TWI748424B - Whitening essential oil composition and its use - Google Patents

Abstract

The present invention discloses a whitening essential oil composition comprising: Taiwan cypress essential oil, red juniper essential oil, Ceylon cinnamon essential oil, star anise essential oil, and anise lavender essential oil. The present invention also discloses that the whitening essential oil composition can be used to whiten skin and inhibit melanin production.

Description

Whitening essential oil composition and its use

The present invention relates to a whitening essential oil composition, in particular to an essential oil composition used for whitening skin and inhibiting melanin production.

Melanogenesis (also known as melanin synthesis) refers to when skin melanocytes (dermal melanocytes) are exposed to environmental factors (such as ultraviolet (UV)) or physiological factors (such as fatigue, stress ( After the induction of stress, chronic inflammation, and abnormal release of α-melanocyte stimulating hormone (α-MSH) in the body, tyrosine in melanocytes The process of being converted into melanin through the catalysis of tyrosinase [it is the rate-limiting step of melanin production] and a series of redox reactions. Melanin can protect the hypodermis of the skin from photodamage caused by ultraviolet rays. However, when melanin is accumulated on the skin in large amounts or is abnormally distributed, it may cause skin disorders, such as freckles. (lentigines), spots (freckle), melasma (melasma), age spots (age spots) and hyperpigmentation (hyperpigmentation) and so on.

In order to achieve the purpose of skin whitening, many melanogenesis inhibitors have been used to lighten or remove the accumulated melanin or dark spots on the skin. Most of these melanogenesis inhibitors are inhibited Mechanisms such as tyrosinase activity, acceleration of tyrosinase degradation, or promotion of melanin decomposition can regulate the production of melanin. Among them, melanin production inhibitors known to be useful for inhibiting tyrosinase activity include hydroquinone, arbutin, and kojic acid.

In recent years, human needs for skin whitening and maintenance have increased day by day. However, the melanin production inhibitors currently used are still not satisfactory in lightening or removing melanin. Therefore, relevant researchers in the field try to find natural active components that can be used to inhibit melanin production from natural sources. For example, extracts or essential oils made from many plant materials have been found to have the effect of inhibiting melanin production. These plants include: Lavandula angustifolia , Cymbopogon citratus , and Citrus medica var.sarcodactylus ), Clove ( Syzygium aromaticum ), Cinnamomum verum , Illicium verum , Curcuma longa , Ocimum basilicum , Rosa rugosa , Oenothera spp., Taiwan cypress ( Chamaecyparis obtusa var.formosana ) (also known as yellow cypress) and red cypress ( Chamaecyparis formosensis ) and so on. However, most of the above-mentioned studies are only limited to the trials of single essential oils, and there are few studies on the use of compound essential oils for whitening functions. Therefore, there is still a need to find compound essential oils with better whitening effects.

After research, the applicant unexpectedly found that a composition containing Taiwan cypress essential oil, red cypress essential oil, Ceylon cinnamon essential oil, star anise essential oil, and lavender essential oil can more effectively inhibit tyrosinase activity. Therefore, the whitening essential oil composition according to the present invention is expected to be useful for whitening skin.

The first object of the present invention is to provide a whitening essential oil composition.

Therefore, the whitening essential oil composition of the present invention includes: Taiwan cypress essential oil, red juniper essential oil, Ceylon cinnamon essential oil, star anise essential oil, and lavender essential oil.

The second object of the present invention is to provide a use of the above-mentioned whitening essential oil composition for preparing a medicine or cosmetic for skin whitening.

The effect of the present invention is that the whitening essential oil composition of the present invention has a good inhibition rate of tyrosinase activity, and can be effectively used in various skin whitening medicines or cosmetics.

The above and other objects, features, and advantages of the present invention will become apparent with reference to the following detailed description.

The whitening essential oil composition of the present invention includes: Taiwan cypress essential oil, red cypress essential oil, Ceylon cinnamon essential oil, star anise essential oil, and anise lavender essential oil.

In the whitening essential oil composition of the present invention, Taiwan cypress essential oil, red cypress essential oil, Ceylon cinnamon essential oil, star anise essential oil, and anise lavender essential oil are obtained by combining the wood and red cypress (Chamaecyparis obtusa var. formosana) of Taiwan cypress (Chamaecyparis obtusa var. formosana). The wood of Chamaecyparis formosensis , the bark of Cinnamomum verum , the fruit of Illicium verum , and the flowers of Lavandula angustifolia are obtained by distillation.

It can be understood that the operating conditions related to the above-mentioned extraction method will be further changed according to factors such as the treatment method of the plant used and the dosage ratio of the plant in order to achieve the best extraction effect. The selection of these operating conditions can be adjusted and changed according to known technologies.

The content of each component of the whitening essential oil composition of the present invention can be adjusted according to actual use. Preferably, the total volume of the whitening essential oil composition is 100 vol%, and the whitening essential oil composition includes: 15-30 vol% Taiwan cypress essential oil, 15~30vol% red juniper essential oil, 20~30vol% Ceylon cinnamon essential oil, 10~30vol% star anise essential oil, and 10~30vol% lavender essential oil.

The whitening essential oil composition according to the present invention has been confirmed through in vitro tests to effectively inhibit tyrosinase activity. Accordingly, the whitening essential oil group according to the present invention The product is expected to have the effect of promoting skin whitening, and therefore can be applied to the preparation of a medicine or cosmetics for skin whitening.

As used herein, the terms "whitening" and "skin color lightening", "bleaching", "whitening", "brightening", "blackening", " "Inhibition of melanin", "lightening the melanin", "inhibition of melanogenesis" and "inhibition of melanin synthesis" can be used interchangeably.

According to the present invention, the medicine can be manufactured into a dosage form suitable for topically administration using techniques well known to those skilled in the art.

According to the present invention, the drug may further include a pharmaceutically acceptable carrier widely used in drug manufacturing technology. For example, the pharmaceutically acceptable carrier may include one or more reagents selected from the group consisting of solvent, buffer, emulsifier, suspending agent, decomposer ), disintegrating agent, dispersing agent, binding agent, excipient, stabilizing agent, chelating agent, diluent , Gelling agent, preservative, wetting agent, lubricant, absorbent Absorption delaying agents, liposomes and the like. The selection and quantity of these reagents fall within the scope of professionalism and routine techniques of those who are familiar with this technique.

According to the present invention, the medicine can also be manufactured into an external preparation suitable for topical application to the skin by using techniques well known to those skilled in the art. This includes, but is not limited to: emulsions , Gel, ointment, cream, patch, liniment, powder, aerosol, spray, lotion , Serum, paste, foam, drop, suspension, salve, bandage and oil.

According to the present invention, the external preparation is prepared by mixing the medicine with a base well known to those skilled in the art.

According to the present invention, the substrate may contain one or more additives selected from the following: water, alcohols, glycols, hydrocarbons (such as petroleum jelly) and white Vaseline (white petrolatum), wax (such as paraffin and yellow wax), preserving agents, antioxidants, surfactants, absorption enhancers enhancers), stabilizers (stabilizing agents), gelling agent (gelling agents) [such as Carbopol ^® 974P (carbopol ^® 974P), microcrystalline cellulose (microcrystalline cellulose) and carboxymethyl cellulose (carboxymethyl cellulose)], Active agents, humectants, odor absorbers, fragrances, pH adjusting agents, chelating agents, emulsifiers, occlusive agents (occlusive agents), emollients, thickeners, solubilizing agents, penetration enhancers, anti-irritants, colorants and propellants (propellants) and so on. The selection and quantity of these additives fall within the scope of professionalism and routine technology of those who are familiar with this technology.

According to the present invention, the cosmetic may further include a cosmetically acceptable adjuvant which is widely used in cosmetic manufacturing technology. For example, the cosmetically acceptable adjuvant may contain one or more agents selected from the group consisting of solvents, gelling agents, active agents, preservatives, antioxidants, screening agents, Chelating agents, surfactants, coloring agents, thickening agents, fillers, fragrances and odor absorbers. The selection and quantity of these reagents fall within the scope of professionalism and routine techniques of those who are familiar with this technique.

According to the present invention, the cosmetic can be made into a shape suitable for skincare or makeup by using techniques well known to those skilled in the art. Formula, this includes, but is not limited to: aqueous solution (aqueous solution), water-alcohol solution (aqueous-alcohol solution) or oily solution (oily solution), oil-in-water type, oil package Water-in-oil type or compound emulsion, gel, ointment, cream, mask, patch, pack, liniment, powder, aerosol, spray, lotion, Cream, paste, foam, dispersion, drops, mousse, sunblock, tonic water, foundation, eyeshadow, makeup remover products , Soap and other body cleansing products.

According to the present invention, the cosmetic can also be used in combination with one or more external use agents with known activity selected from the following: whitening agents (such as tretinoin, catechins) (catechin), kojic acid, arbutin and vitamin C], moisturizers, anti-inflammatory agents, bactericides, ultraviolet absorbers, plant extracts [ Such as aloe extract, skin nutrients, anesthetics, anti-acne agents, antipruritic, analgesic, and anti-dermatitis agents (antidermatitis agents), antihyperkeratolytic agents, anti-dry skin agents, antipsoriatic agents, antiaging agents agents, antiwrinkle agents, antiseborrheic agents, wound-healing agents, corticosteroids and hormones. The selection and quantity of these topical agents fall within the scope of professionalism and routine techniques of those who are familiar with this technique.

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 who needs to promote skin whitening. Preferably, the method includes applying an effective amount of the whitening essential oil composition to the skin of the individual, and for a sufficient time until the melanin of the skin is significantly reduced.

As used herein, the terms "administering" and "administering" and "application" can be used interchangeably.

As used herein, the term "effective amount" means that when the whitening essential oil composition of the present invention is administered to an individual who needs to promote skin whitening, it is sufficient to provide the desired whitening effect and will not be harmful A safe dosage for undesirable adverse side effects to the skin.

As used herein, the terms "effective amount" and "effective dose", "whitening effective amount" and "whitening effective dose" can be used interchangeably.

According to the present invention, the effective amount and frequency of application of the whitening essential oil composition will vary depending on the following factors: to be lightened black The initial condition of the skin area and the desired final whitening effect. Generally speaking, when the whitening essential oil composition according to the present invention is topically applied to the skin, the effective amount per application is usually 5 to 10 mg/cm² of skin area, about 1 to 2 times a day.

The present invention will be further described with the following embodiments, but it should be understood that these embodiments are for illustrative purposes only, and should not be interpreted as limitations on the implementation of the present invention.

General experimental method: 1. Statistical analysis:

In the following examples, all experimental data are expressed as "mean ± standard deviation (SD)".

<Example 1-4> Preparation of the whitening essential oil composition of the present invention

The individual essential oils used to prepare the whitening essential oil composition of the present invention below include: 1. Taiwan cypress ( Chamaecyparis obtusa var. formosana ) essential oil, purchased from Baiguan Biochemical Technology Co., Ltd. (trade name: Taiwan cypress essential oil), concentration 1000ppm; 2. Red cypress ( Chamaecyparis formosensis ) essential oil, purchased from Deli Industrial Co., Ltd. (trade name: Taiwan red cypress essential oil), with a concentration of 1000ppm; 3. Illicium verum (Illicium verum) essential oil, purchased from FPI SALES TAIWAN (commodity) Name: star anise pure essential oil, concentration 1000ppm; 4. Cinnamomum verum essential oil, purchased from Sydney Essential Oil Co. (trade name: Cinnamon Bark Oil), concentration 1000ppm; and 5. Lavandula angustifolia ) essential oil, purchased from Sydney Essential Oil Co. [trade name: Lavender Oil (Bulgaria)], with a concentration of 1000 ppm.

The above 5 kinds of 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.

<Comparative Example 1-5> Single Essential Oil

For comparison, the applicant used the five single essential oils of Taiwan cypress essential oil, red cypress essential oil, Ceylon cinnamon essential oil, star anise essential oil, and lavender essential oil used in the preparation of Examples 1 to 4 as Comparative Examples 1 to 5, respectively.

<Comparative Example 6-8> Control Essential Oil Composition

In addition, the formulations of Comparative Examples 6 to 8 were performed according to the types and contents of the essential oils in Table 2 below to obtain the control essential oil compositions of Comparative Examples 6 to 8.

「-」表示未添加，含量為0vol%。

"-" means no addition, and the content is 0vol%.

<Test> Determination of the ability to inhibit tyrosinase activity

Next, the applicant evaluated the effectiveness of the whitening essential oil composition of the present invention in inhibiting melanin production by measuring the tyrosinase activity of the above-mentioned Examples 1 to 4. In addition, for comparison, Comparative Examples 1 to 8 were also used for the same experiment.

Test method: First, dissolve 4.556 g of monopotassium phosphate and 4.757 g of sodium hydrogen phosphate in 500 mL of deionized water, and then mix them uniformly to obtain a pH of 6.8 67mM phosphate buffer solution (phosphate buffer solution). Next, 50U of tyrosine (L-tyrosine) (purchased from Youhe Trading Co., Ltd.) was added to an appropriate amount of phosphate buffer solution to obtain a tyrosinase solution with a concentration of 50 U/mL.

After that, the single essential oils and essential oil compositions of Examples 1 to 4 and Comparative Examples 1 to 8 and Tween-20 (purchased from Taiwan Merck Co., Ltd.) were set at a ratio of 1:8 (v/v). Mix well, and then add an appropriate amount of phosphate buffer solution, so that the final concentration of each single essential oil and essential oil composition is 1000 ppm. Next, take 50 μL of the essential oil composition of Examples 1 to 4 and the single essential oil and essential oil composition of Comparative Examples 1 to 8 diluted to 1000 ppm, and add 120 μL of 2.5 mM L-3,4-dihydroxyphenylpropane respectively. L-3,4-dihydroxyphenylalanine (L-DOPA) (purchased from Youhe Trading Co., Ltd.) (prepared in phosphate buffer solution), and 100μL of tyrosinase solution and mixed uniformly to form The mixture was placed at 37°C for light protection for 30 minutes, and then the absorbance (OD ₄₇₅ ) was measured with a spectrophotometer at a wavelength of 475 nm. In addition, 0.08 g of Tween-20 was dissolved in 10 mL of phosphate buffer solution as a blank control group to perform the same experiment. If the measured absorbance value (OD ₄₇₅ ) is lower, it means that the ability to inhibit tyrosinase activity is better.

Tyrosinase activity inhibition rate (%) is _{calculated by substituting the measured absorbance value (OD 475} ) into the following formula (I): A=[1-(B/C)]×100 (I )

Among them: A = Inhibition rate of tyrosinase activity (%)

_{B = OD 475} absorbance measured in each embodiment or comparative example

_{C= OD 475} absorbance measured by the blank control group

The expected inhibition rate (%) of the relevant Examples 1 to 4 and Comparative Examples 6 to 8 is the tyrosinase activity inhibition rate measured by the single essential oils of Comparative Examples 1 to 5 and the single essential oils in Examples 1 to 5 Calculated from the content in 4.

After that, analyze the experimental data obtained in accordance with the method described in the first item "Statistical Analysis" of the "General Experimental Methods" above. The results obtained are shown in Table 3, Table 4, and Table 5 below, respectively.

From Table 3 and Table 4, it can be seen that the tyrosinase activity inhibition rate of the single essential oils of Comparative Examples 1 to 5 is about 29% to 53%, and among them, the essential oil of Taiwan Cypress of Comparative Example 1 has the highest tyrosine. Enzyme activity inhibition rate (52.62±1.46%). On the other hand, the inhibition rate of tyrosinase activity of the whitening essential oil composition of Examples 1 to 4 is about 57% to 63%, which is higher than that of Comparative Examples 1 to 5. Moreover, the inhibition rate of tyrosinase activity actually measured in Examples 1 to 4 is much higher than its expected inhibition rate, with a difference of about 14.0% to 18.3%, showing that the results of Examples 1 to 4 cannot be achieved by simply superimposing the effects of Comparative Examples 1 to 5, and it also proves that the whitening essential oil composition of the present invention can effectively inhibit tyrosinase activity, thereby inhibiting melanin production.

It can be seen from Table 4 and Table 5 that the inhibition rate of tyrosinase activity of Comparative Examples 6 to 8 is about 45% to 51%, which are all lower than the inhibition rate of Examples 1 to 4, and compared to the corresponding expected inhibition rate. The inhibition rate of Comparative Examples 6 to 8 also did not increase significantly. Among them, comparative example 7 obtained by mixing Taiwan cypress essential oil, red cypress essential oil, Ceylon cinnamon essential oil, and star anise essential oil, and a comparison obtained by mixing Taiwan cypress essential oil, red cypress essential oil, star anise essential oil, and lavender essential oil In Example 8, the actually measured inhibition rate of tyrosinase activity was only slightly increased compared to its expected inhibition rate; in particular, the Taiwan cypress essential oil, which has a higher inhibition rate of tyrosinase activity (above 45%), was selected. In Comparative Example 6 obtained by mixing red juniper essential oil and Ceylon cinnamon essential oil, the actually measured inhibition rate of tyrosinase activity was even lower than its expected inhibition rate, showing that the results of Examples 1 to 4 of the present invention are not through comparison What can be achieved by the simple replacement or combination of Examples 1 to 5 further proves that the whitening essential oil composition of the present invention must contain Taiwan cypress essential oil, red cypress essential oil, Ceylon cinnamon essential oil, star anise essential oil and lavender essential oil at the same time.

In summary, the whitening essential oil composition according to the present invention can effectively inhibit the activity of tyrosinase due to the combination of specific plant essential oils, thereby achieving the functions of inhibiting melanin production and promoting skin whitening. It is also proved by the foregoing that the whitening essential oil group of the present invention The product has high potential to develop into a melanogenesis inhibitor (ie, skin whitening agent).

All patents and documents cited in this specification are incorporated into this case as reference materials in their entirety. If there is a conflict, the detailed description of the case (including the definition) will prevail.

Although the present invention has been described with reference to the above specific specific examples, it is obvious that many modifications and changes can be made without departing from the scope and spirit of the present invention. Therefore, it is intended that the present invention is only limited by the scope of the patent application attached hereto.

Claims (3)

A whitening essential oil composition comprising: Taiwan cypress essential oil, red cypress essential oil, Ceylon cinnamon essential oil, star anise essential oil, and anise lavender essential oil; wherein the total volume of the whitening essential oil composition is 100 vol%, and the whitening essential oil is composed of Contains: 15~30vol% Taiwan cypress essential oil; 15~30vol% red cypress essential oil; 20~30vol% Ceylon cinnamon essential oil; 10~30vol% star anise essential oil; and 10~30vol% lavender essential oil . The whitening essential oil composition of claim 1, which further comprises a pharmaceutically acceptable carrier or a cosmetically acceptable adjuvant. A whitening essential oil composition as claimed in any one of Claims 1 to 2 is supplied for use in the preparation of a medicine or cosmetic for skin whitening.