CN114712261A - Nano-liposome containing ceramide-like extract and preparation method and application thereof - Google Patents

Abstract

The invention discloses a nanoliposome containing a ceramide-like extract, and a preparation method and application thereof. The invention prepares the nano-liposome containing the ceramide-like extract by taking the ceramide-like extract, cholesterol, phospholipid, glycerol, polyalcohol and water as raw materials. The nano liposome is semitransparent or transparent, and the average particle size is less than 200 nm; the ceramide-like nano liposome has high stability and good water dispersibility, can be directly used as cosmetics and can be optionally matched with a cosmetic formula, so that the difficult problem that the ceramide-like nano liposome is difficult to directly apply to the cosmetics is solved; the preparation method is simple and controllable, and has good repeatability.

Description

Nanoliposome containing ceramide-like extract and its preparation method and application

technical field

The present invention relates to the technical field of carrier systems in cosmetic preparation technology, in particular to a nanoliposome containing ceramide-like extracts and a preparation method and application thereof.

Background technique

Ceramide, namely N-fatty acyl sphingosine, is a class of amide compounds formed by the condensation of sphingosine and long-chain fatty acids. Ceramide is a class of compounds rather than one compound , mainly present in the cell membrane and intercellular matrix of the stratum corneum. The structural characteristics of amides are that in addition to the amide structure, they also contain two lipophilic long-chain alkyl groups and two hydrophilic hydroxyl groups. The ceramide-like extract referred to in the present invention is the ceramide-like (mannose erythritol ester, Mels) extract of the company's previous application (Chinese Patent Application No. 201910667983.7), which is a type of glycolipid biosurfactant In addition to being a high-level biosurfactant, the study found that Mels also contains a spatial structure similar to ceramide, and both contain lipophilic two long-chain alkyl groups and hydrophilic two or more hydroxyl groups similar to ceramides. group. In addition, Mels easily penetrates into the intercellular space of the stratum corneum of the skin, forms liquid crystals, maintains skin moisture, and has the functions of moisturizing, emollient and skin barrier repair, and has some functions similar to ceramides. Most of the existing ceramides are isolated from animals and plants, and the yield is very low and the economic cost is extremely high, which is greatly restricted in application. Therefore, the ceramide-like compound in the present invention has a similar structure and efficacy to ceramide, is safe and non-toxic, and can be used as a substitute for ceramide, thereby improving the effect and reducing the cost.

Liposome is very close to the plasma membrane system of "cell", the most basic structural and functional unit of the human body, and has very good physiological compatibility with the human body. When it is used as a carrier system, the human body rejects it. The reaction is small; the membrane structure of liposome is mainly composed of phospholipids and cholesterol. Phospholipids serve as the basis of the liposome membrane structure, and cholesterol plays a stabilizing role in the liposome structure. When environmental conditions change (such as temperature, osmotic pressure, pH, etc.) etc.), can play a role in enhancing the stability of liposome structure; and ceramide-like is a new type of biologically active substances, mainly containing Mel-A (mannose-1-erythritol-2,3- Dicaproic acid-4,6-diacetate), Mel-B (Mannose-1-erythritol-2,3-dicaproic acid-6-acetate), Mel-C (Mannose- 1-erythritol-2,3-dicaproic acid-4-acetate) three or more Mels active substances, and the content of the three Mels active substances in the ceramide-like extract is more than 45%; Ceramide-like compounds have broad development prospects in the application of skin care and hair care. Cosmetics containing ceramide-like ingredients are becoming a research hotspot. There are many research reports that the use of ceramide-containing topical creams and other products can prevent the loss of skin moisture and inhibit the effect of melanin and brown spots. However, the currently generally prepared ceramide-like extracts are oily liquids, which have poor stability and water dispersibility, and are difficult to be directly applied to cosmetics.

SUMMARY OF THE INVENTION

The primary purpose of the present invention is to overcome the shortcomings and deficiencies of the prior art, and to provide a nanoliposome containing ceramide-like extracts with high stability and good water dispersibility, which can be directly used in cosmetics.

Another object of the present invention is to provide a method for preparing the above ceramide-like extract-like nanoliposomes.

Another object of the present invention is to provide the application of the above-mentioned nanoliposomes containing ceramide-like extracts.

To achieve the above object, the present invention adopts the following technical solutions:

A nanoliposome containing a ceramide-like extract is composed of the following components in mass percentage: 1-10% of the ceramide-like extract, 0.0-3.0% of cholesterol, 3-15% of phospholipids, and 25-50% of glycerol. %, polyol 5-25%, water balance; preferably composed of the following components by mass percentage: ceramide-like extract 3-8%, cholesterol 0.2-0.5%, phospholipid 10%, glycerol 30-35%, Polyol 17-18%, water balance.

The ceramide-like extract is an extract of a new type of bioactive substance containing a type of Mels prepared and extracted by our company through biological emulsion fermentation (refer to patent application CN201910667983.7), mainly containing Mel-A, Mel-B, Mel-C contains three or more Mels active substances, and the content of the three Mels active substances in the ceramide-like extract is more than 45%, which has the effect similar to ceramide.

The phospholipid is at least one of hydrogenated phospholipid, liquid lecithin, soybean lecithin, egg yolk lecithin and cephalin.

The hydrogenated phospholipid is preferably at least one of hydrogenated lecithin and hydrogenated soybean phospholipid.

The purity of the phospholipids is all greater than or equal to 70%.

The polyol is at least one of butanediol and pentanediol; preferably a compound of butanediol and pentanediol; more preferably a compound of butanediol and pentanediol at a mass ratio of 15:2 thing.

The water is preferably at least one of deionized water, purified water and water for injection.

The particle size of the nanoliposome containing the ceramide-like extract is 50-700nm, the average particle size is less than 200nm, and the uniform distribution is translucent or transparent; the preferred particle size is 60-650nm, the average particle size is 60-650nm The particle size is 179 to 197 nm.

The preparation method of the above-mentioned nanoliposome containing ceramide-like extract, comprises the following steps:

(1) heating the ceramide-like extract to 70-80 °C, then adding phospholipids, cholesterol and polyol, and stirring at 70-80 °C to prepare a uniform mixed solution A;

(2) under the temperature of 70-80 ℃, add glycerol to mixed solution A, stir to obtain uniform mixed solution B;

(3) under the temperature of 70-80 ℃, add water to mixed solution B, stir to obtain uniform mixed solution C;

(4) The mixed solution C is kept at a constant temperature of 70-75° C. and homogenized to obtain nanoliposomes containing the ceramide-like extract.

The degree of heating described in the step (1) is preferably heating to 75-80°C.

The stirring described in the step (1) is shear stirring, and the purpose of the shear stirring condition is preferably 120-240 rpm in order to obtain a uniformly mixed system.

The temperature described in step (2) is preferably 70-75°C.

The temperature described in step (3) is preferably 70-75°C.

The conditions of homogenization described in step (4) are preferably: high-pressure homogenization 3-10 times, homogenizing pressure 35-40Mpa, and the last homogenizing pressure 80Mpa; more preferably: high-pressure homogenizing 5-6 times, homogeneous The mass pressure is 35-40Mpa, and the last homogenization pressure is 80Mpa.

Application of the above-mentioned nanoliposome containing ceramide-like extract in the preparation of daily chemical products.

The daily chemical product has at least one of the following effects: moisturizing, skin care, whitening, and removing brown spots.

Compared with the prior art, the present invention has the following advantages and effects:

1. The present invention prepares the oily ceramide-like extract into nano-liposomes, which effectively solves the problem that the ceramide-like extract has poor water dispersibility and is difficult to be directly applied to cosmetics, and at the same time replaces ceramide and expands ceramide. application resources;

2. Since the liposome membrane structure can enhance the stability of the liposome structure, its ceramide-like extract is encapsulated in nano-liposomes to be protected from or less affected by changes in environmental conditions, improving the cerebral-like properties. Stability of amide extracts.

3. The process for preparing ceramide-like extract liposomes in the present invention is simple, and the nano-liposomes have high stability, good water dispersibility and good biocompatibility, and can be directly used as cosmetics, or can be arbitrarily formulated with cosmetics. Compatible with each other; the preparation method is controllable and has good repeatability.

Description of drawings

1 is a particle size distribution diagram of the ceramide-like extract-containing nanoliposomes obtained in Example 1. FIG.

2 is a particle size distribution diagram of the ceramide-like extract-containing nanoliposomes obtained in Example 2. FIG.

3 is a particle size distribution diagram of the ceramide-like extract-containing nanoliposomes obtained in Example 3. FIG.

Detailed ways

The above solution will be further described below with reference to the specific implementation and the accompanying drawings in the description. The following description is only to reflect the purpose, effect and technical characteristics of the present invention, and does not limit the protection scope of the present invention accordingly.

Example 1 Preparation of nanoliposomes containing ceramide-like extracts

1. The composition of the liposome system is shown in Table 1:

Table 1 Composition 1 of nanoliposome system containing ceramide-like extract

prescription composition Mass (g) Mass percentage (%) Ceramide-like extract 80 8.0 Hydrogenated Lecithin 100 10.0 cholesterol 3 0.3 glycerin 350 35.0 Butanediol 150 15.0 Pentylene glycol 20 2.0 purified water 297 29.7

2. Preparation method

(1) Take 80g of ceramide-like extract (prepared with reference to Example 2 of patent CN201910667983.7, the same below), heat it to a temperature of 75°C, add 100g of hydrogenated lecithin, 3g of cholesterol, 150g of butanediol, and 20g of pentanediol, and keep it at a constant temperature. 70 ~ 75 ℃ temperature and stirring, if necessary, shear stirring (150rpm) to make a homogeneous mixture;

(2) under the temperature condition of constant temperature of 70～75 ℃, add glycerin 350g to the above-mentioned mixed solution, stir evenly, and make a homogeneous mixed solution;

(3) under the temperature condition of constant temperature 70～75 ℃, add 297g of purified water to the above-mentioned mixed solution, stir evenly, and make mixed solution;

(4) The above-mentioned mixed solution is kept at a constant temperature of 70-75°C, and is circulated through a high-pressure homogenizer, and the high-pressure homogenization is circulated 6 times. Then, uniform and stable ceramide-like nanoliposomes are obtained;

The obtained ceramide-like nanoliposomes are transparent, and the particle size distribution is measured by a particle size analyzer. The results are shown in Figure 1. The measured liposome particle size of the nanoliposome preparation is 60-420nm. Within the range, the average particle size is 179.2 nm; and it is uniformly distributed.

Stability test: The ceramide-like nanoliposomes were stored in a cool and cool place at room temperature for 24 months, and the appearance and particle size of the liposomes did not change significantly.

Test of water dispersibility: The ceramide-like nanoliposomes were placed in water and stirred, and the water dispersibility was good.

Example 2 Preparation two of nanoliposomes containing ceramide-like extract

1. The composition of the liposome system is shown in Table 2:

Table 2 Composition 2 of nanoliposome system containing ceramide-like extract

prescription composition Mass (g) Mass percentage (%) Ceramide-like extract 50 5.0 Hydrogenated Lecithin 50 5.0 Soy lecithin 50 5.0 cholesterol 2 0.2 glycerin 300 30.0 Butanediol 130 13.0 Pentylene glycol 50 5.0 purified water 368 36.8

2. Preparation method

(1) Take 50 g of ceramide-like extract and heat it to a temperature of 80 °C, add 50 g of hydrogenated lecithin, 50 g of soybean lecithin, 2 g of cholesterol, 130 g of butanediol, and 50 g of pentanediol, keep the temperature at a constant temperature of 70 to 75 °C and stir, if necessary Carry out shear stirring (180rpm), make homogeneous mixed solution;

(2) under the temperature condition of constant temperature of 70～75 ℃, add glycerin 300g to the above-mentioned mixed solution, stir evenly, and make a homogeneous mixed solution;

(3) under the temperature condition of constant temperature 70～75 ℃, add 368g of purified water to the above-mentioned mixed solution, stir evenly, and make mixed solution;

(4) The above-mentioned mixed solution is kept at a constant temperature of 70-75°C, and is circulated through a high-pressure homogenizer, and the high-pressure homogenization is circulated 5 times. Then, uniform and stable ceramide-like nanoliposomes are obtained;

The obtained ceramide-containing nanoliposomes are translucent, and the particle size distribution is measured by a particle size analyzer. The results are shown in Figure 2, and the liposome particle diameter of the nanoliposome preparation is measured at 60 -650nm range, the average particle size is 196.5nm; and uniform distribution.

Stability test: The ceramide-like nanoliposomes were stored in a cool and cool place at room temperature for 24 months, and the appearance and particle size of the liposomes did not change significantly.

Test of water dispersibility: The ceramide-like nanoliposomes were placed in water and stirred, and the water dispersibility was good.

Example 3 Preparation of ceramide-like nanoliposomes

1. The composition of the liposome system is shown in Table 3:

Table 3 Compositions of the ceramide-like nanoliposome system composition three

prescription composition Mass (g) Mass percentage (%) Ceramide-like extract 30 3.0 Hydrogenated Lecithin 40 4.0 liquid lecithin 60 6.0 cholesterol 5 0.5 glycerin 350 35.0 Butanediol 140 14.0 Pentylene glycol 30 3.0 purified water 345 34.5

2. Preparation method

(1) Take 30 g of ceramide-like extract and heat it to a temperature of 80 ° C, add 40 g of hydrogenated lecithin, 60 g of liquid lecithin, 5 g of cholesterol, 140 g of butanediol, and 30 g of pentanediol, keep the temperature at a constant temperature of 70 to 75 ° C and stir, if necessary Shearing and stirring (180rpm) was carried out to make a homogeneous mixed solution;

(2) under the temperature condition of constant temperature of 70～75 ℃, add glycerin 350g to the above-mentioned mixed solution, stir evenly, and make a homogeneous mixed solution;

(3) under the temperature condition of constant temperature 70～75 ℃, add 345g of purified water to the above-mentioned mixed solution, stir evenly, and make mixed solution;

(4) The above-mentioned mixed solution is kept at a constant temperature of 70-75°C, and is circulated through a high-pressure homogenizer, and the high-pressure homogenization is circulated 6 times. Then, uniform and stable ceramide-like nanoliposomes are obtained;

The obtained ceramide-like nanoliposomes are nearly transparent, and the particle size distribution is measured by a particle size analyzer. The results are shown in Figure 3. -550nm range, the average particle size is 183.1nm; and uniform distribution.

Stability test: The ceramide-like nanoliposomes were stored in a cool and cool place at room temperature for 24 months, and the appearance and particle size of the liposomes did not change significantly.

Test of water dispersibility: The ceramide-like nanoliposomes were placed in water and stirred, and the water dispersibility was good.

The above-mentioned embodiments are preferred embodiments of the present invention, but the embodiments of the present invention are not limited by the above-mentioned embodiments, and any other changes, modifications, substitutions, combinations, The simplification should be equivalent replacement manners, which are all included in the protection scope of the present invention.

Claims (10)

1. A nanoliposome containing a ceramide-like extract is characterized by comprising the following components in percentage by mass: 1-10% of ceramide extract, 0.0-3.0% of cholesterol, 3-15% of phospholipid, 25-50% of glycerol, 5-25% of polyalcohol and the balance of water.

2. The nanoliposome containing a ceramide-like extract as claimed in claim 1, which is characterized by comprising the following components in percentage by mass: 3-8% of ceramide extract, 0.2-0.5% of cholesterol, 10% of phospholipid, 30-35% of glycerol, 17-18% of polyalcohol and the balance of water.

3. The nanoliposome containing a ceramide-like extract as claimed in claim 1 or 2, wherein:

the phospholipid is at least one of hydrogenated phospholipid, liquid lecithin, soybean phospholipid, egg yolk lecithin and cephalin;

the polyalcohol is at least one of butanediol and pentanediol.

4. The nanoliposome containing a ceramide-like extract as claimed in claim 3, wherein:

the hydrogenated phospholipid is at least one of hydrogenated lecithin and hydrogenated soybean phospholipid;

the polyalcohol is a compound of butanediol and pentanediol.

5. The nanoliposome containing a ceramide-like extract as claimed in claim 1 or 2, wherein:

the particle size of the nano-liposome containing the ceramide-like extract is 50-700nm, the average particle size is less than 200nm, and the nano-liposome is uniformly distributed.

6. The method for preparing nanoliposomes containing a ceramide-like extract as claimed in any one of claims 1 to 5, which comprises the steps of:

(1) heating ceramide-like extract to 70-80 deg.C, adding phospholipid, cholesterol and polyalcohol, and stirring at 70-80 deg.C to obtain uniform mixed solution A;

(2) adding glycerol into the mixed solution A at the temperature of 70-80 ℃, and uniformly stirring to obtain a uniform mixed solution B;

(3) adding water into the mixed solution B at the temperature of 70-80 ℃, and uniformly stirring to obtain a uniform mixed solution C;

(4) and (3) keeping the temperature of the mixed solution C at 70-75 ℃, and homogenizing to obtain the nanoliposome containing the ceramide-like extract.

7. The method of claim 6, wherein:

the heating degree in the step (1) is 75-80 ℃;

the temperature in the step (2) is 70-75 ℃;

the temperature in the step (3) is 70-75 ℃.

8. The method of claim 6, wherein:

the homogenization conditions in the step (4) are as follows: homogenizing for 3-10 times at high pressure of 35-40MPa, and homogenizing for the last time at 80 MPa.

9. Use of the nanoliposome containing a ceramide-like extract as claimed in any one of claims 1 to 5 in the preparation of daily chemical products.

10. Use according to claim 9, characterized in that: the daily chemical product has at least one of the following effects: moisturizing, caring skin, whitening, and eliminating speckle.

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