JP7411327B2 - 天然抽出物を含有する組成物、ならびに皮膚および毛髪に対するその使用 - Google Patents
天然抽出物を含有する組成物、ならびに皮膚および毛髪に対するその使用 Download PDFInfo
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- JP7411327B2 JP7411327B2 JP2018526632A JP2018526632A JP7411327B2 JP 7411327 B2 JP7411327 B2 JP 7411327B2 JP 2018526632 A JP2018526632 A JP 2018526632A JP 2018526632 A JP2018526632 A JP 2018526632A JP 7411327 B2 JP7411327 B2 JP 7411327B2
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Description
白髪化(白髪症)、または色素生成および毛幹内沈着の欠乏は、多くの文化においてきわめて望ましくない、老化の明らかな兆候である。白髪化は、いくつかの内的および外的要因の相互反応から生じる、複雑な現象である。内的要因としては、遺伝子にプログラムされているプロセスが挙げられ、このプロセスにより、若白髪、遺伝性疾患、および自然老化プロセスが引き起こされ得る。外的要因としては、環境的要因(例えば風、高温、タバコの煙、化学物質、UV照射など)、栄養効果、薬物効果、および情緒的ストレスが挙げられる。これらの要素すべてが、毛髪色素形成の不能に寄与する分子および細胞プロセスを誘導する。
本開示は、天然生成物(複数可)、例えば、ボタニカル抽出物、藻類抽出物、酵母抽出物、菌類抽出物もしくは微生物抽出物、またはそのような抽出物の分画(複数可)、またはそれらの組合せ(複数可)(まとめて「天然抽出物」と定義される)であるが、それらに限定されない天然生成物(複数可)を含む天然抽出物(複数可)の生成物を(例えば、それを必要とする哺乳動物、例としてヒトに)局所送達するための組成物を特徴とする。一例では、本開示の天然抽出物は、(1)活性な、非変性カタラーゼおよび/またはグルタチオンペルオキシダーゼを含有する、あるいは(2)カタラーゼ様活性(例えば、過酸化水素を分解する、または排除する)を有する、あるいは(3)カタラーゼ強化活性(例えば、遺伝子発現、タンパク質翻訳または過酸化水素分解もしくは排除の増進を引き起こす他の活性を向上させる)を有する、あるいは(4)カタラーゼ安定化活性、またはそのような活性の1つもしくは複数の組合せ(まとめて「カタラーゼ関連活性」もしくは「カタラーゼ様活性」と定義される)を有する。別の実施形態では、本開示の天然供給源(例えばボタニカル、植物、藻類、酵母、菌類または微生物)は、L-メチオニンを用いて成長させる、もしくはそれを強化する、もしくはそれを補充する、もしくはそれを生成するように設計する、もしくはそれと組み合わせることができる、または天然抽出物そのものをL-メチオニンと組み合わせることができる。
詳細な説明
本開示は、ある天然抽出物は、過酸化水素の排除にきわめて有効であるという認識に関し、したがって、これらは、皮膚および毛髪の自然な色を保つ、または、白髪化の出現もしくは脱色した皮膚病変を防止する、もしくは遅くする、もしくは低減する、もしくは逆行させる、または、皮膚、頭皮、毛髪および爪の老化の一般的兆候ならびに高齢者の皮膚の特定の兆候を低減するために使用できる。
化粧品または医薬担体
有用な組成物は、1つもしくは複数の防腐剤、または1つもしくは複数の抗酸化剤、または1つもしくは複数のキレート剤、またはそれらの組合せを含み得る安定化系を含み得る。防腐剤は、微生物の分解を実質的に防止するために有用である。防腐剤の例は、フェノキシエタノール、パラベンおよび天然の防腐剤を含むが、それらに限定されず、これらは、当業者に公知である。他の防腐剤の例は、以下、「Cosmetic Handbook」と呼ぶ、International Cosmetic Ingredient Dictionary and Handbook、WenningerおよびMcEwen編(CTFA、第7版、1997年)の1654~55頁に見出すことができる。組成物は、重量に対して約0.01%から約20%の防腐剤を含み得る(より好ましくは、場合により、重量に対して約0.5%から約5%)。微生物の混入は、ガンマ線照射、もしくは電子ビーム照射、もしくはX線照射など、精密濾過、または、本開示に記載されている特定の活性の排除を引き起こさない他の標準手順(例えば短時間の加熱処理)によっても排除することができる。
追加の化粧活性剤
天然抽出物を含有する組成物は、他の化粧活性剤(例えば、合成化合物(複数可)、または天然供給源から単離される化合物(複数可)、または組織に対する化粧効果もしくは治療効果を有する化合物の混合物を含有する天然抽出物(複数可))も含有し得る。本明細書に記載されている有用な組成物は、天然生成物(複数可)に加えて、皮膚、毛髪および爪に有益な他の作用剤も含有し得る。そのような作用剤の例は、抗炎症剤(例えば副腎皮質ステロイド、NSAIDまたは抗炎症活性を有するボタニカル抽出物、例えばアロエベラ)、かゆみ止め剤、局所用鎮痛剤、抗酸化剤(例えばビタミンCおよび誘導体、ビタミンEおよび誘導体、抗酸化活性を有するボタニカル抽出物)、カタラーゼ様またはSOD様活性(例えばサレムMN化合物、例としてEUK作用剤のファミリー)を有する作用剤、表皮、皮膚および小胞再生剤ならびに皮膚向上剤、毛髪および爪組織再生剤(例えばレチノイド、レチノイド誘導体、レチノール、レチナール、アルファヒドロキシ酸、コエンザイム-Q、増殖因子などを含む)、抗生物質および抗微生物剤、抗真菌剤、抗酵母剤、抗寄生生物剤、免疫系向上剤、フケ防止剤およびてかり防止剤(例えばミコナゾール、ケトコナゾール、エルビオール、イトラコナゾール、コールタールなどの作用剤を含む)、洗剤、界面活性剤、保湿剤、栄養剤、ビタミン、ミネラル、エネルギー増強剤、毛髪または爪の成長促進剤、毛髪の成長遅延剤、皮膚コンディショニング剤、臭気防止剤(例えば臭気マスキング剤またはpH変化剤)、デオドラント、制汗剤、着色剤、色素、色マスキング剤、色素生成向上剤または色素送達向上剤(例えばペプチド、PAR-2活性化物質、MC1Rリガンド、アルファMSHおよびその模倣物質など)、色素生成向上剤または色素生成阻害剤、メチオニンスルホキシド還元酵素活性に影響を与える作用剤(例えば、メチオニンの酸化を防止できるL-メチオニン)、ならびに皮膚、頭皮、毛髪または爪のウエルネスおよび美容を強化する、当業者に公知の他の作用剤を含むが、それらに限定されない。
形態
本開示の組成物は、化粧品としてまたは医薬として許容される形態および担体、例えば溶液、懸濁液、エマルション(マイクロエマルションおよびナノエマルションを含む)、ローション、クリーム、ゲル、スティック、スプレー、軟膏、クレンジング液、ウォッシュ、固形バー、シャンプー、毛髪コンディショナー、ネイルポリッシュ、ネイルストレングスナー、ペースト、フォーム、粉末、ムース、シェービングクリーム、シェービングゲル、ワイプ、パッチ、ヒドロゲル、フィルム形成生成物、マスク、液滴、粘膜接着剤などと使用できるが、それらに限定されない。
組成物および方法
本開示は、哺乳動物の白髪化プロセスを低減する方法であって、頭皮または他の望ましい無毛ではない皮膚領域に、安全かつ有効量の本開示の組成物を適用するステップを含む、方法を特徴とする。適用の頻度は、処置される領域、末端使用者の年齢、健康状態、毛髪のタイプおよび皮膚のタイプ、処置の持続時間および性質、用いられる特定の組成物、化粧品としてまたは医薬として許容される、利用される特定の担体、ならびに同様の要因によって異なると考えられる。例えば、いくつかの例において、適用は、定期的であってよいが、他の例では適用は1日1回または2回であってよい。
実施例1
この試験は、試験剤の過酸化水素崩壊活性を評価した。カタラーゼアッセイキットは、Cayman Chemical Co.(Ann Arbor、MI)から得た。このアッセイは、Purpald(4-アミノ-3-ヒドラジノ-5-メルカプト-1,2,4-トリアゾール)を比色アッセイにおける色原体として使用して、過酸化水素排除活性(例えばカタラーゼ活性)を測定する。試験は、過酸化水素の存在下でのメタノールとの反応に基づき、試料に存在する有効な活性に比例する、540nmでの光学密度(OD)の変化を伴う。色原体として使用されるPurpaldは、生成されたホルムアルデヒドと二環式複素環を形成し、酸化の際に無色から紫色に変化する。
実施例2
この試験は、培養した通常のヒトケラチノサイトの内因性の細胞の過酸化水素分解活性および排除活性に対する試験材料の効果を評価した。Purpald(4-アミノ-3-ヒドラジノ-5-メルカプト-1,2,4-トリアゾール)を比色アッセイにおける色原体として使用して過酸化水素分解活性を測定するために、処置した細胞のタンパク質溶解物を使用した。試験は、過酸化水素の存在下でのメタノールとの反応に基づき、試料に存在する有効な活性に比例する、540nmでの光学密度(OD)の変化を伴っていた。色原体として使用されるPurpaldは、生成されたホルムアルデヒドと二環式複素環を形成し、酸化の際に無色から紫色に変化する。
実施例3
この試験の目的は、過酸化水素による傷害に反応した、培養ヒト表皮のケラチノサイトにおける、試験材料の細胞内における抗酸化活性を評価することであった。細胞を、試験材料で処理し、H2DCFDAで標識し、その後、過酸化水素に曝露した。相対蛍光は、細胞内における活性酸素(ROS)に対する指標として測定した。試験は、未処理および過酸化水素のみで処理した試料と比較すると、細胞内の有効な抗酸化活性に比例した蛍光の変化を伴っていた。
実施例4
天然抽出物ゲル製剤の調製。天然抽出物は、水またはリン酸塩緩衝液または他の水溶液中で懸濁される天然供給源の液体試料(懸濁液)として、または試料粉末として調製して、例えば10~100mg/mL(1~10% w/v)保存懸濁液を作ることができる。懸濁液は、例えば1~10分間混合される(例えばボルテックスされる)べきであり、次いで、天然の材料は、例えば4℃にてサイズ縮小して、細胞を崩壊させるべきである(例えば加圧破断、ジェットミル、ボールミル、または、例えば30~50%の出力での、例えば10分間の音波処理により)。次いで、大きい粒子は、分離されるべきであり(例えば、500~1000rpmで、4℃にて10分間の遠心分離により)、沈殿物は廃棄されるべきである。上澄みは、製剤中に直接使用できる、または、さらなるサイズ選択を施すことができる(例えば、懸濁液または溶液は、0.2ミクロン孔径フィルターを使用して濾過できる)。生じた天然物質の均一化溶液は、製剤中に直接使用できる、またはさらに乾燥させ(例えば凍結乾燥、噴霧乾燥またはフリーズドライさせ)、製剤中に乾燥粉末として使用することができる。
天然抽出物の水中油製剤の調製。天然抽出物は、実施例4と同様にして調製できる。水中油エマルションの2つの実施例は、表5で提示されている。このタイプの製剤を調製するために、脂質相の原料は、約50~85℃にて組み合わせられ、混合されるべきであり、次いで、約40~60℃に冷却されるべきである。別の容器では、増粘剤は、水性の天然抽出物または水もしくは水溶液中で再構成される粉末の天然抽出物と、ゆっくり組み合わせることができる。例えば、水性相の残りを約10分間混合した後で、原料を添加し、混合し、次いで、脂質相の可能な限りのほぼ最低温度に加熱できる。次いで、2つの相を組み合わせて、例えば約10分間混合し、室温に冷却することができる。追加の活性剤は、両方の相の中で、または混合の後で組み合わせることができる。本開示に記載されている生物学的活性は、過剰な熱が望ましい活性を低下させ得るので、モニターされるべきである。
天然抽出物の油中水製剤の調製。天然抽出物は、実施例4と同様にして調製できる。油中水製剤の2つの実施例は、表6で提示されている。このタイプの製剤を調製するために、皮膚軟化剤(例えばミネラル油)を溶融させてよい。次いで、他の油相原料を添加してよく、混合物を例えば約75℃に加熱して、均一な混合を可能にすることができる。水性相の原料は、別々に混合でき、液体油相の可能な限りの最低温度に温められるべきであり(一方、天然抽出物の生物学的活性の保持が確認される)、次いで、2つの混合物は、凝結するまで撹拌させてよい。追加の活性剤は、両方の相の中で、または混合の後で組み合わせることができる。
Claims (4)
- 白髪化を低減するための組成物であって、ポルフィリディウムバイオマスの水性抽出物、および医薬としてまたは化粧品として許容される担体を含み、頭皮または無毛ではない皮膚に適用され、
前記水性抽出物が、(i)0.05%(w/v)で少なくとも2nmol/分/mlの過酸化水素分解もしくは排除活性、または(ii)0.5%(w/v)で、内因性ケラチノサイト過酸化水素分解もしくは排除活性を少なくとも50%向上させる活性を有し、
前記組成物が、不溶性ポルフィリディウム材料を含まない、組成物。 - 高齢者の皮膚の状態を改善するための組成物であって、ポルフィリディウムバイオマスの水性抽出物、および医薬としてまたは化粧品として許容される担体を含み、65歳を超える対象の皮膚に適用され、
前記水性抽出物が、(i)0.05%(w/v)で少なくとも2nmol/分/mlの過酸化水素分解活性、または(ii)0.5%(w/v)で、内因性ケラチノサイトの過酸化水素分解および排除活性を、少なくとも50%向上させる活性を有し、
前記組成物が、不溶性ポルフィリディウム材料を含まない、組成物。 - 対象において、低色素性皮膚病変の出現を低減するための組成物であって、ポルフィリディウムバイオマスの水性抽出物、および医薬としてまたは化粧品として許容される担体を含む組成物を、それを必要とする対象の皮膚に適用され、
前記水性抽出物が、(i)0.05%(w/v)で少なくとも2nmol/分/mlの過酸化水素分解活性、または(ii)0.5%(w/v)で、内因性ケラチノサイト過酸化水素分解および排除活性を少なくとも50%向上させる活性を有し、
前記組成物が、不溶性ポルフィリディウム材料を含まない、組成物。 - 前記組成物が、L-メチオニンをさらに含む、請求項1から3のいずれか一項に記載の組成物。
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JP2018534337A (ja) | 2018-11-22 |
US20170135925A1 (en) | 2017-05-18 |
KR20180081602A (ko) | 2018-07-16 |
EP3377084A4 (en) | 2019-08-07 |
CA3005842A1 (en) | 2017-05-26 |
EA201891183A1 (ru) | 2018-12-28 |
AU2022204824A1 (en) | 2022-07-28 |
US20200297608A1 (en) | 2020-09-24 |
US10206861B2 (en) | 2019-02-19 |
WO2017087177A3 (en) | 2017-07-13 |
AU2016357227A1 (en) | 2018-05-31 |
WO2017087177A2 (en) | 2017-05-26 |
CN108472322A (zh) | 2018-08-31 |
US10675233B2 (en) | 2020-06-09 |
US20170135949A1 (en) | 2017-05-18 |
EP3377084A2 (en) | 2018-09-26 |
HK1258675A1 (zh) | 2019-11-15 |
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