil phase is selected from caprylic capric triglyceride, squalane, microalgal oil or silicone oil.

The liposome provided by the invention can realize stable and efficient wrapping of active ingredients, the liposome has better stability, can keep the active ingredients more stable at high temperature, has better skin permeability, and the liposome diluent has high transmittance and smaller particle size, and can be used for manufacturing transparent products.

The invention provides a method for preparing liposome encapsulating active ingredients, which comprises the following steps:

The active ingredients are wrapped in the liposome in the preparation process, so that the active ingredients can be stably and efficiently wrapped, the obtained liposome has better stability, and water is added in the preparation process, so that the liposome has good dispersibility in an aqueous solution, reduced viscosity and increased fluidity, can be quickly dissolved in water, improves the convenience of the liposome in use, and is easy to add into various dosage forms.

And because the oil phase is added in the preparation process, the active ingredients can be fully dissolved, the skin feeling of the liposome can be improved, and the stability of the liposome can be improved.

For example, when the active ingredient is vitamin, the vitamin can play a role in synergistically clearing DPPH free radicals, and the vitamin can be stabilized, permeated into skin and promoted to keep and utilize the activity of the vitamin.

the content of the sodium surfactin is 0.01-0.5%, preferably 0.2-0.5%;

the polyol is 50-70%;

the water accounts for 5-20%;

the active ingredient is 0.1-10%; and

the oil phase is 10-30%.

In one embodiment, the active ingredient is an oil soluble active ingredient, preferably the active ingredient is a vitamin, a vitamin derivative, idebenone, coenzyme Q10 or a ceramide.

In one embodiment, the oil phase is selected from squalane, caprylic capric triglyceride, microalgal oil or silicone oil.

In one embodiment, homogenization is carried out at a temperature of 70-85 ℃, preferably for a time of 10-15 minutes.

In one embodiment, after homogenization, high pressure homogenization is again performed before obtaining liposomes at a temperature of 70-85 ℃ and a pressure of 800-1000bar for 3-5 cycles.

The liposome has faster solubility, improves the convenience of the liposome in use, and is easy to add into various dosage forms.

The liposome of the invention is directly prepared in the preparation process, so that the active ingredients in the prepared liposome are relatively stable, and the total amount of the active ingredients entering the skin is more and deeper.

The invention provides a cosmetic composition, which comprises the liposome or the liposome prepared by the method.

In one embodiment, the cosmetic composition further comprises an adjuvant, which is well known in the art, for example, the adjuvant may be disodium EDTA, hexylene glycol, and the like.

In one embodiment, the liposome is 0.1-10% by mass in the cosmetic composition.

For example, the liposome may be 0.1%, 0.5%, 1%, 2%, 3%, 4%, 5%, 6%, 7%, 8%, 9%, 10%, etc. in mass percentage in the cosmetic composition.

The invention provides the application of the liposome or the liposome prepared by the method in cosmetics.

Examples

The invention is described generally and/or specifically for the materials used in the tests and the test methods, in the following examples,% means wt%, i.e. percent by weight, unless otherwise specified. The reagents or instruments used are not indicated by manufacturers, and are all conventional reagent products commercially available, wherein hydrogenated lecithin is obtained from Nippon Kogyo, and surfactin sodium is obtained from Huaxi Biotech Co., Ltd.

EXAMPLE 1 preparation of liposomes

(1) Uniformly mixing 1% of hydrogenated lecithin, 0.2% of sodium surfactin and 61.8% of glycerol to obtain an alcohol phase;

(2) adding 20% of squalane and 2% of vitamin A palmitate into the alcohol phase, mixing, adding 15% of deionized water, and homogenizing at 75 ℃ to obtain a homogeneous mixture;

(3) homogenizing the homogenized mixture under high pressure at 75 deg.C under 800bar for 3 times to obtain liposome coated with vitamin.

EXAMPLE 2 preparation of liposomes

2% of hydrogenated lecithin, 0.2% of sodium surfactin and 60.8% of glycerin are mixed uniformly to obtain an alcohol phase, and the liposome coated with vitamins is obtained by the same preparation method as that of example 1.

EXAMPLE 3 preparation of liposomes

3% of hydrogenated lecithin, 0.2% of sodium surfactin and 59.8% of glycerin were mixed uniformly to obtain an alcohol phase, and liposomes encapsulating vitamins were obtained in the same manner as in example 1 except for the preparation method.

EXAMPLE 4 preparation of liposomes

2% of hydrogenated lecithin, 0.05% of sodium surfactin and 60.95% of glycerin are mixed uniformly to obtain an alcohol phase, and the liposome coated with vitamins is obtained by the same preparation method as that of example 1.

EXAMPLE 5 preparation of liposomes

2% of hydrogenated lecithin, 0.1% of sodium surfactin and 60.9% of glycerin are mixed uniformly to obtain an alcohol phase, and the liposome coated with vitamins is obtained by the same preparation method as that of example 1.

EXAMPLE 6 preparation of liposomes

2% of hydrogenated lecithin, 0.3% of sodium surfactin and 60.7% of glycerin are mixed uniformly to obtain an alcohol phase, and the liposome coated with vitamins is obtained by the same preparation method as that of example 1.

EXAMPLE 7 preparation of liposomes

2.5% of hydrogenated lecithin, 0.5% of sodium surfactin and 60% of glycerin were mixed uniformly to obtain an alcohol phase, and liposomes encapsulating vitamins were obtained in the same manner as in example 1 except for the preparation method.

EXAMPLE 8 preparation of liposomes

5% of hydrogenated lecithin, 0.25% of sodium surfactin and 57.75% of glycerin were mixed uniformly to obtain an alcohol phase, and liposomes encapsulating vitamins were obtained in the same manner as in example 1 except for the preparation method.

EXAMPLE 9 preparation of liposomes

4% of hydrogenated lecithin, 0.1% of sodium surfactin and 58.9% of glycerin are mixed uniformly to obtain an alcohol phase, and the liposome coated with vitamins is obtained by the same preparation method as that of example 1.

EXAMPLE 10 preparation of liposomes

The same procedure as in example 1 was repeated except that 8% hydrogenated lecithin, 0.1% sodium surfactin and 54.9% glycerin were mixed uniformly to obtain an alcohol phase, and a liposome containing vitamins was obtained.

EXAMPLE 11 preparation of liposomes

The same procedure as in example 1 was repeated except that 10% hydrogenated lecithin, 0.1% sodium surfactin and 52.9% glycerin were mixed uniformly to obtain an alcohol phase, and a liposome containing vitamins was obtained.

EXAMPLE 12 preparation of liposomes

The same procedure as in example 1 was repeated except that 2% hydrogenated lecithin, 0.01% sodium surfactin and 60.99% glycerin were mixed uniformly to obtain an alcohol phase, and a liposome containing vitamins was obtained.

Comparative example 1 preparation of liposomes

The dosage of the comparative example 1 and the dosage of the example 2 are the same, and the difference is that the comparative example 1 is prepared into liposome, and then the vitamin is wrapped in the liposome to obtain the liposome wrapped with the vitamin, and the specific preparation method is shown in the preparation method of the example 1 and the preparation method of the experimental example 2 of CN 111671664A.

Comparative example 2 preparation of liposomes

Comparative example 2 was used in the same amount as in example 9, except that comparative example 2 did not use water during the preparation process, and vitamin-encapsulated liposomes were obtained, and it was seen that it was not easy to prepare vitamin-encapsulated liposomes because water was not added during the preparation process.

Comparative example 3 preparation of liposomes

Comparative example 3 and example 3 were used in the same amount, except that in comparative example 3, soybean non-hydrogenated lecithin was used.

TABLE 1 amount of raw materials used in examples and comparative examples

Experimental example 1 stability test

The vitamin-encapsulated liposomes prepared in examples 1 to 12 and comparative examples 1, 2 and 3 were measured for particle size, Zeta potential, viscosity and light transmittance by an Anton Paar Liposizer 500 instrument, and the results are shown in Table 2.

TABLE 2 results of the different liposomes

As shown in Table 2, in examples 2, 4, 5, 6 and 12, the same amount of hydrogenated lecithin is used, and the particle size of the liposome is reduced and the Zeta potential is increased along with the addition of the sodium surfactin within a certain range, which indicates that the stability of the liposome is improved; meanwhile, the viscosity is gradually reduced, the fluidity is increased, the convenience of the liposome in use is improved, and the liposome can be quickly dissolved in water; while the better the transparency of the liposome dilution. It can be seen from comparison of examples 1, 2 and 3 with examples 5, 9, 10 and 11 that the stability of liposomes is improved with the increase of hydrogenated lecithin in a certain range when the amount of sodium surfactin is constant, but the stability of liposomes is not greatly affected by further increase of the amount of hydrogenated lecithin, and the viscosity of liposomes is rather increased and the absorbance is decreased.

The liposome prepared by the embodiment of the invention has better performances, namely better stability, viscosity and transmittance.

Experimental example 2 measurement of encapsulation efficiency

The vitamin-encapsulated liposomes prepared in example 2 and comparative example 1 were subjected to encapsulation efficiency measurement.

The encapsulation efficiency of the active vitamin is tested by a dialysis bag method: the pretreated dialysis bag is washed by deionized water, 5ml of liposome is quantitatively put into the dialysis bag, and the two ends of the dialysis bag are tightly sealed by a fixing clamp. Then the dialysis bag is put into 500ml of prepared release medium solution (2% Tween80+ 20% propylene glycol aqueous solution), the temperature is controlled at 37 ℃, the stirring is carried out for a certain time, samples are respectively taken at 1h, 2h, 4h, 8h and 24h, the content of the vitamin A palmitate is tested by HPLC, and the encapsulation rate is calculated. The encapsulation efficiency EN% ((1-Cf/Ct) × 100%).

Wherein Cf is the amount of free drug and Ct is the total amount of drug in the liposome suspension.

Encapsulation efficiency after 324 h in Table

	Encapsulation efficiency of 24h
		Example 2	96％
Comparative example 1	25％

As can be seen from the above table, the encapsulation efficiency was high only when the active ingredient was prepared together with the liposome, whereas the encapsulation efficiency was low in comparative example 1, in which the liposome was prepared first and then the active ingredient was put into the liposome.

Experimental example 3 measurement of dissolution Rate

Vitamin-coated liposomes obtained in examples 1 to 12 and vitamin-coated liposomes prepared in comparative examples 1, 2 and 3 were dissolved in deionized water at the same mass, and the rate of complete dissolution in water was measured, and the results are shown in Table 4.

TABLE 4 dissolution speedometer

	Dissolution time/s
		Example 1	31
Example 2	20
		Example 3	21
Example 4	107
		Example 5	30
Example 6	18
		Example 7	17
Example 8	15
		Example 9	33
Example 10	42
		Example 11	175
Example 12	153
		Comparative example 1	52
Comparative example 2	254
		Comparative example 3	23

As can be seen from the data in Table 4 above, the liposomes prepared in the examples have a faster dissolution rate in water, which improves the convenience of the liposomes in use and is easily added to various dosage forms.

Experimental example 4 physicochemical indices at different temperatures

After the samples obtained in example 3 and comparative example 3 were left at the following different temperatures for 3 months, particle size and PDI were measured using an Anton Paar particle sizer, pH was measured using a Metlor pH meter, and compared with the instant data, and the results are shown in table 5.

As can be seen from the following table, after example 3 is placed, the particle size, PDI and pH value of the sample are small, indicating that the system stability is good. In contrast, in comparative example 3, the liposome using non-hydrogenated lecithin showed a large particle size, a low pH value and a broad particle size distribution after 3 months of storage. This indicates that liposomes prepared using hydrogenated lecithin are relatively stable.

TABLE 5 physicochemical indices of liposomes described in example 3 and comparative example 3

Experimental example 5 stability of retinoid in liposome

The results of measuring the content of vitamin A palmitate by HPLC (measurement conditions: isopropyl alcohol and methanol as mobile phases, flow rate 1mL/min, DAD as a detector, detection wavelength 275nm, C18 column) after allowing the liposome-encapsulated vitamin A palmitate and the vitamin A palmitate oil solution obtained in example 3 to stand at 48 ℃ for 5 days are shown in Table 6.

Table 6 comparison of example 3 and vitamin a palmitate oil solution

	Content of VA palmitate in oil solution%	Content of coated VA palmitate%
			Initial value	2.0	2.0
After 5 days (48 degree)	1.68	2.0

As can be seen from the results shown in table 6, the stability to vitamin a palmitate was greatly improved after vitamin encapsulation.

Experimental example 6 human skin penetration test

Measurement by the residual amount measurement method: the liposome coated with Vitamin a Palmitate (VA-pal) described in example 3 is attached to or applied to a specific part of the skin according to a certain specification, the liposome is periodically taken out, the VA-pal remained on the patch is extracted by isopropanol, and the content detection is carried out by using HPLC, and the operation is continuously carried out. The skin was tested for the amount of VA-pal contained in the stratum corneum at different depths. The results of comparing the amount and depth of penetration of VA-pal into the stratum corneum of the skin are shown in FIGS. 1 and 2.

As can be seen from FIGS. 1 and 2, after wrapping VA-pal, the VA-pal enters the skin in a greater amount and more deeply than the non-wrapped VA-pal oil solution.

In conclusion, the liposome for encapsulating the active ingredient can realize stable and efficient encapsulation of the active ingredient, the obtained liposome has better stability, can keep the active substance more stable at high temperature and has better skin permeability, and in addition, water is added in the preparation process, so that the obtained liposome has good dispersibility in aqueous solution, reduced viscosity and increased fluidity, can be quickly dissolved in water, improves the convenience of the liposome in use, and is easy to add into various dosage forms.

The foregoing is directed to preferred embodiments of the present invention, other and further embodiments of the invention may be devised without departing from the basic scope thereof, and the scope thereof is determined by the claims that follow. However, any simple modification, equivalent change and modification of the above embodiments according to the technical essence of the present invention are within the protection scope of the technical solution of the present invention.

Claims

2. The liposome of claim 1, wherein the hydrogenated lecithin is present in an amount of 1-10%, preferably 2-8%, and more preferably 2-5% by mass of the liposome;

the content of the sodium surfactin is 0.01-0.5%, preferably 0.2-0.5%;

the polyol is 40-80%;

the water accounts for 5-20%; and

the active ingredient is 0.1-10%.

3. The liposome according to claim 1 or 2, wherein the mass ratio of the hydrogenated lecithin to the sodium surfactin is 1:0.01-0.25, preferably 1: 0.05-0.2.

4. The liposome according to any one of claims 1 to 3, wherein the polyhydric alcohol is selected from one or more of glycerol, butylene glycol and propylene glycol;

preferably, the active ingredient is an oil-soluble active ingredient, and preferably, the active ingredient is a vitamin, a vitamin derivative, idebenone, coenzyme Q10, ceramide, or an analog thereof.

5. The liposome according to any of claims 1 to 4, wherein the liposome further comprises an oil phase, preferably, the oil phase is 10-30% by mass of the liposome;

preferably, the oil phase is selected from caprylic capric triglyceride, squalane, microalgal oil or silicone oil.

6. A method for preparing liposomes encapsulating an active ingredient comprising the steps of:

7. The method according to claim 6, wherein the hydrogenated lecithin is present in an amount of 1-10%, preferably 2-8%, and more preferably 2-5% by mass of the liposome;

the content of the sodium surfactin is 0.01-0.5%, preferably 0.2-0.5%;

the polyol is 40-80%;

the water accounts for 5-20%;

the active ingredient is 0.1-10%; and

the oil phase is 10-30%,

preferably, the mass ratio of the hydrogenated lecithin to the sodium surfactin is 1:0.01-0.25, and more preferably 1: 0.05-0.2.

8. The method according to claim 6 or 7, wherein the polyhydric alcohol is selected from one or more of glycerin, butylene glycol, and propylene glycol;

preferably, the active ingredient is an oil-soluble active ingredient, preferably, the active ingredient is a vitamin, a vitamin derivative, idebenone, coenzyme Q10, ceramide or an analogue thereof;

9. A cosmetic composition comprising a liposome according to any one of claims 1 to 5 or prepared by a method according to any one of claims 6 to 8;

preferably, the liposome accounts for 0.1-10% of the cosmetic composition by mass percentage.

10. Use of a liposome according to any of claims 1 to 5 or prepared according to the method of any of claims 6 to 8 in the cosmetic field.