CN106309152A - Water-dispersible oil-in-oil lipid nanocapsule and preparation method thereof - Google Patents

Abstract

The invention relates to a water-dispersible oil-in-oil lipid nanocapsule containing lipoic acid and vitamin E oil and a preparation method of the water-dispersible oil-in-oil lipid nanocapsule. The preparation method includes: sequentially evenly mixing, by weight percentage, 0.1-5% of the lipoic acid, 0.1-20% of vitamin E oil, 1-10% of phospholipid, 2-20% of dipropylene glycol, 50-80% of glycerin and the like at 40-80 DEG C, and performing high-pressure homogenizing treatment to obtain the transparent or semitransparent water-dispersible oil-in-oil lipid nanocapsule containing the lipoic acid and the vitamin E oil, wherein the particle size of the water-dispersible oil-in-oil lipid nanocapsule is 250 nanometers. The water-dispersible oil-in-oil lipid nanocapsule is simple to prepare, good in water dispersity, good in bioavailability, good in repeatability, and the like.

Description

A kind of water-dispersible oil-in-oil lipid nanocapsule and preparation method thereof

technical field

The invention relates to a method for preparing water-dispersible oil-in-oil lipid nanocapsules containing lipoic acid and vitamin E oil, and belongs to the technical field of cosmetics.

Background technique

Lipoic acid is a coenzyme that exists in the mitochondria, similar to vitamins. After being absorbed by the human body, it can be quickly converted into dihydrolipoic acid in the cell, and then excreted from the cell membrane to participate in the extracellular metabolic cycle. Lipoic acid and dihydrolipoic acid can scavenge almost all oxygen free radicals in the body. Lipoic acid is widely used in cosmetics and pharmaceutical and healthcare industries due to its strong oxidizing ability. In the medical and health care industry, lipoic acid is mainly used to treat diabetes and its complications, acute coronary syndrome, protect ischemia-reperfusion injury, strengthen liver function, and improve dementia. In the field of cosmetics, people mainly use lipoic acid's strong antioxidant capacity to remove excess free radicals in the body, so as to delay aging and protect the skin.

Vitamin E is a very important fat-soluble antioxidant. It is mainly used clinically to reduce the risk of myocardial infarction and cerebral infarction. External use of vitamin E can reduce the circumference and freckles caused by photoaging, scavenge free radicals, and can also protect the human body from the damage caused by ultraviolet radiation.

Although both lipoic acid and vitamin E have good antioxidant properties, their water solubility is poor, resulting in low bioavailability of both. In addition, since lipoic acid and vitamin E have strong antioxidant capacity, they are easily oxidized by oxygen in the air when exposed to the air, and lipoic acid will have a pungent odor after oxidation, so this has also become a bottleneck in application.

Nano-carriers place active ingredients inside nanoscale carrier particles through dissolution and encapsulation, improve the solubility, bioavailability, and stability of active ingredients, increase targeting and sustained release, and improve compatibility, which is beneficial to the active ingredients. Absorb and utilize.

Contents of the invention

Technical problem: In order to solve the above problems, the invention provides a water-dispersible oil-in-oil lipid nanocapsule containing lipoic acid and vitamin E oil and a preparation method thereof, the purpose of which is to provide a high loading capacity, good water solubility, The lipid nanocapsule preparation containing lipoic acid and vitamin E oil with good stability and excellent compatibility enables it to fully exert the effects of active ingredients such as lipoic acid and vitamin E.

Technical scheme: a kind of water-dispersible oil-in-oil lipid nanocapsule containing lipoic acid and vitamin E oil of the present invention is characterized in that: the lipid nanocapsule contains the following components by weight percentage:

The percentage by weight is 0.1%-5% lipoic acid, 0.1%-20% vitamin E oil, 1%-10% phospholipid, 2%-20% dipropylene glycol, and 50%-80% glycerin.

The phospholipid used in the water-dispersible oil-in-oil lipid nanocapsule containing lipoic acid and vitamin E oil in the present invention is one or more than one mixture of soybean lecithin, egg yolk lecithin and hydrogenated phospholipids.

The phospholipid used in the water-dispersible oil-in-oil lipid nanocapsule containing lipoic acid and vitamin E oil in the present invention is preferably soybean lecithin with PC content ≥ 50.

The preparation method of the water-dispersible oil-in-oil lipid nanocapsule containing lipoic acid and vitamin E oil of the present invention is carried out according to the following steps:

Step (1): Lipoic acid and vitamin E oil are fully dissolved at a temperature of 40° C. to 80° C. and stirring conditions according to the formula ratio to obtain a mixture I.

Step (2): According to the formula ratio, phospholipids and dipropylene glycol are fully dissolved at a temperature of 40°C to 80°C and stirring conditions, and the mixed solution is added to the above mixture I, and the mixture is heated at a temperature of 40°C to 80°C and Mixing into a homogeneous solution under stirring conditions gives mixture II.

Step (3): preheating the glycerol in the proportion of the formula and adding it to the above mixture II, and mixing it into a homogeneous solution at a temperature of 40° C. to 80° C. under stirring conditions to obtain a mixture III.

Step (4): The above-mentioned mixture III is subjected to high-pressure homogenization treatment, the high-pressure homogenization pressure is 400-1000 bar, the number of cycles is 1-6 times, and a transparent or translucent water-dispersible oil containing lipoic acid and vitamin E oil is obtained after cooling. Oil-in-Oil Lipid Nanocapsules.

Another object of the present invention is to provide an application of a water-dispersible oil-in-oil lipid nanocapsule containing lipoic acid and vitamin E oil in the preparation of skin care cosmetics.

Beneficial effects: the water-dispersible oil-in-oil lipid nanocapsules containing lipoic acid and vitamin E oil of the present invention have the following advantages: the appearance of the product is translucent or transparent, it has good water solubility, the product quality is stable, and the preparation method is simple. Good repeatability and convenient large-scale production. Because the particle size of the lipid nanocapsule is small, the closing effect on the skin is strengthened, and the moisturizing effect of cosmetics is increased. And the formula contains phospholipid, which is similar to skin lipid structure, so lipoic acid and vitamin E are easy to penetrate into the deep layer of the skin, giving full play to the effects of lipoic acid, vitamin E and other ingredients, and these advantages make the effectiveness of active ingredients on the skin significantly increased.

Description of drawings

Fig. 1 is a schematic diagram of the process steps of the present invention.

detailed description

The present invention will be further described below in conjunction with embodiment. These examples illustrate the present invention and do not limit the scope of the present invention. The implementation conditions adopted 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 tests.

Example 1: Lipoic acid and vitamin E oil-water dispersible oil-in-oil lipid nanocapsule preparation method

As shown in Figure 1, the preparation steps of this embodiment are as follows:

1. Weigh 0.42g of lipoic acid and 10g of vitamin E oil, put them into a 250ml beaker, put them in a 60°C water bath and stir at 300r/min until completely mixed to obtain mixture I.

2. Weigh 5g of phospholipid (PC50), 10g of dipropylene glycol to fully dissolve the phospholipid under 80°C temperature and stirring conditions, and add this mixture to the above mixture I, stir the mixture II in a 60°C water bath at 300r/min for 5min .

3. Weigh 74.58g of glycerin and preheat it to 60°C, add it to the above mixture II, stir in a 60°C water bath at 300r/min for 5min, and mix to form a homogeneous solution to obtain mixture III.

4. The above-mentioned mixture III is subjected to high-pressure homogenization treatment, the high-pressure homogenization pressure is 600 bar, and the number of cycles is 2 times.

5. Obtain transparent lipoic acid and vitamin E oil-water dispersible oil-in-oil lipid nanocapsules after cooling, obtain water dispersion liquid after 200 times dilution with deionized water, and this dispersion liquid records its particle diameter by photon correlation spectroscopy (PCS) 188.53nm.

Example 2: Lipoic acid and vitamin E oil-water dispersible oil-in-oil lipid nanocapsule preparation method

As shown in Figure 1, the preparation steps of this embodiment are as follows:

1. Weigh 0.5g of lipoic acid and 10g of vitamin E oil, put them into a 250ml beaker, put them in a 60°C water bath and stir at 300r/min until completely mixed to obtain mixture I.

2. Weigh 5g of phospholipid (PC60), 10g of dipropylene glycol to fully dissolve the phospholipid under 80°C temperature and stirring conditions, and add this mixture to the above mixture I, stir the mixture II in a 60°C water bath at 300r/min for 5min .

3. Weigh 74.5g of glycerin and preheat it to 60°C, add it to the above mixture II, stir in a 60°C water bath at 300r/min for 5min, and mix to form a homogeneous solution to obtain mixture III.

4. The above-mentioned mixture III is subjected to high-pressure homogenization treatment, the high-pressure homogenization pressure is 600 bar, and the number of cycles is 2 times.

5. Obtain transparent lipoic acid and vitamin E oil-water dispersible oil-in-oil lipid nanocapsules after cooling, obtain water dispersion liquid after 200 times dilution with deionized water, and this dispersion liquid records its particle diameter by photon correlation spectroscopy (PCS) 192.50nm.

Example 3: Lipoic acid and vitamin E oil-water dispersible oil-in-oil lipid nanocapsule preparation method

As shown in Figure 1, the preparation steps of this embodiment are as follows:

1. Weigh 0.25g of lipoic acid and 5g of vitamin E oil, put them into a 250ml beaker, place them in a 60°C water bath and stir at 300r/min until completely mixed to obtain mixture I.

2. Weigh 4.2g of phospholipid (PC60), 8.4g of dipropylene glycol to fully dissolve the phospholipid under 80°C temperature and stirring conditions, and add this mixture to the above mixture I, stir in a 60°C water bath at 300r/min for 5min Mixture II.

3. Weigh 82.15g of glycerin and preheat it to 60°C, add it to the above mixture II, stir in a 60°C water bath at 300r/min for 5min, and mix to form a homogeneous solution to obtain mixture III.

4. The above-mentioned mixture III is subjected to high-pressure homogenization treatment, the high-pressure homogenization pressure is 600 bar, and the number of cycles is 2 times.

5. Obtain transparent lipoic acid and vitamin E oil-water dispersible oil-in-oil lipid nanocapsules after cooling, obtain water dispersion liquid after 200 times dilution with deionized water, and this dispersion liquid records its particle diameter by photon correlation spectroscopy (PCS) 207.6nm.

Example 4: Lipoic acid and vitamin E oil-water dispersible oil-in-oil lipid nanocapsule preparation method

As shown in Figure 1, the preparation steps of this embodiment are as follows:

1. Weigh 0.6g of lipoic acid and 13g of vitamin E oil, put them into a 250ml beaker, put them in a 60°C water bath and stir at 300r/min until completely mixed to obtain mixture I.

2. Weigh 5g of phospholipid (PC60), 10g of dipropylene glycol to fully dissolve the phospholipid under 80°C temperature and stirring conditions, and add this mixture to the above mixture I, stir the mixture II in a 60°C water bath at 300r/min for 5min .

3. Weigh 71.4g of glycerin and preheat it to 60°C, add it to the above mixture (II), stir in a 60°C water bath at 300r/min for 5min and mix to form a homogeneous solution to obtain mixture (III).

4. The above-mentioned mixture (III) is homogenized under high pressure, the pressure of the high pressure homogenization is 600 bar, and the number of cycles is 2 times.

5. Obtain transparent lipoic acid and vitamin E oil-water dispersible oil-in-oil lipid nanocapsules after cooling, obtain water dispersion liquid after 200 times dilution with deionized water, and this dispersion liquid records its particle diameter by photon correlation spectroscopy (PCS) 190.8nm.

The above examples are only preferred implementations of the present invention, but the implementation of the present invention is not limited by the above examples, and any other changes, modifications, combinations, Simplification and replacement should be equivalent replacement methods, and all are included in the protection scope of the present invention. The present invention uses water-dispersible oil-in-oil lipid nanocapsules to wrap lipoic acid and vitamin E oil, which can well improve and solve the above-mentioned application bottleneck, and can also increase moisturizing effect, improve skin feel, and the like. The present invention comes from this.

Claims (5)

1. a water dispersible oil bag oils and fats matter nanocapsule, it is characterised in that: this lipid nanometer capsule be a kind of containing thioctic acid and The water dispersible oil bag oils and fats matter nanocapsule of vitamin E oil, including following components, percentage by weight is: 0.1%～5% sulfur is pungent Acid, 0.1%～20% vitamin E oil, 1%～10% phospholipid, 2%～20% dipropylene glycol, 50%～80% glycerol.

2. require described water dispersible oil bag oils and fats matter nanocapsule according to claim 1, it is characterised in that: described phospholipid is big The mixture of the one or more than one in bean lecithin, Ovum Gallus domesticus Flavus lecithin or hydrogenated phospholipid.

3. require described water dispersible oil bag oils and fats matter nanocapsule according to claim 1, it is characterised in that: phospholipid used is preferably The soybean lecithin of PC content >=50.

4. the preparation method of the water dispersible oil bag oils and fats matter nanocapsule as described in claim 1 requires, it is characterised in that The method sequentially includes the following steps:

Step 1: make thioctic acid fill under 40 DEG C～80 DEG C of temperature and stirring condition thioctic acid and vitamin E oil by formula proportion Dissolving is divided to obtain mixture I；

Step 2: make phospholipid abundant under 40 DEG C～80 DEG C of temperature and stirring condition by formula proportion phospholipid and dipropylene glycol Dissolve, and this mixed liquor is added in said mixture I, under 40 DEG C～80 DEG C of temperature and stirring condition, be mixed into uniform solution Obtain mixtures II；

Step 3: be added in said mixture II, under 40 DEG C～80 DEG C of temperature and stirring condition after formula proportion glycerol is preheated It is mixed into uniform solution and obtains mixtures III；

Step 4: being processed by said mixture III high pressure homogenize, high pressure homogenize pressure is 400～1000bar, and cycle-index is 1 ～6 times, obtain the transparent or translucent water dispersible oil bag oil lipid nanometer containing thioctic acid and vitamin E oil after cooling Capsule.

5. a water dispersible oil bag oils and fats matter nanocapsule as claimed in claim 1, it is characterised in that: this water dispersible oil bag Oils and fats matter nanocapsule is applied in preparing skin protection cosmetics.