KR20120018609A - Aqueous nanoemulsion composition containing mastic gum - Google Patents

Abstract

PURPOSE: An aqueous nanoemulsion composition containing mastic gum is provided to ensure bioavailability and for excellent storage and pH stability. CONSTITUTION: An aqueous nanoemulsion composition containing mastic gum contains 5-60 wt% of mastic gum, 5-50 wt% of oil, 3-30 wt% of polyglycerin fatty acid ester as an emulsifier, 0.1-15 wt% of sugar fatty acid ester, 1-40 wt% of propylene glycol, and water for the remaining amount. The mastic gum is obtained from Pistacia lentiscus. The viscosity of the composition is 1-100 Cp. The oil includes olive oil, sunflower seed oil, MCT(medium chain triglyceride), jojoba oil, or macadamia oil. The polyglycerin fatty acid ester includes polyglycerin stearic acid, polyglycerin myristic acid, polyglycerin oleic acid, or polyglycerin lauric acid.

Description

Aqueous nanoemulsion composition containing mastic gum {AQUEOUS NANOEMULSION COMPOSITION CONTAINING MASTIC GUM}

The present invention is 5 to 60% by weight mastic gum, 5 to 50% by weight oil, 3 to 30% by weight polyglycerin fatty acid ester as emulsifier, 0.1 to 15% by weight sucrose fatty acid ester as auxiliary emulsifier, 1 to 40% by weight propylene glycol And it relates to a mastic gum-containing aqueous nanoemulsion composition comprising a residual amount of water, the mastic gum-containing aqueous nanoemulsion composition of the present invention has a high bioavailability, has excellent storage stability and pH stability.

Mastic tree ( Pistacia lentiscus ) is an evergreen shrub of the family Sumacaceae. It is 2 to 3 meters tall, grows very slowly, and grows after 40 to 50 years, and produces gum from the 5 year old tree. Mastic trees live for over 100 years, but begin to age in about 70 years. Only Chia varieties, cultivated exclusively in the southern part of the Greek island of Chios, produce pure, unique and superlative mastic gum. Variants, microclimates, and climates of this plant, which are found only on the island of Chios, are crucial for mastic production. Mastic is a sap of a mastic tree that grows only on the Greek island of Chios, with no added chemicals. The harvest of the mastic takes place from July to early October, with a sharp extension that cuts the mastic tree and releases secretions to obtain sap. Mastic is like a teardrop on a wound Flows and drops fall to the ground. The mastic is crystal clear and has a bitter bite at first, but the bitter taste soon disappears, leaving a distinctive aroma.

Mastic has been widely used in medicine, food and beauty since ancient Greek times, and various researches on the efficacy of mastic have been conducted. Investigating how the natural chios mastic prevents the harmful effects (toxicity) of the bacteria surrounding the teeth, 41.5% showed that bacterial plaques were significantly higher when chewing systematically than when nothing was chewed. Has been reported to decrease (Keiso Takahashi, 2003). Studies conducted at the University of Nottingham have shown that even a small amount of mastic (1 mg per day for 2 weeks) is a Helicobacter. pylori ) has been shown to be able to cure peptic ulcer disease. Electron microscopic observations show that mastic causes structural changes in Helicobacter pylori, which may explain the anti-ulcer activity of mastic, and that mastic contains antibacterial activity against pyloric spiral bacteria. (New England Journal of Medicine, 1998). In a study on the chemical composition and antibacterial activity of mastic essential oils extracted from mastic oil, the Greek pharmacological society said, “Mastic oil has shown notable antimicrobial activity. It also showed significant antifungal activity ”(The Journal of Dermatologic Surgery and Oncology, 1992).

Functional materials used in the fields of food, beverages, cosmetics and pharmaceuticals have many natural materials. Although most functional materials show excellent efficacy / effect, they are very unstable to external environmental factors such as light, heat and oxygen. It is insoluble in water, general organic solvents and oils, so its use is limited and examples of such substances cannot be enumerated. Currently, it is used by stabilizing by emulsion or encapsulation in solution using surfactants or emulsifiers. However, when these methods are used, micelles are agglomerated or self-decompose by the diffusion of functional substances from solution. Therefore, the functional substances are not sufficiently stabilized physically and chemically, and thus there is a limitation in using them in actual industry. Thus, studies to overcome this problem have been continuously conducted in each field, but no clear solution has been proposed.

In the case of mastic gum, its efficacy is scientifically researched, and its utilization is increasing in various forms such as gum, toothpaste, spa, and cosmetics, but mastic gum is not easily dissolved in water, and thus there are many limitations in using it.

Keiso Takahashi et al., Journal of Periodontology, April 2003, Vol. 74, No. 4, pp. 501-505 New England Journal of Medicine, Vol. 339, Issue 26, Dec. 24, 1998, p. 1946 The Journal of Dermatologic Surgery and Oncology, Volume 18, Issue 11, November 1992, p. 990

Accordingly, the present invention provides a mastic gum-containing aqueous nanoemulsion composition having excellent bioavailability, storage stability, pH stability and the like while containing mastic gum as an active ingredient.

In order to achieve the above object, the present invention provides 5 to 60% by weight of mastic gum, 5 to 50% by weight of oil, 3 to 30% by weight of polyglycerin fatty acid ester as emulsifier, 0.1 to 15% by weight of sucrose fatty acid ester as auxiliary emulsifier, propylene It provides a mastic gum-containing aqueous nanoemulsion composition comprising 1 to 40% by weight of glycol and the balance of water.

The aqueous nanoemulsion composition of the present invention contains mastic gum as an active ingredient. Since mastic gum may not be easily dissolved in a solvent and may take a long time, it is more preferable to dissolve the mastic gum in a solvent and then to dissolve it in a solvent than to directly dissolve the mastic gum in a solvent. . The aqueous nanoemulsion composition of the present invention comprises mastic gum at 5 to 60% by weight, more preferably 10 to 50% by weight. When the mastic gum is included in less than 5% by weight in the present invention may be a weak biophysical effect of the mastic gum, when contained in excess of 60% by weight may be a good melted mastic gum or precipitated for a long time exposure. have.

The aqueous nanoemulsion composition of the present invention contains oil as a solvent for dissolving mastic gum. The oil in the present invention is not particularly limited as long as it can dissolve the mastic gum, but preferably olive oil, sunflower oil, medium chain triglyceride (MCT) oil, jojoba oil or macadamia nut oil may be used alone or in combination. Can be. The aqueous nanoemulsion composition of the present invention comprises 5 to 50% by weight of oil, more preferably 10 to 40% by weight, more preferably 15 to 35% by weight of oil. In the present invention, when the oil is included in less than 5% by weight it may be difficult to dissolve the mastic gum, and when included in more than 50% by weight may lower the emulsion stability.

The aqueous nanoemulsion composition of the present invention comprises a polyglycerol fatty acid ester as an emulsifier. In the present invention, the polyglycerol fatty acid ester, for example, polyglycerol stearic acid, polyglycerin myristic acid, polyglycerol oleic acid or polyglycerol lauric acid may be used alone or mixed but is not limited thereto. The aqueous nanoemulsion composition of the present invention comprises 3 to 30% by weight, more preferably 5 to 20% by weight of polyglycerin fatty acid ester. In the present invention, when the polyglycerol fatty acid ester is included in less than 3% by weight, the emulsification effect may be weak and the emulsion stability may be lowered. When the polyglycerol fatty acid is contained in an amount of more than 30% by weight, the viscosity of the aqueous composition may increase.

The aqueous nanoemulsion composition of the present invention contains sucrose fatty acid ester as an auxiliary emulsifier in order to emulsify the mastic gum more stably. In the present invention, for example, sucrose fatty acid ester, sucrose stearic acid ester, sucrose palmitate ester, sucrose myristic acid ester, sucrose oleic acid ester or sucrose lauric acid ester may be used alone or in combination, but is not limited thereto. The aqueous nanoemulsion composition of the present invention comprises sucrose fatty acid ester in an amount of 0.1 to 15% by weight, more preferably 1 to 10% by weight. In the present invention, when the sucrose fatty acid ester is included in less than 0.1% by weight, the emulsion stability may be lowered, and when included in excess of 15% by weight, there may be a problem that the viscosity of the aqueous composition is increased.

The aqueous nanoemulsion composition of the present invention comprises propylene glycol to prevent precipitation of the mastic gum and to dissolve the mastic gum with a relatively small amount of emulsifier. The aqueous nanoemulsion composition of the present invention contains 1 to 40% by weight of propylene glycol, more preferably 5 to 30% by weight. In the present invention, when the propylene glycol is included in less than 1% by weight, the storage stability of the aqueous nanoemulsion composition is reduced. If included in excess of 40% by weight, the emulsion may become unstable and separate.

The mastic gum-containing aqueous nanoemulsion composition of the present invention contains a residual amount of water, for example, 5 to 85% by weight of water in addition to the above components.

The mastic gum-containing aqueous nanoemulsion composition of the present invention preferably has a viscosity of 1 to 100 cP (centipoise).

The mastic gum-containing aqueous nanoemulsion composition of the present invention has high bioavailability, can exhibit efficacy in a small amount, and has excellent storage stability, so that it does not precipitate or float even after long-term storage at room temperature (25 ° C) or high temperature (45 ° C). Do not. In addition, the mastic gum-containing aqueous nanoemulsion composition of the present invention is very stable at a wide range of pH (pH 2 to 10), and thus can be used in various formulations. Mastic gum-containing aqueous nanoemulsion composition of the present invention can be applied to various fields, such as beverages, food, cosmetics, functional foods and pharmaceuticals, depending on the desired purpose, for this purpose, in addition to the above-mentioned ingredients, thickeners, sweeteners, excipients, fragrances Various additives, such as these, can be further included as needed.

The mastic gum-containing aqueous nanoemulsion composition of the present invention not only has excellent storage stability, pH stability and transparency, but also can efficiently absorb mastic gum, and thus has high bioavailability.

1 is a result of measuring the size of the particle diameter of the nanoemulsion of Example 1 using Photal ELS-Z.
2 is a result of measuring the size of the particle diameter of the nanoemulsion of Example 3 using Photal ELS-Z.
3 is an enlarged photograph of the nanoemulsion of the present invention using a frozen electron microscope.
Figure 4 is a photograph of the percutaneous absorption of the mastic gum (A: Negative control (phosphate buffer); B: nanoemulsion containing glycerin; C: nanoemulsion containing propylene glycol).

Hereinafter, the present invention will be described in detail by way of examples. However, the embodiments are only illustrated to help the understanding of the present invention, and the scope of the present invention is not limited thereto.

Example  One

To the composition of Table 1 was prepared an aqueous nanoemulsion composition by the following method. The mastic gum powder was crushed with a grinder and dissolved in olive oil. After addition of polyglycerol stearic acid and sucrose stearic acid ester, water and propylene glycol were added and stirred well, and then passed five times at 1,000 bar continuously in a high-pressure microemulsifier, followed by sterile filtration and packaging.

Example  2

It was prepared in the same manner as in Example 1, except that the components shown in Table 2 were used.

Example  3

Except for using the components shown in Table 3, was prepared in the same manner as in Example 1.

Example  4

It was prepared in the same manner as in Example 1, except that the components shown in Table 4 were used.

Example  5

It was prepared in the same manner as in Example 1, except that the components shown in Table 5 were used.

Experimental Example  One

After preparing the composition, the appearance was visually observed for layer separation and precipitation. Stability was stored at room temperature (25 ° C.) and 45 ° C. constant temperature bath and the change was measured.

1) Layer Separation, Precipitation, and Stability of Nanoemulsion Composition

2) The color change of the mastic gum was observed at room temperature (25 ° C.) and high temperature (45 ° C.) in Examples 1 to 2 for two years, and there was no change in color.

3) pH stability

pH stability at pH 2, 5, 7 and 10 was visually observed at room temperature (25 ° C.) and the results are shown in Table 7 below.

From the above results, it was found that the aqueous composition according to the present invention had excellent storage stability, transparency without discoloration, and stability at a wide range of pH.

Experimental Example  2: Of nanoemulsion  Particle distribution measurement

The particle distribution of the nanoemulsions prepared in Examples 1 and 3 was measured using Photal ELS-Z and then shown in FIGS. 1 and 2, respectively. As a result, it was found that the diameter of the particles was 350 nm in Example 1 and 90 nm in Example 3.

Experimental Example  3: Nano Emulsion  Particle shooting

Particles of the nanoemulsion prepared in Example 3 were taken. Since the particle size of the nanoemulsion was too fine to be measured by a general optical microscope, it was photographed using a frozen electron microscope (JEM 1010, JEOL, Japan) (FIG. 3). It can be seen from FIG. 3 that the nanoemulsion was well formed with a relatively uniform size.

Experimental Example  4: Mastic Transdermal  Absorption Promotion Effect Experiment

Female hairless guinea pigs (strain IAF / HA-hrBR) of about 8 weeks were used. The abdominal skin of the guinea pig was excised and mounted in a Franz-type diffusion cell (Lab fine instruments, Korea). 50mM phosphate buffer (pH 7.4, 0.1M NaCl) was added to the receptor vessel (5 ml) of the Franz-type diffusion cell, and the diffusion cell was mixed and dispersed at 600 rpm at 32 ° C. Due to this difficulty, experiments were performed using fluorescein isothiocyanate (FITC), a reagent that is water soluble and used for staining upon cellular and transdermal absorption. 50 μl of FITC and nanoemulsion were placed in a donor container. Absorption and diffusion were carried out according to a predetermined time, and the skin where absorption and diffusion occurred was 0.64 cm ² . After absorption and diffusion of the active ingredient, the dried kimwipes or the 10 ml of ethanol are not absorbed and the emulsion remaining on the skin is washed. Then, the tip is spread using the tip-type equalizer to diffuse and diffuse the active ingredient into the receptor chamber. Was observed (FIG. 4).

As can be seen in the fluorescent material absorption aspect of Figure 4, the aqueous nanoemulsion composition according to the present invention was found to efficiently absorb transdermal mastic gum, in particular, the nanoemulsion containing propylene glycol is in the nanoemulsion containing glycerin Compared to the percutaneous absorption rate was much better.

Claims (6)

5 to 60% by weight of mastic gum, 5 to 50% by weight of oil, 3 to 30% by weight of polyglycerin fatty acid ester as emulsifier, 0.1 to 15% by weight of sucrose fatty acid ester as auxiliary emulsifier, 1 to 40% by weight of propylene glycol and the balance A mastic gum-containing aqueous nanoemulsion composition comprising water. The mastic gum-containing aqueous nanoemulsion composition according to claim 1, wherein the viscosity is 1 to 100 cP. The mastic gum-containing aqueous nanoemulsion composition according to claim 1, wherein the oil is at least one selected from the group consisting of olive oil, sunflower oil, medium chain triglyceride (MCT), jojoba oil and macadamia nut oil. The mastic gum-containing aqueous nanoemulsion composition according to claim 1, wherein the polyglycerol fatty acid ester is at least one selected from the group consisting of polyglycerol stearic acid, polyglycerin myristic acid, polyglycerol oleic acid, and polyglycerol lauric acid. . The aqueous mastic gum-containing aqueous solution according to claim 1, wherein the sucrose fatty acid ester is at least one selected from the group consisting of sucrose stearic acid ester, sucrose palmitate ester, sucrose myristic acid ester, sucrose oleic acid ester and sucrose lauric acid ester. Nanoemulsion Composition. A cosmetic or food comprising the mastic gum-containing aqueous nanoemulsion composition of any one of claims 1 to 5.

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