JP6957289B2 - Whitening cosmetic composition - Google Patents

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JP6957289B2
JP6957289B2 JP2017181860A JP2017181860A JP6957289B2 JP 6957289 B2 JP6957289 B2 JP 6957289B2 JP 2017181860 A JP2017181860 A JP 2017181860A JP 2017181860 A JP2017181860 A JP 2017181860A JP 6957289 B2 JP6957289 B2 JP 6957289B2
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信一 篠▲崎▼
篤史 泉
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メディカランド株式会社
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Description

本発明は、美白化粧料組成物に関する。 The present invention relates to a whitening cosmetic composition.

美白化粧料に含まれる美白成分として、塩化ステアリルジメチルベンジルアンモニウム−ハイドロキノン分子錯体(「ステアラルコニウムクロリド(以下、「SHQ」と呼ぶことがある)(特許文献1)が知られている。 As a whitening ingredient contained in whitening cosmetics, a stearyldimethylbenzylammonium chloride-hydroquinone molecular complex (“stearylconium chloride (hereinafter, may be referred to as“ SHQ ”)) (Patent Document 1) is known.

一方、乳酸−グリコール酸共重合体(以下、「PLGA」と呼ぶことがある)は、内部に物質を抱合できるナノ粒子を形成することが公知の物質であり、PLGAナノ粒子の内部に医薬品を抱合させて体内の必要箇所に送達する、薬剤送達系(DDS)が知られている(特許文献2〜4)。また、フラーレンナノ粒子をDDSに用いることも知られている(特許文献5)。さらに、白金コロイド粒子(「プラチナナノコロイド」とも呼ばれる)は、抗酸化作用があることが知られており、化粧料組成物の添加剤としても用いられている(特許文献6)。 On the other hand, a lactic acid-glycolic acid copolymer (hereinafter sometimes referred to as "PLGA") is a substance known to form nanoparticles capable of conjugating a substance inside, and a drug is placed inside the PLGA nanoparticles. A drug delivery system (DDS) that conjugates and delivers to a required place in the body is known (Patent Documents 2 to 4). It is also known that fullerene nanoparticles are used for DDS (Patent Document 5). Further, platinum colloid particles (also referred to as "platinum nanocolloids") are known to have an antioxidant effect, and are also used as additives in cosmetic compositions (Patent Document 6).

特開2004-99542号公報Japanese Unexamined Patent Publication No. 2004-99542 特開2006-28031号公報Japanese Unexamined Patent Publication No. 2006-28031 特開2006-131577号公報Japanese Unexamined Patent Publication No. 2006-131577 特開2011-529492号公報Japanese Unexamined Patent Publication No. 2011-529492 特開2005-281231号公報Japanese Patent Application Laid-Open No. 2005-281231 特開2012-031086号公報Japanese Unexamined Patent Publication No. 2012-031086

本発明の目的は、優れた美白効果を有する新規な美白化粧料組成物を提供することである。 An object of the present invention is to provide a novel whitening cosmetic composition having an excellent whitening effect.

本願発明者らは、鋭意研究の結果、PLGAのようなナノ粒子と、SHQとを含む化粧料が、顕著な美白効果を発揮することを見出し、本発明を完成した。 As a result of diligent research, the inventors of the present application have found that a cosmetic containing nanoparticles such as PLGA and SHQ exerts a remarkable whitening effect, and completed the present invention.

すなわち、本発明は、ナノ粒子と、塩化ステアリルジメチルベンジルアンモニウム−ハイドロキノン分子錯体とを含む美白化粧料組成物であって、前記ナノ粒子が、乳酸−グリコール酸共重合体ナノ粒子である、美白化粧料組成物を提供する。
That is, the present invention is a whitening cosmetic composition containing nanoparticles and a stearyldimethylbenzylammonium chloride-hydroquinone molecular complex , wherein the nanoparticles are lactic acid-glycolic acid copolymer nanoparticles. The composition is provided.

本発明により、優れた美白効果を発揮する新規な美白化粧料組成物が提供された。 INDUSTRIAL APPLICABILITY According to the present invention, a novel whitening cosmetic composition exhibiting an excellent whitening effect has been provided.

本発明の美白化粧料組成物中に必須成分として含まれるナノ粒子としては、PLGAナノ粒子、フラーレンナノ粒子及び白金コロイド粒子が好ましい。これらのうち、美白効果の観点から、PLGAナノ粒子が特に好ましい。これらのナノ粒子自体及びその製造方法は公知であり、市販もされているので、市販品を用いることができる。PLGA及びフラーレンは、ナノ粒子を形成してその内部に所望の物質を抱合することができ、DDSに用いられている。ナノ粒子の粒径は特に限定されず、通常、平均粒径が10nm〜1000nm程度、特に50nm〜400nm程度であるが、これに限定されるものではない。ナノ粒子の配合量は、特に限定されないが、組成物全量に対して通常、0.001質量%〜30質量%程度、好ましくは、0.05質量%〜5.0質量%程度、さらに好ましくは0.2質量%〜1.0質量%程度である。 As the nanoparticles contained as essential components in the whitening cosmetic composition of the present invention, PLGA nanoparticles, fullerene nanoparticles and platinum colloidal particles are preferable. Of these, PLGA nanoparticles are particularly preferable from the viewpoint of whitening effect. Since these nanoparticles themselves and their production methods are known and commercially available, commercially available products can be used. PLGA and fullerenes are used in DDS because they can form nanoparticles and conjugate desired substances within them. The particle size of the nanoparticles is not particularly limited, and the average particle size is usually about 10 nm to 1000 nm, particularly about 50 nm to 400 nm, but is not limited thereto. The blending amount of the nanoparticles is not particularly limited, but is usually about 0.001% by mass to 30% by mass, preferably about 0.05% by mass to 5.0% by mass, and more preferably 0.2% by mass to 1.0% by mass with respect to the total amount of the composition. It is about%.

本発明の美白化粧料組成物中に必須成分として含まれるSHQ自体及びその製造方法は公知であり、化粧料に含まれる美白成分としても公知のものである。SHQも市販されているので、市販品を用いることができる。SHQの配合量は、特に限定されないが、ナノ粒子100質量部に対して通常、1質量部〜10000質量部程度、好ましくは10質量部〜1000質量部程度、さらに好ましくは100質量部〜400質量部程度である。 SHQ itself contained as an essential ingredient in the whitening cosmetic composition of the present invention and a method for producing the same are known, and are also known as whitening ingredients contained in cosmetics. Since SHQ is also commercially available, a commercially available product can be used. The blending amount of SHQ is not particularly limited, but is usually about 1 part by mass to 10000 parts by mass, preferably about 10 parts by mass to 1000 parts by mass, and more preferably 100 parts by mass to 400 parts by mass with respect to 100 parts by mass of nanoparticles. It is about a part.

本発明の化粧料組成物は、上記各成分を溶媒中に含むものでよく、溶媒としては水が好ましい。溶媒が水の場合、化粧水の形態となる。化粧水の場合、各成分を水に入れ、ホモジナイズすることにより、本発明の化粧料を製造することができる。また、本発明の化粧料組成物は、化粧水の形態に限らず、周知の方法によりクリームやゲルの形態とすることもできる。クリームの形態にする場合、周知のとおり、モノステアリン酸グリセリル, モノステアリン酸ポリエチレングリコール、ポリソルベート、ポリオキシエチレン硬化ヒマシ油、ポリオキシエチレンラウリルエーテル類等の添加剤を、例えば0.10質量%〜20.00質量%程度添加することによりクリームの形態にすることができる。また、ゲルの形態にする場合、周知のとおり、カルボキシビニルポリマー、(アクリレーツ/アクリル酸アルキル )クロスポリマー、ポリアクリルアミド、ゼラチン、ヒドロキシエチルセルロース、キサンタンガム、ジラウロイルグルタミン酸リシンNa、アクリレーツクロスポリマー、ベントナイト類、ヘクトライト類、(アクリレーツ/イタコン酸ステアレス-20)コポリマー、ヒドロキシプロピルデンプンリン酸、ポリグルタミン酸Na、ポリビニルピロリドン、(ビニルピロリドン/VA)コポリマー、ステアロキシヒドロキシプロピルメチルセルロース、ポリビニルアルコール、シロキクラゲ多糖体等の添加剤を、例えば0.01質量%〜10.00質量%程度添加することによりゲルの形態にすることができる。 The cosmetic composition of the present invention may contain each of the above components in a solvent, and water is preferable as the solvent. When the solvent is water, it is in the form of a lotion. In the case of lotion, the cosmetic of the present invention can be produced by putting each component in water and homogenizing it. Further, the cosmetic composition of the present invention is not limited to the form of a lotion, and may be in the form of a cream or gel by a well-known method. In the form of cream, as is well known, additives such as glyceryl monostearate, polyethylene glycol monostearate, polysorbate, polyoxyethylene hydrogenated castor oil, and polyoxyethylene lauryl ethers are added, for example, from 0.10% by mass to 20.00% by mass. It can be made into a cream form by adding about%. In the case of gel form, as is well known, carboxyvinyl polymer, (acrylic acid / alkyl acrylate) crosspolymer, polyacrylamide, gelatin, hydroxyethyl cellulose, xanthan gum, lysine dilauroyl glutamate Na, acrylicyrrolid crosspolymer, bentonites, etc. , Hectrites, (Acrylate / steareth itaconate-20) copolymer, hydroxypropyl starch phosphate, Na polyglutamate, polyvinylpyrrolidone, (vinylpyrrolidone / VA) copolymer, stearoxyhydroxypropylmethylcellulose, polyvinyl alcohol, white jellyfish polysaccharide, etc. The gel can be formed by adding, for example, about 0.01% by mass to 10.00% by mass of the additive of.

本発明の化粧料組成物は、上記した必須成分に加え、化粧料に用いられている各種の添加剤をさらに含んでいてもよい。このような添加剤としては、抗酸化剤、抗菌剤、保湿剤、抗炎症剤、界面活性剤等を挙げることができるがこれらに限定されるものではない。抗酸化剤としては、アスコルビン酸およびその誘導体、プラセンタ、ハイドロキノンおよびその誘導体、トラネキサム酸、コウジ酸、トコフェロール、レモン果汁等を例示することができる。抗菌剤としては、パラベン類、フェノキシエタノール、ペンチレングリコール、オクタンジオール等を例示することができる。保湿剤としては、グリセリン、ブチレングリコール(BG)、ヒアルロン酸Na、セラミド類、コンドロイチン硫酸Na、コラーゲン、カンゾウ葉エキス、アマチャヅル葉エキス、ゲットウ葉エキス等を例示することができる。抗炎症剤としては、グリチルリチン酸ジカリウム、アラントイン、オウゴンエキス、オタネニンジンエキス、カミツレエキス、カンゾウフラボノイド等を例示することができる。界面活性剤としては、PEG水添ヒマシ油等を挙げることができる。 The cosmetic composition of the present invention may further contain various additives used in cosmetics in addition to the above-mentioned essential ingredients. Examples of such additives include, but are not limited to, antioxidants, antibacterial agents, moisturizers, anti-inflammatory agents, surfactants and the like. Examples of the antioxidant include ascorbic acid and its derivatives, placenta, hydroquinone and its derivatives, tranexamic acid, kojic acid, tocopherol, lemon juice and the like. Examples of the antibacterial agent include parabens, phenoxyethanol, pentylene glycol, octanediol and the like. Examples of the moisturizer include glycerin, butylene glycol (BG), sodium hyaluronate, ceramides, chondroitin sulfate Na, collagen, citrus leaf extract, Jiaogulan leaf extract, and getto leaf extract. Examples of the anti-inflammatory agent include dipotassium glycyrrhizinate, allantoin, ginseng extract, ginseng extract, chamomile extract, licorice flavonoid and the like. Examples of the surfactant include PEG hydrogenated castor oil and the like.

以下、本発明を実施例に基づき具体的に説明する。もっとも、本発明は下記実施例に限定されるものではない。 Hereinafter, the present invention will be specifically described based on examples. However, the present invention is not limited to the following examples.

実施例1〜3、比較例1、2
1. 化粧料組成物の調製
下記表1に示す組成の化粧水を調製した。表1に示す各成分を、表1に示す量だけ計り取り、精製水を加えて全量を100gとした。この際、精製水を適量加えた後にホモジナイズし、さらに精製水を加えて全量を100gとした。対照としては、精製水を用いた。なお、各成分としては市販品を用いた。PLGAの平均粒子径は88nm、フラーレンの平均粒子径は300nm、白金コロイド粒子の平均粒子径は250nmであった。
Examples 1 to 3, Comparative Examples 1 and 2
1. 1. Preparation of cosmetic composition A lotion having the composition shown in Table 1 below was prepared. Each component shown in Table 1 was weighed by the amount shown in Table 1, and purified water was added to make the total amount 100 g. At this time, an appropriate amount of purified water was added and then homogenized, and purified water was further added to bring the total amount to 100 g. Purified water was used as a control. Commercially available products were used as each component. The average particle size of PLGA was 88 nm, the average particle size of fullerenes was 300 nm, and the average particle size of platinum colloidal particles was 250 nm.

Figure 0006957289
*グリコール溶液:濃グリセリン10g + 1,3-BG 10g + PEG-60水添ヒマシ油 2g
Figure 0006957289
* Glycol solution: Concentrated glycerin 10g + 1,3-BG 10g + PEG-60 Hydrogenated castor oil 2g

2. 美白効果試験
美白効果の評価は、メラノサイト含有ヒト3次元培養表皮モデル(商品名ラボサイト メラノ・モデル、ジャパン・ティッシュ・エンジニアリング社製)を使用し、その取り扱い説明書に従って、メラニン生成量を測定することにより行った。具体的には次のとおりに行った。
2. Whitening effect test To evaluate the whitening effect, use a human three-dimensional cultured epidermis model containing melanocytes (trade name: Labsite Melano Model, manufactured by Japan Tissue Engineering), and measure the amount of melanin produced according to the instruction manual. I went by. Specifically, it was carried out as follows.

メラノサイト含有ヒト3次元培養表皮モデルに、上記各例の組成物を表2に示す量だけ加え、14日間培養した。陽性対照及び陰性対照は、各0.05mL添加した。培養した3次元培養表皮をマイクロチューブに回収し、緩衝液(1% SDS、0.05mmol/L EDTA、10 mmol/L Tris-HCl)150μLを加えて浸漬させた。これに、プロテアーゼK(5mg/mL)3μLを添加し、45℃で16時間処理し、さらに、プロテアーゼK(5mg/mL)3μLを添加し、45℃で4時間処理した。前記処理後、500mmol/L 炭酸ナトリウムを含有する30% 過酸化水素水25μLを添加し、80℃で30分反応させた。前記反応液を遠心分離(15,000rpm、10分)して、上清を回収した。前記上清について、波長405nmの吸光度(Abs.405nm)と波長570nmの吸光度(Abs.570nm)とを測定し、Abs.405nmからAbs.570nmを差し引いた。そして、別途作成した検量線から、ウェルあたりのメラニン量を算出した。また、生成メラニン量について、陰性対照における生成メラニン量を100%として、相対値を求めた。なお、同じ実験を3回行い、平均値をとった。結果を下記表2に示す。 To the melanocyte-containing human three-dimensional cultured epidermis model, the compositions of each of the above examples were added in the amounts shown in Table 2 and cultured for 14 days. 0.05 mL each of positive and negative controls was added. The cultured three-dimensional cultured epidermis was collected in a microtube, and 150 μL of a buffer solution (1% SDS, 0.05 mmol / L EDTA, 10 mmol / L Tris-HCl) was added and immersed. To this, 3 μL of proteinase K (5 mg / mL) was added and treated at 45 ° C. for 16 hours, and further 3 μL of proteinase K (5 mg / mL) was added and treated at 45 ° C. for 4 hours. After the above treatment, 25 μL of 30% hydrogen peroxide solution containing 500 mmol / L sodium carbonate was added, and the mixture was reacted at 80 ° C. for 30 minutes. The reaction solution was centrifuged (15,000 rpm, 10 minutes), and the supernatant was collected. With respect to the supernatant, the absorbance at a wavelength of 405 nm (Abs. 405 nm) and the absorbance at a wavelength of 570 nm (Abs. 570 nm) were measured, and Abs. From 405 nm to Abs. 570 nm was subtracted. Then, the amount of melanin per well was calculated from the calibration curve prepared separately. In addition, the relative value of the amount of melanin produced was determined with the amount of melanin produced in the negative control as 100%. The same experiment was performed three times, and the average value was taken. The results are shown in Table 2 below.

メラニン量(%)=〔Bs-Bb / Bn-Bb〕×100
Bs: 評価物質の吸光度(405nm-570nm)
Bn: 陽性対照(ビタミンE:)の吸光度(405nm-570nm)
Bb:陰性対象(ブランク):精製水(IPA単独)吸光度
Amount of melanin (%) = [Bs-Bb / Bn-Bb] x 100
Bs: Absorbance of the evaluation substance (405nm-570nm)
Bn: Absorbance of positive control (vitamin E :) (405nm-570nm)
Bb: Negative subject (blank): Purified water (IPA alone) Absorbance

また、メラノサイトの生存率も確認した。これは具体的には、MTT(3-(4,5-ジメチル-2-チアゾリル)-2,5-ジフェニルテトラゾリウムブロミド)試薬を使用して、前記取り扱い説明書に従って求めた。陰性対照の生細胞数を100%として、相対値を求めた。その結果、各例、各添加量とも、生存率は97%以上であり、細胞の死滅はほとんど起きていないことが確認された。 We also confirmed the survival rate of melanocytes. This was specifically determined using the MTT (3- (4,5-dimethyl-2-thiazolyl) -2,5-diphenyltetrazolium bromide) reagent and according to the instructions above. The relative value was calculated with the number of living cells of the negative control as 100%. As a result, it was confirmed that the survival rate was 97% or more in each case and each addition amount, and that almost no cell death occurred.

Figure 0006957289
Figure 0006957289

表2に示されるとおり、特に添加量0.5mLの結果に最もよく表されているように、本発明の組成物を0.5mL添加した場合には、メラニン生成量が41%〜51%にまで低減されるのに対し、ナノ粒子を含まずにSHQのみを含む比較例1や、公知の美白成分であるアスコルビン酸のみを含む比較例2では、メラニン生成量は77%又は84%にまでしか低減されておらず、本発明の組成物の顕著な美白効果が確認された。また、ナノ粒子がPLGAナノ粒子である場合に最も美白効果が高かった。 As shown in Table 2, especially when 0.5 mL of the composition of the present invention was added, the amount of melanin produced was reduced to 41% to 51%, as is best shown in the result of the addition amount of 0.5 mL. On the other hand, in Comparative Example 1 containing only SHQ without nanoparticles and Comparative Example 2 containing only ascorbic acid, which is a known whitening component, the amount of melanin produced was reduced to only 77% or 84%. However, a remarkable whitening effect of the composition of the present invention was confirmed. In addition, the whitening effect was highest when the nanoparticles were PLGA nanoparticles.

Claims (1)

ナノ粒子と、塩化ステアリルジメチルベンジルアンモニウム−ハイドロキノン分子錯体とを含む美白化粧料組成物であって、前記ナノ粒子が、乳酸−グリコール酸共重合体ナノ粒子である、美白化粧料組成物A whitening cosmetic composition comprising nanoparticles and a stearyldimethylbenzylammonium chloride-hydroquinone molecular complex , wherein the nanoparticles are lactic acid-glycolic acid copolymer nanoparticles .
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