CN103800207A - Glycolic acid lipid particle and preparation method thereof - Google Patents

Abstract

The invention discloses a glycolic acid lipid particle and a preparation method thereof. The glycolic acid lipid particle is calculated according to the weight percentage of its raw material components: glycolic acid 2-8%; emulsifier 12-28% ; Lipid material 25-45%; the rest is deionized water. Wherein the emulsifier is selected from at least two compounds: polyethylene glycol-30-dipolyhydroxystearate, polyglycerin-2-dipolyhydroxystearate, Span, polyoxyethylene-21-stearate ester, Tween, PEG-23 laurate alcohol ether; the lipid material is selected from the following compounds: glyceryl monostearate, glyceryl monolaurate, monoglyceryl caprate. The glycolic acid lipid particle has good stability, water solubility and low irritation, the preparation method is simple and controllable, and has good repeatability, and can be applied to the preparation of cosmetics containing glycolic acid.

Description

Glycolic acid lipid particle and preparation method thereof

technical field

The invention belongs to the technical field of carrier systems in cosmetic preparation technology, and relates to a lipid particle with glycolic acid as an active ingredient and a preparation method thereof.

Background technique

Glycolic acid, also known as glycolic acid, is an α-hydroxy acid mainly extracted from sugarcane. Glycolic acid is the fruit acid with the smallest molecular weight. It has excellent affinity to the skin and can penetrate deep into the skin to achieve a significant moisturizing effect.

Glycolic acid can accelerate the exfoliation of aging keratinocytes, remove accumulated keratin, increase the speed of epithelial cell metabolism, promote skin renewal, improve hyperkeratosis, roughness, dark spots, and post-inflammatory pigmentation or abnormalities, making the skin smooth and bright . At the same time, glycolic acid can make the keratinized plugs around the pores easy to fall off, and unblock the hair follicles, effectively preventing the clogging of pores, thereby improving symptoms such as acne and enlarged pores.

In terms of improving aging skin, glycolic acid can stimulate the hyperplasia and rearrangement of hyaluronic acid, acid mucus polysaccharide, collagen and elastic fibers in the dermis, making the skin firm and elastic, and significantly reducing fine lines and wrinkles. At the same time, the increase of hyaluronic acid can improve the skin's own water retention capacity, which can solve the problem of dry skin.

Therefore, currently on the market, glycolic acid is often used in skin care and skin rejuvenation products to moisturize, moisturize the skin, promote epidermal renewal, and effectively solve skin aging, wrinkles, dark spots, acne and other problems in a short period of time. However, due to its small molecular weight, glycolic acid is more likely to directly penetrate into the deeper layers of the skin, even into the dermis, and then directly affect the metabolism of the basal layer cells, so it often produces tingling and burning sensations when used. And the higher the amount of glycolic acid added, the greater the corresponding irritation and the more serious the degree of concurrent inflammation.

At present, researchers at home and abroad have adopted carrier technology to develop carrier delivery systems such as W/O/W multiple emulsions, liposomes, and microcapsules for water-soluble active ingredients. W/O/W multiple emulsions embed the active ingredients in the inner phase, which has the advantages of improving the stability of the active ingredients, slow release, targeting, etc. It is a thermodynamically unstable system. Combined with solid lipid nanoparticle technology, solid lipid embedding active ingredients is adopted, and solid lipid is used to replace liquid lipid in traditional W/O/W multiple emulsions, which can effectively lock the internal phase, prevent the external phase from penetrating and avoid Austrian ripening improves system stability to a certain extent, so the present invention comes from it. Utilizing the present invention is beneficial to avoid direct contact of a large amount of free glycolic acid with the skin to reduce its irritation, and at the same time, due to the slow-release and controlled-release properties of the carrier, it is beneficial to control the release of glycolic acid and its concentration on the skin surface to ensure the full play of glycolic acid. effect.

Contents of the invention

The purpose of the present invention is to provide a glycolic acid lipid particle with high stability, good water solubility and low irritation, so as to solve the problems of high irritation of glycolic acid in the prior art. Moreover, the prepared glycolic acid lipid particles can be conveniently added to cosmetics.

In order to solve these problems in the prior art, the technical solution provided by the invention is:

A kind of glycolic acid lipid particle, its loading active component is glycolic acid, it is characterized in that described lipid particle calculates according to the mass percent of its raw material component:

The preferred technical scheme is: the glycolic acid lipid microparticle component is calculated by its weight percentage as:

The preferred technical scheme is: the glycolic acid lipid microparticle component is calculated by its weight percentage as:

The preferred technical scheme is: the glycolic acid lipid microparticle component is calculated by its weight percentage as:

The preferred technical solution is: the first emulsifier is selected from one of polyethylene glycol-30-dipolyhydroxystearate, polyglycerin-2-dipolyhydroxystearate, Span 80 or Any combination of two or more.

The preferred technical solution is: the second emulsifier is selected from one or any combination of two or more of polyoxyethylene (21) stearyl ether, Tween 80, and polyoxyethylene (23) lauryl ether.

The preferred technical solution is: the lipid material is selected from one of glyceryl monostearate, glyceryl monolaurate and glyceryl monocaprate, or any combination of two or more.

The preferred technical solution is: the particle size range of the glycolic acid lipid particle is 300-500nm.

Another object of the present invention is to provide a method for preparing the glycolic acid lipid particle, characterized in that the method comprises the following steps:

(1) Weigh the first emulsifier and lipid material according to the formula ratio, heat and mix the first emulsifier and lipid material to obtain a liquid oil phase.

(2) Weigh glycolic acid and deionized water according to the proportion of the formula, and mix them evenly to obtain the water phase.

(3) Add the water phase to the oil phase at the preset temperature, stir for 5-10 minutes, and control the stirring speed at 200-500r/min to obtain a clear and transparent W/O emulsion, and then cool the W/O emulsion to room temperature;

(4) Weigh the second emulsifier according to the formula ratio, add the second emulsifier into the W/O emulsion obtained in step (3) at the preset temperature, stir for 10-30 minutes, and control the speed at 300-800r/min, The glycolic acid lipid particle can be obtained after cooling to room temperature.

The preferred technical solution is: the preset temperature in the method is 60-75°C.

Another object of the present invention is to provide an application of the glycolic acid lipid particles in the preparation of skin care cosmetics.

The glycolic acid lipid particles obtained in the present invention can be well dispersed in water. The principle of the present invention is to combine multiple emulsions and solid lipid nanoparticles preparation technology, apply these two technologies to the embedding of water-soluble active ingredients, effectively solve the problem of traditional multiple emulsion thermodynamic instability and the difficulty of embedding water-soluble active ingredients in solid lipid nanoparticles. Composition issue. The lipid particles obtained by using the two-step emulsification method to embed glycolic acid in solid lipids have good stability and can effectively reduce the irritation of glycolic acid.

The glycolic acid lipid particle structure of the present invention is similar to the traditional W/O/W multiple emulsion, the difference is that the present invention uses solid lipids instead of liquid lipids, and the internal phase is squeezed and deformed after solidification. The structure of the glycolic acid lipid particles of the present invention is the same as that of traditional solid lipid nanoparticles in that solid lipids are used for embedding. The lipid particle structure realizes the embedding of the water-soluble component glycolic acid. The glycolic acid lipid particle of the present invention has the advantages of high stability, no leakage of active components, ability to embed water-soluble components, stable internal phase particle size, and the like.

With respect to the defective of prior art, advantage of the present invention is:

1. The preparation process conditions of the present invention are controllable, and glycolic acid lipid particles with a weight percentage of 2-8% can be prepared by adjusting the stirring speed and stirring time.

2. The glycolic acid lipid particles prepared by the present invention have good stability, and can be stored at room temperature, -4°C, and 40°C for more than one year without delamination. After being diluted 10 times, they can be centrifuged under high-speed centrifugation conditions (10000r/min) for 10min without delamination. Stratification occurs.

3. The pH of the glycolic acid lipid particles prepared by the present invention is 2-3, which is within the pH range where glycolic acid exerts its best effect.

4. The present invention can effectively reduce the stimulation of glycolic acid, and can be applied in the cosmetics industry. It can be added into cosmetic preparations to give full play to the efficacy of glycolic acid, so as to achieve the effect of long-term skin care and beauty.

5. The preparation process of the present invention is simple and convenient, and has high repeatability.

Description of drawings

The present invention will be further described below in conjunction with accompanying drawing and embodiment:

Fig. 1 is the preparation method flowchart of glycolic acid lipid particle of the present invention;

Figure 2 is a schematic diagram of the structure of particles dispersed in water; where (a) is a traditional W/O/W multiple emulsion, (b) is a traditional solid lipid nanoparticle (b); (c) is the sugar obtained by the present invention Alkyd lipid particles.

Detailed ways

The above solution will be further described below in conjunction with specific embodiments. It should be understood that these examples are used to illustrate the present invention and not to limit the scope of the present invention. The implementation conditions used in the examples can be further adjusted according to the conditions of specific manufacturers, and the implementation conditions not indicated are usually the conditions in routine experiments.

The preparation of embodiment 1 glycolic acid lipid particles

The raw material formula of glycolic acid lipid particles in the present embodiment is:

The specific preparation method is as follows:

1. Weigh 28 grams of polyethylene glycol-30-dipolyhydroxystearate, 24 grams of monoglyceride caprate, and 12 grams of glyceryl monostearate, heat and mix to obtain the oil phase.

2. Weigh 8 grams of glycolic acid and 8 grams of deionized water, stir well to obtain the water phase

3. Slowly add the water phase to the oil phase, stir at 65°C for 10 min, and control the speed at 300 r/min to obtain a clear and transparent emulsion, and cool to room temperature.

4. Weigh 20 grams of polyoxyethylene (23) lauryl ether, add it to the solid system obtained in step (3), stir at 65°C for 30 minutes, and control the speed at 500 r/min. Then cool to room temperature to obtain glycolic acid lipid particles.

5. The particle size of the obtained glycolic acid lipid particles was measured by photon correlation spectroscopy (PCS) to be 320.12 nm.

Preparation of embodiment 2 glycolic acid lipid particles

The raw material formula of glycolic acid lipid particles in the present embodiment is:

The specific preparation method is as follows:

1. Weigh 20 grams of polyglycerol-2-dipolyhydroxystearate, 20 grams of glyceryl monocaprate and 10 grams of glyceryl monostearate, heat and mix to obtain an oil phase.

2. Weigh 4 grams of glycolic acid and 26 grams of deionized water, stir well to obtain the water phase

3. Slowly add the water phase to the oil phase, stir at 65°C for 10 min, and control the speed at 300 r/min to obtain a clear and transparent emulsion, and cool to room temperature.

4. Weigh 20 g of polyoxyethylene (21) stearyl ether, add it into the solid system obtained in step (3), stir at 65°C for 30 min, and control the speed at 500 r/min. Then cool to room temperature to obtain glycolic acid lipid particles.

5. The particle size of the obtained glycolic acid lipid particles was measured by photon correlation spectroscopy (PCS) to be 358.71 nm.

The preparation of embodiment 3 glycolic acid lipid particles

The raw material formula of glycolic acid lipid particles in the present embodiment is:

The specific preparation method is as follows:

1. Weigh 28 grams of Span 80, 24 grams of glyceryl monolaurate and 12 grams of glyceryl monostearate, heat and mix to obtain the oil phase.

2. Weigh 2 grams of glycolic acid and 22 grams of deionized water, stir well to obtain the water phase

3. Slowly add the water phase to the oil phase, stir at 65°C for 10 min, and control the speed at 300 r/min to obtain a clear and transparent emulsion, and cool to room temperature.

4. Weigh 12 grams of Tween 80, add it to the solid system obtained in step (3), stir at 65°C for 30 minutes, and control the speed at 500r/min. Then cool to room temperature to obtain glycolic acid lipid particles.

5. The particle size of the obtained glycolic acid lipid particles was measured by photon correlation spectroscopy (PCS) to be 482.39nm.

As shown in Figure 2, the comparison results of structural changes after traditional W/O/W multiple emulsions, traditional solid lipid nanoparticles, and glycolic acid lipid particles obtained by the present invention are dispersed in water; where (a) is glycol Acid W/O/W multiple emulsion; (b) is glycolic acid solid lipid nanoparticles; (c) is glycolic acid lipid particles.

As can be seen from Figure 2, the glycolic acid lipid particle structure of the present invention has structural differences with traditional W/O/W multiple emulsions and solid lipid nanoparticles; the glycolic acid lipid particle structure of the present invention is different from The traditional W/O/W multiple emulsion is similar, the difference is that the present invention uses solid lipid instead of liquid lipid, and the internal phase is squeezed and deformed after solidification. The structure of the glycolic acid lipid particles of the present invention is the same as that of traditional solid lipid nanoparticles in that solid lipids are used for embedding. The lipid particle structure realizes the embedding of the water-soluble component glycolic acid. Such glycolic acid lipid particle structure has the common advantages of W/O/W multiple emulsions and solid lipid nanoparticles, while abandoning the corresponding defects.

Specifically, the glycolic acid lipid particle of the present invention has a structure similar to multiple emulsions, but the difference lies in the use of solid lipids, while the multiple emulsions are liquid lipids. The present invention is essentially a new structure, based on multiple emulsions, using solid lipid nanoparticles for reference, utilizing the high melting point of solid lipids, as long as the storage temperature does not exceed the lipid melting point, the system is relatively stable; In addition, the instability of multiple emulsions also lies in the transmission between the inner and outer phases. The inner phase can be transported to the outer phase through liquid oil, resulting in leakage of active ingredients; Thin or even broken, the system is unstable; and the use of solid lipids can block this transmission, ensuring the stability of the system. It should also be noted that the solid lipid nanoparticles are prepared by directly dissolving the active ingredient in the oil, that is to say, it realizes the embedding of the fat-soluble ingredient, and glycolic acid is a water-soluble ingredient, so Solid lipid nanoparticles cannot be used for glycolic acid entrapment.

The above examples are only to illustrate the technical conception and characteristics of the present invention, and its purpose is to allow people familiar with this technology to understand the content of the present invention and implement it accordingly, and cannot limit the protection scope of the present invention. All equivalent changes or modifications made according to the spirit of the present invention shall fall within the protection scope of the present invention.

Claims (8)

1. a glycolic acid lipid particle, its load active ingredient is glycolic acid, it is characterized in that described lipid particle counts by the mass percent of its raw material component:

2. The glycolic acid lipid particle according to claim 1, characterized in that the first emulsifier is selected from polyethylene glycol-30-dipolyhydroxystearate, polyglycerol-2-dipolyhydroxy One of stearate and Span 80 or any combination of two or more. 3. The glycolic acid lipid particle according to claim 1, characterized in that the second emulsifier is selected from polyoxyethylene (21) stearyl ether, Tween 80, polyoxyethylene (23) lauryl alcohol One or any combination of two or more ethers. 4. glycolic acid lipid particle according to claim 1, it is characterized in that described lipid material is selected from a kind of in glyceryl monostearate, glyceryl monolaurate, glyceryl monocaprate or Any combination of two or more. 5. The glycolic acid lipid particle according to claim 1, characterized in that the particle diameter of the glycolic acid lipid particle is in the range of 300-500 nm. 6. A method for preparing the glycolic acid lipid particle described in any one of claims 1 to 5, characterized in that the method comprises the following steps: (1) Weigh the first emulsifier and lipid material according to the formula ratio, heat and mix the first emulsifier and lipid material to obtain a liquid oil phase. (2) Weigh glycolic acid and deionized water according to the proportion of the formula, and mix them evenly to obtain the water phase. (3) Add the water phase to the oil phase at the preset temperature, stir for 5-10 minutes, and control the stirring speed at 200-500r/min to obtain a clear and transparent W/O emulsion, and then cool the W/O emulsion to room temperature; (4) Weigh the second emulsifier according to the formula ratio, add the second emulsifier into the W/O emulsion obtained in step (3) at the preset temperature, stir for 10-30 minutes, and control the speed at 300-800r/min, The glycolic acid lipid particle can be obtained after cooling to room temperature. 7. The method according to claim 6, characterized in that the preset temperature in said method is 60-75°C. 8. An application of the glycolic acid lipid particle described in any one of claims 1 to 5 in the preparation of skin care cosmetics.

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