阅读说明：本技术 美白精油组合物及其应用 (Whitening essential oil composition and application thereof ) 是由 王晓芬 易光辉 吕佳桦 于 2020-05-15 设计创作，主要内容包括：本发明涉及美白精油组合物及其在美白皮肤与抑制黑色素生成上的应用。本发明揭示一种美白精油组合物,包含：扁柏(Chamaecyparis obtusa var.formosana)精油、红桧精油、锡兰肉桂精油、八角茴香精油,以及狭叶薰衣草精油。本发明亦揭示该美白精油组合物可被用来美白皮肤以及抑制黑色素生成。本发明亦揭示该美白精油组合物作为制备用来美白皮肤之医药品或化妆品的应用。(The invention relates to a whitening essential oil composition and application thereof in whitening skin and inhibiting melanin generation. The invention discloses a whitening essential oil composition, which comprises the following components: hinoki (chamaetyparis obtusa var. fortmosana) essential oil, sabina chinensis essential oil, cinnamomum zeylanicum essential oil, anise essential oil, and lavandula angustifolia essential oil. The invention also discloses that the whitening essential oil composition can be used for whitening skin and inhibiting melanin generation. The invention also discloses the application of the whitening essential oil composition in preparing medicines or cosmetics for whitening skin.)

1. A whitening essential oil composition is characterized in that: the whitening essential oil composition comprises: hinoki essential oil, red juniper essential oil, Ceylon cinnamon essential oil, anise essential oil, and Lavandula angustifolia essential oil.

2. Whitening essential oil composition according to claim 1, characterized in that: the whitening essential oil composition comprises the following components in an amount of 100 vol% of the total volume of the whitening essential oil composition:

15-30 vol% of hinoki essential oil;

15-30 vol% of red juniper essential oil;

20-30 vol% of cinnamon stannum essential oil;

10-30 vol% of star anise essential oil; and

10-30 vol% of lavender angustifolia essential oil.

3. Whitening essential oil composition according to claim 1, characterized in that: the whitening essential oil composition further comprises a pharmaceutically acceptable carrier or a cosmetically acceptable adjuvant.

4. Use of the whitening essential oil composition of any one of claims 1 to 3 for the preparation of a medicament or cosmetic for whitening the skin.

Technical Field

The present invention relates to a whitening essential oil composition, and more particularly, to an essential oil composition for whitening skin and inhibiting melanin production.

Background

Melanogenesis (melanin synthesis) refers to a process in which tyrosine (tyrosine) in melanocytes is converted into melanin (melanin) through catalysis of tyrosinase (tyrosine) by an enzyme after induction of skin melanocytes by environmental factors such as Ultraviolet (UV) or physiological factors such as fatigue (fatigue), stress (stress), chronic inflammation (chronic inflammation) and abnormal alpha-melanocyte stimulating hormone (alpha-MSH) release in vivo, and a series of redox reactions. Melanin can protect the hypodermis (hypodermis) of the skin from light damage caused by ultraviolet rays (photodemage), but skin diseases (skin disorders) such as freckles (lentigines), spots (freckle), melasma (melasma), age spots (age spots), hyperpigmentation (hyperpigmentation), and the like may be caused when melanin is accumulated on the skin in a large amount or is abnormally distributed.

In order to achieve skin whitening (skin whitening), many melanogenesis inhibitors (melanogenesis inhibitors) have been used to lighten or remove melanin or black spots accumulated on the skin, and these melanogenesis inhibitors mostly control the production of melanin by inhibiting the activity of tyrosinase, accelerating the degradation of tyrosinase, or promoting the decomposition of melanin. Among them, known melanin production inhibitors that can be used for inhibiting tyrosinase activity include hydroquinone (hydroquinone), arbutin (arbutin), kojic acid (kojic acid), and the like.

In recent years, there has been an increasing demand for skin whitening and caring, but the melanin production inhibitors currently used have still not been ideal in terms of lightening or removing melanin. Therefore, the relevant researchers in this field have tried to find natural active ingredients from natural sources that can be used for inhibiting melanin production. For example, extracts or essential oils made from a number of plant materials have been found to have utility in inhibiting melanin production, including: lavandula angustifolia (Lavandula angustifolia), Cymbopogon citrina (Cymbopogon citrifolia), bergamot (Citrus medica var. sarcodactylis), clove (Syzygium aromaticum), Cinnamomum zeylanicum (Cinnamomum verum), Aniseed (Illicium verum), Curcuma longa (Curcuma longa), Ocimum basilicum (Ocimum basilicum), rose (Rosa rugosa), Oenothera species (Oenothera spp.), Chamaecyparis obtusa (also called Chamaecyparis obtusa var. formosana), and Sabina chinensis (Chamaecarpa formosana). However, most of the above studies are only limited to the tests of single essential oil, and there are few studies on the whitening function of compound essential oil. Therefore, there is still a need to find compound essential oil with better whitening effect.

Disclosure of Invention

Through research, the applicant unexpectedly found that: a composition containing hinoki essential oil, red juniper essential oil, Ceylon cinnamon essential oil, star anise essential oil and Lavandula angustifolia essential oil can inhibit tyrosinase activity more effectively. Therefore, the whitening essential oil composition according to the present invention is expected to be available for whitening skin.

Accordingly, in a first aspect, the present invention provides a whitening essential oil composition comprising: hinoki (chamaetyparis obtusa var. fortmosana) essential oil, sabina chinensis essential oil, cinnamomum zeylanicum essential oil, anise essential oil, and lavandula angustifolia essential oil.

The whitening essential oil composition of the present invention, wherein the total volume of the whitening essential oil composition is 100 vol%, and the whitening essential oil composition comprises:

15-30 vol% of hinoki essential oil;

15-30 vol% of red juniper essential oil;

20-30 vol% of cinnamon stannum essential oil;

10-30 vol% of star anise essential oil; and

10-30 vol% of lavender angustifolia essential oil.

The whitening essential oil composition further comprises a pharmaceutically acceptable carrier or a cosmetically acceptable adjuvant.

In a second aspect, the present invention provides a use of the whitening essential oil composition as described above for preparing a pharmaceutical or cosmetic for whitening skin. .

The invention has the beneficial effects that: the whitening essential oil composition has better tyrosinase activity inhibition rate, and can be effectively used for various medicaments or cosmetics for whitening skin.

Detailed Description

The whitening essential oil composition comprises: hinoki (chamaetyparis obtusa var. formosana) essential oil, sabina chinensis essential oil, cinnamomum zeylanicum essential oil, anise essential oil, and lavandula angustifolia essential oil.

In the whitening essential oil composition of the present invention, hinoki essential oil, red juniper essential oil, stannum cinnamon essential oil, star anise essential oil, and Lavandula angustifolia essential oil are obtained by distilling and extracting wood of hinoki (chamaeecia obtusa var. fortiana), wood of red juniper (chamaeecia formosenis), bark of Cinnamomum zeylanicum (Cinnamomum verum), fruit of star anise (illium verum), and flower of Lavandula angustifolia (Lavandula angustifolia), respectively.

It can be understood that the operating conditions for the above extraction method are further varied depending on the treatment method of the plant used, the ratio of the amount of the plant used, and other factors, so as to achieve the optimum extraction effect. The choice of these operating conditions can be adjusted and varied according to the state of the art.

The content of each component of the whitening essential oil composition of the present invention can be adjusted according to actual use, and preferably, the total volume of the whitening essential oil composition is 100 vol%, and the whitening essential oil composition comprises: 15-30 vol% of hinoki essential oil, 15-30 vol% of red juniper essential oil, 20-30 vol% of Ceylon cinnamon essential oil, 10-30 vol% of star anise essential oil and 10-30 vol% of lavandula angustifolia essential oil.

The whitening essential oil composition according to the present invention was confirmed to effectively inhibit tyrosinase activity through in vitro experiments. Accordingly, the whitening essential oil composition according to the present invention is expected to have an effect of promoting skin whitening, and thus may be applied to the preparation of pharmaceuticals or cosmetics for whitening skin.

As used herein, the terms "lightening" and "skin color lightening", "bleaching", "clear", "whitening", "darkening", "lightening the melanin", "inhibiting the melanin production", and "inhibiting the melanin synthesis" are used interchangeably.

According to the present invention, the pharmaceutical product may be formulated into a dosage form suitable for topical (topically) administration using techniques well known to those skilled in the art.

According to the present invention, the pharmaceutical may further comprise a pharmaceutically acceptable carrier (pharmaceutically acceptable carrier) which is widely used in pharmaceutical manufacturing technology. For example, the pharmaceutically acceptable carrier may comprise one or more agents selected from the group consisting of: solvents (solvent), buffers (buffer), emulsifiers (emulsifying), suspending agents (suspending agent), disintegrating agents (disintegrant), disintegrating agents (disintegrating agent), dispersing agents (dispersing agent), binding agents (binding agent), excipients (excipient), stabilizers (stabilizing agent), chelating agents (chelating agent), diluents (diluent), gelling agents (gelling agent), preservatives (preserving), wetting agents (wetting agent), lubricants (lubricating), absorption delaying agents (absorption delaying agent), liposomes (liposome) and the like. The selection and amounts of these agents are within the skill and routine skill of those in the art.

According to the present invention, the medicament may also be manufactured into external preparations (external preparation) suitable for topical application to the skin using techniques well known to those skilled in the art, including, but not limited to: creams (creams), patches (patches), liniments (liniments), powders (powders), aerosols (aerogels), sprays (sprays), emulsions (positions), serums (serums), pastes (pastes), foams (foams), drops (drops), suspensions (suspensions), ointments (salves), bandages (bandages) and oils (oils).

According to the invention, the external preparation is prepared by mixing the pharmaceutical with a base (base) as known in detail to the person skilled in the art.

According to the invention, the substrate may comprise one or more additives (additives) selected from the following group: water, alcohols, glycols, hydrocarbons, such as waxesy) and white petrolatum (white petrolatum)]Wax (wax) [ such as Paraffin and yellow wax (yellow wax)]Preserving agents (preserving agents), antioxidants (antioxidants), surfactants (surfactants), absorption enhancers (absorption enhancers), stabilisers (stabilizing agents), gelling agents (gelling agents) [ such as974P(974P), microcrystalline cellulose (microcrystalline cellulose) and carboxymethyl cellulose (carboxymethyl cellulose)]Active agents (actives), moisturizers (humectants), odor absorbers (odor absorbers), perfumes (fragrans), pH adjusting agents (pH adjusting agents), chelating agents (chelating agents), emulsifiers (emulsifiers), occlusive agents (occlusive agents), softeners (emulsifiers), thickeners (thickeners), solubilizing agents (solubilizing agents), penetration enhancers (penetration enhancers), anti-irritants (anti-irritants), colorants (colorants), and propellants (propellants). The selection and amounts of these additives are within the expertise and routine skill of those skilled in the art.

According to the present invention, the cosmetic may further comprise a cosmetically acceptable adjuvant (cosmetically acceptable adjuvant) which is widely used in cosmetic manufacturing technology. For example, the cosmetically acceptable adjuvant may comprise one or more agents selected from the group consisting of: solvents (solvent), gelling agents, active agents, preservatives (preservative), antioxidants, screening agents (screening agents), chelating agents, surfactants, colouring agents (colouring agents), thickening agents (thickening agents), fillers (filler), fragrances and odour absorbers. The selection and amounts of these agents are within the skill and routine skill of those in the art.

According to the present invention, the cosmetic may be manufactured in a form suitable for skin care (skincare) or makeup (makeup) using techniques well known to those skilled in the art, including, but not limited to: aqueous solutions (aqueous solutions), aqueous-alcoholic solutions (aqueous-alcoholic solutions) or oily solutions (oil solutions), emulsions in the form of oil-in-water type, water-in-oil type or compound type, gels, ointments, creams, masks (masks), patches (packs), liniments, powders, aerosols, sprays, lotions, serums, pastes, foams, dispersions, drops, mousses (mousses), sunblocks, lotions (toiletries), foundations (foundations), eyeshadows (eyeshadows), make-up removal products (make-up removal products), soaps (soaps), and other body cleansing products (body cleansing products).

According to the invention, the cosmetic may also be used in combination with one or more known active external agents (external use agents) selected from the following: whitening agents (whitening agents) [ such as retinoic acid (tretinoin), catechins (catechin), kojic acid, arbutin and vitamin C ], moisturizers, anti-inflammatory agents (anti-inflammatory agents), bactericides (bacteriodes), ultraviolet absorbers (ultraviolets absorbers), plant extracts (plant extracts) [ such as aloe extract (aloe extract) ], skin nutrients (skin nutrients), anesthetics (anesthesics), anti-acne agents (anti-acne agents), antipruritic agents (antipruritic), analgesic agents (analgesic), anti-dermatitis agents (antipermatitis agents), anti-hyperkeratotic agents (antiperokeratotic agents), anti-dry skin agents (anti-dry skin agents), anti-dry tinea agents (anti-dry skin agents), anti-aging agents (anti-aging agents), anti-wrinkle agents (anti-rinking agents), anti-seborrheic agents (anti-anemarrhena agents), wound healing agents (wound-healing agents), corticosteroids (corticosteriodic agents), and hormones (hormones). The selection and amounts of these external agents are within the skill and routine skill of those skilled in the art.

The present invention also provides a method for whitening skin, which comprises administering the whitening essential oil composition of the present invention to an individual in need of skin whitening promotion. Preferably, the method comprises applying to the skin of the subject an effective amount of a whitening essential oil composition for a sufficient period of time until the melanin of the skin is significantly lightened.

As used herein, the terms "administering" and "administration" are used interchangeably.

As used herein, the term "effective amount" means a safe amount sufficient to provide a desired whitening effect without causing undesirable adverse side effects to the skin when the whitening essential oil composition of the present invention is administered to an individual in need of skin whitening promotion.

As used herein, the terms "effective amount" and "effective dose" (effective dose), "whitening effective amount" and "whitening effective dose" may be used interchangeably.

According to the present invention, the effective amount and frequency of application (frequency of application) of the whitening essential oil composition may vary depending on the following factors: the initial condition of the area of skin to be depigmented (initial condition) and the final whitening effect to be achieved. In general, when the whitening essential oil composition according to the present invention is topically applied to the skin, the effective amount per application is generally 5 to 10mg per square centimeter of skin area, about 1 to 2 times per day.

The invention will be further described with respect to the following examples, but it should be understood that these examples are for illustration only and should not be construed as limiting the practice of the invention.

General experimental methods:

1. statistical analysis (statistical analysis):

in the following examples, all experimental data are expressed as "mean ± Standard Deviation (SD)".

< examples 1-4> preparation of whitening essential oil composition of the present invention

The following individual essential oils used to prepare the whitening essential oil composition of the present invention include:

1. hinoki (chamaetyparis obtusa var. fortusana) essential oil, purchased from baiguan biochemical science and technology ltd, with a concentration of 1000 ppm;

2. essential oil of red juniper (chamaetyparis formosensis) available from delphing corporation at a concentration of 1000 ppm;

3. illicium verum essential oil, available from FPI SALES Taiwan Branch of China (trade name: pure Illicium verum essential oil), with a concentration of 1000 ppm;

4. cinnamomum zeylanicum (Cinnamomum verum) Essential Oil, available from Sydney Essential Oil Co. (trade name: Cinnamon Bark Oil), at a concentration of 1000 ppm; and

5. lavender angustifolia (Lavandula angustifolia) Essential Oil, available from Sydney Essential Oil Co [ trade name: lavender Oil (Bulgaria) ], concentration 1000 ppm.

The above 5 single essential oils were mixed according to the formula shown in table 1 below to obtain the whitening essential oil compositions of examples 1 to 4.

TABLE 1 formulation of whitening essential oil composition of examples 1 to 4

< comparative examples 1 to 5> Single ingredient essential oils

For comparison, 5 single-component essential oils of hinoki essential oil, red juniper essential oil, cinnamon essential oil, anise essential oil and lavandula angustifolia essential oil used for preparing examples 1 to 4 were respectively used as comparative examples 1 to 5 by the applicant.

< comparative examples 6 to 8> comparative essential oil compositions

The formulations of comparative examples 6 to 8 were further carried out according to the kinds and contents of essential oils of table 2 below to obtain the control essential oil compositions of comparative examples 6 to 8.

TABLE 2 formulation of control essential oil composition of comparative examples 6 to 8

"means not added, and the content is 0 vol%.

< test > determination of the ability to inhibit tyrosinase Activity

Next, the applicant evaluated the effect of the whitening essential oil composition of the present invention on the inhibition of melanin production by measuring tyrosinase activity (tyrosinase activity) of the above examples 1 to 4. In addition, for comparison, comparative examples 1 to 8 were also subjected to the same experiment.

The test method comprises the following steps: first, 4.556g of potassium dihydrogen phosphate (monobasic phosphate) and 4.757g of disodium hydrogen phosphate (Sodium hydrogen phosphate) were dissolved in 500mL of deionized water, respectively, and then mixed uniformly to obtain a 67mM phosphate buffer solution (phosphate buffer solution) having a pH of 6.8. Next, 50U of tyrosinase (L-tyrosine) (available from Youkou and trade Co., Ltd.) was added to an appropriate amount of phosphate buffer solution to obtain a tyrosinase solution with a concentration of 50U/mL.

Thereafter, the single essential oil and essential oil compositions of examples 1 to 4 and comparative examples 1 to 8 were mixed with Tween-20 (available from merck gmbh, taiwan) at a ratio of 1: 8(v/v), and then adding a proper amount of phosphate buffer solution to ensure that the final concentration of each single essential oil and the essential oil composition is 1000 ppm. Then, 50. mu.L of each of the essential oil compositions of examples 1 to 4 and the single essential oils and essential oil compositions of comparative examples 1 to 8 diluted to 1000ppm was added with 120. mu.L of 2.5mM L-3,4-dihydroxyphenylalanine (L-3,4-dihydroxyphenylalanine, L-DOPA) (available from Youke and trade, Inc.) (prepared in phosphate buffer solution) and 100. mu.L of tyrosinase solution, and the resulting mixture was uniformly mixed, and the mixture was kept in a dark place at 37 ℃ for 30 minutes, and then the absorbance (OD) was measured by a spectrophotometer at a wavelength of 475nm₄₇₅). In addition, 0.08g of Tween-20 was dissolved in 10mL of phosphate buffer solution to serve as a blank control group to carry out the same experiment. If the measured absorbance value (OD)₄₇₅) The lower the level, the better the ability to inhibit tyrosinase activity.

Tyrosinase activity inhibition (%) was determined by measuring the absorbance (OD)₄₇₅) Calculated by substituting the following formula (I):

A＝[1-(B/C)]×100 (I)

wherein: tyrosinase activity inhibition rate (%)

B-OD measured in each example or comparative example₄₇₅Absorbance value

C-OD measured in blank control group₄₇₅Absorbance value

The expected inhibition (%) for examples 1 to 4 and comparative examples 6 to 8 was calculated from the tyrosinase activity inhibition measured for the single essential oils of comparative examples 1 to 5 and the contents of the single essential oils in examples 1 to 4.

Thereafter, the experimental data obtained were analyzed according to the method described in "statistical analysis" of item 1 of the above "general experimental methods". The results obtained are shown in tables 3,4 and 5 below, respectively.

TABLE 3 tyrosinase activity inhibition rates of comparative examples 1 to 5

TABLE 4 tyrosinase activity inhibition rates of examples 1 to 4

^*: a represents Chamaecyparis obtusa (Chamaecyparis obtusa var. fortusana) essential oil; b represents the essential oil of the red juniper; c represents the cinnamon essential oil; d represents anise essential oil; and E represents lavender angustifolia essential oil.

TABLE 5 tyrosinase activity inhibition rates of comparative examples 6 to 8

^*: a represents Chamaecyparis obtusa (Chamaecyparis obtusa var. fortusana) essential oil;b represents the essential oil of the red juniper; c represents the cinnamon essential oil; d represents anise essential oil; and E represents lavender angustifolia essential oil.

As can be seen from tables 3 and 4, the tyrosinase activity inhibition rates of the single essential oils of comparative examples 1 to 5 fell to about 29% to 53%, and the cypress essential oil of comparative example 1 had the highest tyrosinase activity inhibition rate (52.62. + -. 1.46%). On the other hand, the tyrosinase activity inhibition rates of the whitening essential oil compositions of examples 1 to 4 were approximately 57% to 63%, which were higher than those of comparative examples 1 to 5. Moreover, the tyrosinase activity inhibition rates actually measured in examples 1 to 4 are much higher than the expected inhibition rates, and the difference is about 14.0% to 18.3%, which shows that the results of examples 1 to 4 cannot be achieved by the simple superposition of the effects of comparative examples 1 to 5, and simultaneously proves that the whitening essential oil composition of the invention can effectively inhibit the tyrosinase activity and further inhibit the melanin generation.

As can be seen from tables 4 and 5, the tyrosinase activity inhibition rates of comparative examples 6 to 8 fall within about 45% to 51%, which are lower than those of examples 1 to 4, and the inhibition rates of comparative examples 6 to 8 are not significantly improved compared to the corresponding expected inhibition rates. Among them, comparative example 7 obtained by mixing hinoki (chamaetyparis obtusa var. formosana) essential oil, sabina rubra juniper essential oil, cinnamomum zeylanicum essential oil, and anisum acutangula essential oil, and comparative example 8 obtained by mixing hinoki (chamaetyparis obtusa var. formosana) essential oil, sabina rubra juniper essential oil, anisum acutangula essential oil, and lavandula angustifolia essential oil, the actual measured tyrosinase activity inhibition rate was only slightly increased compared with the expected inhibition rate; in particular, in comparative example 6 in which hinoki essential oil, hinoki essential oil and Ceylon cinnamon essential oil having a high tyrosinase activity inhibition rate (45% or more) were selected, the actually measured tyrosinase activity inhibition rate was even lower than the expected tyrosinase activity inhibition rate, showing that the results of examples 1 to 4 of the present invention were not achieved by simple substitution or combination of comparative examples 1 to 5, and further proving that the whitening essential oil composition of the present invention necessarily contains hinoki (Chamaecyparis obtusa var. fortunei) essential oil, hinoki essential oil, Ceylon cinnamon essential oil, Illicium verum essential oil and Lavandula angustifolia essential oil at the same time.

In summary, the whitening essential oil composition according to the present invention contains the specific plant essential oil combination, so that the tyrosinase activity can be effectively inhibited, and the effects of inhibiting melanin generation and promoting skin whitening can be achieved. From the foregoing, it is also demonstrated that the whitening essential oil composition of the present invention has a high potential to develop into a melanogenesis inhibitor (i.e., skin whitening agent).

All patents and documents cited in this specification are incorporated herein by reference in their entirety. In case of conflict, the present detailed description, including definitions, will control.

While the invention has been described with reference to the specific embodiments described above, it will be apparent that numerous modifications and variations can be made without departing from the scope and spirit of the invention. It is the intention, therefore, to be limited only as indicated by the claims appended hereto.