CN117462447A - 包含硫糖铝的皮肤再生用化妆品组合物 - Google Patents
包含硫糖铝的皮肤再生用化妆品组合物 Download PDFInfo
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- CN117462447A CN117462447A CN202310936329.8A CN202310936329A CN117462447A CN 117462447 A CN117462447 A CN 117462447A CN 202310936329 A CN202310936329 A CN 202310936329A CN 117462447 A CN117462447 A CN 117462447A
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- Prior art keywords
- skin
- hyaluronic acid
- levan
- sucralfate
- composition
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Abstract
本发明涉及包含(i)硫糖铝、(ii)果聚糖及(iii)透明质酸、其盐或其衍生物的皮肤再生用化妆品组合物。在利用本发明的皮肤再生用化妆品组合物的情况下,增加因照射紫外线而减少的层粘连蛋白332(层粘连蛋白5)及XVII型胶原蛋白的蛋白质表达,由此具有坚固地结合皮肤结构的功效,增加过氧化物酶体增殖物激活受体γ辅激活因子‑1α基因表达并呈现出优秀的伤口愈合效果,因此可有效地用于皮肤损伤恢复,增加丝聚蛋白的表达,由此具有强化皮肤屏障的效果,减少白细胞介素‑6蛋白质的表达,由此可有效地用于皮肤舒缓。
Description
技术领域
本发明涉及包含硫糖铝(sucralfate)的皮肤再生用化妆品组合物。
背景技术
皮肤作为人体中直接与外部环境接触的身体器官,具有保护人体内部的功能,且是由多种功能的细胞和具有与此相匹配的物性的物质构成的复杂的器官。皮肤可大体分为表皮(epidermis)、真皮(dermis)及皮下脂肪(hypodermis)等三种。在真皮层中结合有具有弹性的固体物质(纤维)和具有粘性的液体物质,使得皮肤可以维持固有弹性。通常,随着年龄的增长,皮肤将会暴露于紫外线、污染、压力等环境,从而会给皮肤带来功能降低和萎缩性变化,且会发生皮肤细胞数量减少或皮肤的厚度减少的现象。
已知皮肤皱纹的增加和弹性减少是由于存在于真皮内的细胞外基质(extracellular matrix,ECM)的变形及减少而发生,且影响存在于表皮与真皮之间的基底膜的结构及功能变化或皮肤老化。据报道,老年人的皮肤中的皮肤基底膜(basementmembrane)已损伤及破坏,在20多岁的年轻人的皮肤中,暴露于紫外线的脸部等皮肤中也有损伤的基底膜。皮肤基底膜的结构及功能变化是因为如下原因,分解皮肤基底膜的结构成分的纤溶酶(plasmin)和基质金属蛋白酶(MMP,matrix metalloproteinase)等蛋白质分解酶的活性因紫外线而增加并破坏基底膜结构成分,随着年龄的增长,作为基底膜结构成分的层粘连蛋白(laminin)332(5)、胶原蛋白(collagen)IV、胶原蛋白XVII、胶原蛋白VII等的表达也会减少(Mechanisms of Ageing and Development.156,14-16,2016)。
因这种皮肤基底膜结构成分的分解及生成减少而导致的皮肤基底膜的损伤被认为是皮肤中的皱纹形成、弹性降低等皮肤老化的直接原因中的一种。在基底膜结构成分中的层粘连蛋白332(5)起到通过坚固地固定表皮和真皮来向表皮与真皮之间赋予安全性的必要作用,与30多岁相比,在60多岁的皮肤中其表达显著减少。并且,据报道,在受损的皮肤中,随着层粘连蛋白332(5)的生成,损伤部位的再生得到促进,在人工皮肤模型中,当从外部给药层粘连蛋白332(5)时,皮肤基底膜的组织(assembly)得到促进(Journal ofDermatological Science.25,S51-59,2000)。
据报道,作为其他因子的XVII型胶原蛋白(collagen type XVII)也作为表皮与真皮的稳定附着所必要的半桥粒结构成分(hemidesmosome component),当缺乏XVII型胶原蛋白时,呈现出表皮玻璃症、皮肤萎缩症、表皮干细胞群(epidermal stem cellpopulation)减少(Journal of Investigative Dermatology.129,2288-2295,2009)。
在皮肤真皮的情况下,已知产能效率高的氧化磷酸化过程最为重要。但是,因外部环境压力,线粒体脱氧核糖核酸(DNA)损伤将会累积,当以此合成的复合物(complex)蛋白质结构发生变形时,无法形成用于产能的线粒体膜电位差,氧化磷酸化过程无法正常进行,从而三磷酸腺苷(ATP,adenosine triphosphate)生成将会减少,同时,电子泄漏将会增加,从而活性氧类将会增加。由此,当向皮肤细胞的供给并不顺畅时,细胞为了抵消这些能量而经过非线粒体机制的解糖过程。尤其,据报道,占据皮肤真皮的90%的胶原蛋白(collagen)糖化反应生成物(glycation product)容易积累,且增加细胞内氧化压力并减少真皮的收缩能,从而带来皮肤弹性减少、皱纹生成、皮肤颜色变化(J.Soc.Cosmet.ScientistsKorea,38(3),237-245,2012)。
另一方面,主要在微生物的生成物中发现,且最近也在多种草木和树木的根及大麦或小麦等植物发现的左聚糖(levan)作为以β(2→6)连接的果糖(fructose)聚合物,具有数十万个果糖残基(fructose residue),通过多个微生物(枯草芽孢杆菌(Bacillussubtilis)、多粘芽孢杆菌(Bacillus polymyxa)、左气杆菌(Aerobacter levanicum)、链球菌属(Streeptococcus sp.)、假单胞菌属(Pseudomonas sp.)、棒状杆菌(Corynebacteriumlaevaniformans)、运动发酵单胞菌(Zymomonas mobilis)等),以蔗糖(sucrose)为基质来生成。左聚糖在皮肤中的保湿效果优秀且对细胞完全没有毒性,从而适合作为化妆品组合物原料来使用。
现有技术文献
专利文献
专利文献1:EP 02714705 B1
发明内容
本发明人为了发现可以预防或改善因皮肤的结构及性能变化而引发的皱纹形成、弹性降低、萎缩、干燥、皮肤损伤等的化妆品组合物而努力进行了研究。结果,查明了与包含各单一成分或两种成分的组合物相比,包含(i)硫糖铝(sucralfate)、(ii)果聚糖(fructan)及(iii)透明质酸(hyaluronic acid)、其盐或其衍生物的化妆品组合物具有显著的伤口愈合效果、使因紫外线(UVB)而失调的(dysregulated)基因的转录或蛋白质的表达恢复的效果、真皮表皮连接部(DEJ,dermal-epidermal junction)强化效果及皮肤再生效果,由此完成了本发明。
因此,本发明的目的在于,提供包含i)硫糖铝(sucralfate)、(ii)果聚糖(fructan)及(iii)透明质酸(hyaluronic acid)、其盐或其衍生物的皮肤再生用化妆品组合物。
本发明的再一目的在于,提供包含(i)硫糖铝(sucralfate)、(ii)果聚糖(fructan)及(iii)透明质酸(hyaluronic acid)、其盐或其衍生物的皮肤弹性改善用化妆品组合物。
本发明的另一目的在于,提供包含(i)硫糖铝(sucralfate)、(ii)果聚糖(fructan)及(iii)透明质酸(hyaluronic acid)、其盐或其衍生物的皱纹改善用化妆品组合物。
本发明的还有一目的在于,提供包含(i)硫糖铝(sucralfate)、(ii)果聚糖(fructan)及(iii)透明质酸(hyaluronic acid)、其盐或其衍生物的皮肤保湿用化妆品组合物。
本发明的又一目的在于,提供包含(i)硫糖铝(sucralfate)、(ii)果聚糖(fructan)及(iii)透明质酸(hyaluronic acid)、其盐或其衍生物的皮肤损伤改善用化妆品组合物。
根据本发明一实施方式,本发明提供包含(i)硫糖铝(sucralfate)、(ii)果聚糖(fructan)及(iii)透明质酸(hyaluronic acid)、其盐或其衍生物的皮肤再生用化妆品组合物。
并且,本发明提供组合物在皮肤再生中的用途,上述组合物包含(i)硫糖铝(sucralfate)、(ii)果聚糖(fructan)及(iii)透明质酸(hyaluronic acid)、其盐或其衍生物。
本发明人为了发现可以预防或改善因皮肤的结构及性能变化而引发的皱纹形成、弹性降低、萎缩、干燥、皮肤损伤等的化妆品组合物而努力进行了研究。结果,查明了与包含各单一成分或两种成分的组合物相比,包含(i)硫糖铝(sucralfate)、(ii)果聚糖(fructan)及(iii)透明质酸(hyaluronic acid)、其盐或其衍生物的化妆品组合物具有显著的伤口愈合效果、使因紫外线而失调的基因的转录或蛋白质的表达恢复的效果、真皮表皮连接部(DEJ)强化效果及皮肤再生效果。
本发明的皮肤再生用化妆品组合物具有增加层粘连蛋白332(5),XVII型胶原蛋白及丝聚蛋白(filaggrin)的表达的功效,引导过氧化物酶体增殖物激活受体γ辅激活因子-1α(PGC-1α)的表达和细胞的生长,由此具有使细胞活性化的功能。并且,减少白细胞介素-6(IL-6)的蛋白质的表达,由此具有皮肤舒缓功能。
在本说明书中,术语“化妆品组合物”意味着为了皮肤的清洁、美化、维持健康或促进健康而使用的组合物。
在本说明书中,术语“硫糖铝”为通过以下化学式1表示的化合物,是指蔗糖八硫酸盐(sucrose octasulphate)的碱性铝盐(salt)。
化学式1
在本说明书中,术语“果聚糖”是指至少一个果糖基-果糖结合构成大多数结合的化合物。并且,本发明的果聚糖包括果糖(fructose)通过β-(2,1)-结合和/或β-(2,6)-结合连接的多糖类和在一个葡萄糖分子结合有至少两个果糖残基的寡糖或多糖类。在本说明书中,果聚糖的链长度为至少3个、至少5个、至少10个、至少15个、至少20个、至少25个、至少30个、至少40个或至少50个。在本说明书中,果聚糖可以为菊粉(inulin)、左聚糖(levan)、梯牧草果聚糖(phlein)或裸麦果糖胶(graminin),但并不局限于此。
在本发明的一具体例中,上述果聚糖包括直链和/或侧链。
在本发明的再一具体例中,上述果聚糖可以为变形的果聚糖。例如,变形的果聚糖包括醚化果聚糖、酯化果聚糖、二羟基菊粉等,但并不局限于此。
在本发明的另一具体例中,上述果聚糖为葡萄糖基果糖基单位为2个至20个的低聚果糖。
在本发明的又一具体例中,上述果聚糖为包含β-(2,1)侧链的β-(2,6)果糖聚合物。
在本发明的一实例中,上述果聚糖为2000Da至100000kDa。
在本发明的一实例中,相对于上述组合物,上述硫糖铝包含0.01%(w/v)至1.0%(w/v)。
在本发明的另一实例中,相对于上述组合物,上述硫糖铝包含0.05%(w/v)至0.5%(w/v)、0.05%(w/v)至0.4%(w/v)、0.05%(w/v)至0.3%(w/v)、0.05%(w/v)至0.2%(w/v)、0.05%(w/v)至0.1%(w/v)、0.1%(w/v)至0.5%(w/v)、0.1%(w/v)至0.4%(w/v)、0.1%(w/v)至0.3%(w/v)或0.1%(w/v)至0.2%(w/v)。
在本发明的一实例中,在上述组合物中,(i)上述硫糖铝、(ii)果聚糖及(iii)透明质酸(hyaluronic acid)、其盐或其衍生物的重量比为1:1:1至1:5:0.1。
在本发明的再一实例中,上述重量比为1:1:1至1:5:0.1、1:1:1至1:5:0.2、1:1:1至1:5:0.5、1:1:1至1:5:1、1:1:1至1:4:0.1、1:1:1至1:4:0.2,1:1:1至1:4:0.5、1:1:1至1:4:1、1:1:1至1:3:0.1、1:1:1至1:3:0.2、1:1:1至1:3:0.5、1:1:1至1:3:1、1:1:1至1:2:0.1、1:1:1至1:2:0.2、1:1:1至1:2:0.5或1:1:1至1:2:1。在本发明的另一实例中,上述重量比为1:5:0.1至1:5:0.5。在本发明的还有一实例中,上述重量比为1:5:0.2。
在本发明的一实例中,上述果聚糖为左聚糖(levan)、菊粉、梯牧草果聚糖、裸麦果糖胶或这些的组合。
在本发明的一实例中,上述果聚糖为2000Da至100000kDa。
在本说明数中,术语“左聚糖(levan)”是指具有β-2,1-连接的侧链的β-2,6-连接的果聚糖。
上述左聚糖可从细菌和/或植物生产。上述左聚糖可以为2000Da至33000Da。上述左聚糖可以为2000kDa至100000kDa。
上述细菌为选自由枯草芽孢杆菌、多粘芽孢杆菌、左气杆菌、链球菌属、假单胞菌属、棒状杆菌以及运动发酵单胞菌组成的组中的一种以上,但并不局限于此。
在本发明的一实例中,上述透明质酸的盐或衍生物为乙酰化透明质酸钠(sodiumacetylated hyaluronate)、透明质酸钠(sodium hyaluronate)、透明质酸钾(potassiumhyaluronate)、水解透明质酸(hydrolyzed hyaluronic acid)、水解透明质酸钠(hydrolyzed sodium hyaluronate)、透明质酸钠交联聚合物(sodium hyaluronatecrosspolymer)、羟丙基三甲基氯化铵透明质酸(hydroxypropyltrimonium hyaluronate)、寡聚透明质酸(oligo hyaluronic acid)或这些的组合。
在本说明书中,术语“乙酰化透明质酸钠(sodium acetylated hyaluronate)”是指透明质酸钠的羟基被乙酰基取代的衍生物,可以被缩写成sodium acetylated HA。
本领域已知与透明质酸相比,上述乙酰化透明质酸钠在皮肤中呈现出显著的保湿效果。
在本发明的一实例中,上述透明质酸(hyaluronic acid)、其盐或其衍生物的分子量为5000Da至1500000Da。
在本发明的一实例中,上述组合物增加选自由层粘连蛋白332(层粘连蛋白5)、XVII型胶原蛋白、过氧化物酶体增殖物激活受体γ辅激活因子-1α(Peroxisomeproliferator-activated receptor gamma coactivator 1-alpha)及丝聚蛋白组成的组中的一种以上蛋白质或编码其的基因的表达或转录。
在本说明书中,术语“层粘连蛋白”是指作为所有基底膜(basement membrane)的重要结构成分的细胞外糖蛋白(extracellular glycoprotein),以由α、β及γ链(chain)形成的异三聚体(heterotrimer)αβγ组装,在哺乳动物中至少存在16个同源异构体(isoform)。
在本说明书中,术语“层粘连蛋白332”是指由之前也被公知为层粘连蛋白5的α3、β3及γ2链形成的异三聚体蛋白质,是作为将表皮附着在真皮来提供针对皮肤完整性(skinintegrity)和外部机械力量的阻抗性的基底膜区域的真皮表皮连接部(dermal-epidermaljunction,DEJ)的必要结构成分。层粘连蛋白332(层粘连蛋白5)在通过与作为两个受体的α6β4或α3β1整联蛋白(integrin)的相互作用来在基底膜接合(adhesion)上皮组织(epithelial tissue)过程中起到重要作用。
在本说明书中,术语“XVII型胶原蛋白”是指也被公知为BP180(180kDa bullouspemphigoid antigen)或BPAG2的II型跨膜胶原蛋白(type II transmembrane collagen),在皮肤、粘膜及眼睛的上皮半桥粒中表达。
在本说明书中,术语“丝聚蛋白(FLG)”作为引起角蛋白中间体(keratinintermediate)的凝聚和压缩的微丝凝聚蛋白(filament-aggregating protein),是指皮肤屏障(skin barrier)的发达和维持所必要的结构蛋白质。
在本说明书中,术语“过氧化物酶体增殖物激活受体γ辅激活因子-1α(Peroxisome proliferator-activated receptor gamma coactivator1-alpha)”是指可以提高线粒体的生物合成、呼吸能力、氧化磷酸化及脂肪酸β-氧化的转录辅激活因子(transcriptional coactivator)。
在本发明的一实例中,上述组合物减少白细胞介素-6(Interleukin6)的蛋白质或编码其的基因的表达或转录。
在本说明书中,术语“白细胞介素-6”是指具有对炎症免疫反应及造血的多效性(pleiotropic effect)的水溶性介导因子(mediator),起到促炎细胞因子(pro-inflammatory cytokine)和抗炎肌因子(anti-inflammatory myokine)的作用。
根据本发明的再一实施例,本发明提供包含(i)硫糖铝(sucralfate)、(ii)果聚糖(fructan)及(iii)透明质酸(hyaluronic acid)、其盐或其衍生物的皮肤弹性改善用化妆品组合物。
并且,本发明提供组合物在改善皮肤弹性中的用途,上述组合物包含(i)硫糖铝(sucralfate)、(ii)果聚糖(fructan)及(iii)透明质酸(hyaluronic acid)、其盐或其衍生物。
根据本发明的另一实施方式,本发明提供包含(i)硫糖铝(sucralfate)、(ii)果聚糖(fructan)及(iii)透明质酸(hyaluronic acid)、其盐或其衍生物的皱纹改善用化妆品组合物。
并且,本发明提供组合物在改善皱纹中的用途,上述组合物包含(i)硫糖铝(sucralfate)、(ii)果聚糖(fructan)及(iii)透明质酸(hyaluronic acid)、其盐或其衍生物。
根据本发明的还有一实施方式,本发明提供包含(i)硫糖铝(sucralfate)、(ii)果聚糖(fructan)及(iii)透明质酸(hyaluronic acid)、其盐或其衍生物的皮肤保湿用化妆品组合物。
并且,本发明提供组合物在皮肤保湿中的用途,上述组合物包含(i)硫糖铝(sucralfate)、(ii)果聚糖(fructan)及(iii)透明质酸(hyaluronic acid)、其盐或其衍生物。
根据本发明的又一实施方式,本发明提供包含(i)硫糖铝(sucralfate)、(ii)果聚糖(fructan)及(iii)透明质酸(hyaluronic acid)、其盐或其衍生物的皮肤损伤改善用化妆品组合物。
并且,本发明提供组合物在改善皮肤损伤中的用途,上述组合物包含(i)硫糖铝(sucralfate)、(ii)果聚糖(fructan)及(iii)透明质酸(hyaluronic acid)、其盐或其衍生物。
在本发明的一实例中,上述皮肤损伤因紫外线而起。
在本发明的又一实例中,上述皮肤损伤因外部刺激而起。在本发明的又一实例中,上述外部刺激可以是暴露于污染、微尘或超微尘。在本发明的又一实例中,上述皮肤损伤因压力或老化而起。
在本说明书中,术语“改善”意味着维持或促进皮肤健康的所有行为。
在本发明的一实例中,本发明的化妆品组合物可以包含作为有效成分的(i)硫糖铝、(ii)果聚糖及(iii)透明质酸、其盐或其衍生物和通常用于化妆品组合物的成分,例如,还可包含抗氧化剂、稳定剂、增溶剂、维生素、颜料及香料等通常的辅助剂以及载体。
上述载体可以为一元醇(乙醇或丙醇)、多元醇(甘油、1,3-丁二醇或丙二醇)、高级脂肪酸(棕榈酸或亚麻酸)、油脂(小麦胚芽油、山茶油、荷荷巴油、橄榄油、角鲨烷、葵花籽油、澳洲坚果花生油、鳄梨油、大豆氢化卵磷脂或脂肪酸甘油酯)等,但并不局限于。并且,根据需要,可以追加添加表面活性剂、杀菌剂、抗氧化剂、紫外线吸收剂、抗炎剂和清凉剂。
上述表面活性剂可以为聚氧乙烯、氢化蓖麻油、聚氧乙烯、油基醚、聚氧乙烯单油酸酯、聚氧乙烯、单硬脂酸甘油酯、脱水山梨糖醇单硬脂酸酯、聚氧乙烯单油酸酯、脱水山梨糖醇、蔗糖脂肪酸酯、单月桂酸六甘油酯、聚氧乙烯还原羊毛脂、聚乙氧基化脂肪醇(POE)、甘油焦谷氨酸、异硬脂酸、二酯、N-乙酰谷氨酰胺和异硬脂酸酯等,但并不局限于此。
上述杀菌剂可以为氢硫酚、三氯生、葡萄糖酸氯己定、苯氧乙醇、间苯二酚、异丙基甲基苯酚、甘菊环(azulene)、水杨酸、吡啶酮锌等,但并不局限于此。
上述抗氧化剂只要是选自由丁基羟基茴香醚、没食子酸、没食子酸丙酯及异抗坏血酸组成的组成的一种以上就可以使用。
上述紫外线吸收剂可以为二羟基二苯甲酮等二苯甲酮类、黑色素、对氨基苯甲酸乙酯、对二甲氨基苯甲酸2-乙基己酯、西诺西特、对甲氧基肉桂酸2-乙基己酯、2-(2-羟基-5-甲基苯基)苯并三唑、尿刊酸及金属氧化物微粒子,但并不局限于此。
上述抗炎剂可以为甘草酸二钾、尿囊素等,清凉剂可以为红辣椒酊剂、1-薄荷醇等,但并不局限于此。
在本发明的一实例中,上述化妆品组合物可被制成选自溶液、外用药膏、凝胶、乳霜、泡沫、乳液、化妆水、皮肤软化剂、爽肤水、收敛剂、润肤乳、保湿乳液、营养乳液、按摩霜、营养霜、保湿霜、护手霜、润肤露、营养化妆水、柔肤水、面膜、柔顺水、乳液、底妆、精华液、营养精华液、安瓶、头发安瓶、头皮护理、生发剂、护发素、头发护理品、润发乳、洗发水、冲洗型护发素、护发素洗发水、养发洗发水、发胶、发蜡、发胶、染料、肥皂、洗面奶、洁面泡沫、洁面乳、清洁霜、沐浴添加剂、沐浴露、防晒霜、太阳油、悬浮液、乳剂、膏体、粉末、肥皂、含有表面活性剂的洁面乳、油、粉底、粉底、乳液粉底、蜡粉底、贴片和喷雾剂组成的组中的剂型,但并不局限于此。
本发明的化妆品组合物可追加包含选自由水溶性维生素、有用维生素、高分子肽、高分子多糖、鞘脂、海藻提取物组成的组中的成分。
水溶性维生素只要是可配合化妆品组合物的水溶性维生素就能使用任何物质,优选地,在本发明中可以使用的水溶性维生素包括维生素B1、维生素B2、维生素B6、吡哆醇、盐酸吡哆醇、维生素B12、泛酸、烟酸、烟酰胺、叶酸、维生素C、维生素H等及其盐(盐酸硫胺素、抗坏血酸钠等)或衍生物(2-磷酸抗坏血酸钠盐、2-磷酸抗坏血酸镁盐等)。水溶性维生素可通过一般的微生物转化法、微生物培养物纯化法、酶法或化学合成法等方法来制成。
有用维生素只要是可配合化妆品组合物的有用维生素就能使用任何物质,优选地,在本发明中可以使用的水溶性维生素包括维生素A、胡萝卜素、维生素D2、维生素D3、维生素E(d1-α生育酚、d-α生育酚、d-α生育酚)及其衍生物(抗坏血酸棕榈酸酯、抗坏血酸硬脂酸酯、抗坏血酸棕榈酸酯、dl-α生育酚醋酸酯、dl-α生育酚烟酸酯、维生素E、DL-泛醇、D-泛醇、泛乙基醚等)。有用维生素可通过一般的微生物转化法、微生物培养物纯化法、酶法或化学合成法等方法来制成。
高分子肽只要是可配合化妆品组合物的高分子肽就能使用任何物质,优选地,可以为胶原蛋白、水解胶原蛋白、明胶、弹性蛋白、水解弹性蛋白、角蛋白等。高分子肽可通过一般的微生物培养物纯化法、酶法或化学合成法等方法来制成或通常由猪或牛的真皮、蚕丝纤维等天然物质纯化后使用。
高分子多糖只要是可配合化妆品组合物的高分子多糖就能使用任何物质,优选地,可以为羟乙基纤维素、黄原胶、透明质酸钠、硫酸软骨素或其盐(钠盐等)等。例如,硫酸软骨素或其盐等可通常从哺乳动物或鱼类纯化后使用。
鞘脂只要是可配合化妆品组合物的鞘脂就能使用任何物质,优选地,可以为神经酰胺、植物鞘氨醇、鞘糖脂等。鞘脂通常通过常规方法从哺乳动物、鱼类、贝类、酵母或植物纯化或通过化学合成形成。
海藻提取物只要是可配合化妆品组合物的海藻提取物就能使用任何物质,优选地,可以为褐藻提取物、红藻提取物、绿藻提取物等,并且,在本发明中使用的海藻提取物包括从这些海藻提取物中纯化的卡拉胶、精氨酸、海藻酸钠、海藻酸钾等。海藻提取物通过常规方法从海藻中纯化而成。
在本发明的化妆品组合物还可以配合通常配合在化妆品组合物的其他成分。
此外能够添加的配合成分可以为油脂成分、保湿剂、润肤剂、表面活性剂、有机和无机颜料、有机粉末、紫外线吸收剂、防腐剂、杀菌剂、抗氧化剂、植物提取物、pH调节剂、醇类、颜料、香料、血液循环促进剂、清凉剂、止汗剂、纯化水等。
作为油脂成分,可以为酯油、烃油、硅油、氟油、动物油、植物油等。
酯油可以为三2-乙基己酸甘油酯、2-乙基己酸鲸蜡酯、肉豆蔻酸异丙酯、肉豆蔻酸丁酯、棕榈酸异丙酯、硬脂酸乙酯、棕榈酸辛酯、异硬脂酸异鲸蜡酯、硬脂酸丁酯、亚油酸乙酯、亚油酸异丙酯、油酸乙酯、肉豆蔻酸异鲸蜡酯、肉豆蔻酸异硬脂酯、棕榈酸异硬脂酯、肉豆蔻酸辛基十二烷基酯、异硬脂酸异鲸蜡酯、癸二酸二乙酯、己二酸二异丙酯、新戊酸异烷基酯、三(辛基、癸酸)甘油、三羟甲基丙烷三2-乙基己酸酯、三羟甲基丙烷三异硬脂酸酯、四2-乙基己酸酯五醇、辛酸鲸蜡酯、月桂酸癸酯、月桂酸己酯、肉豆蔻酸癸酯、硬脂酸肉豆蔻酯、肉豆蔻酸鲸蜡酯、硬脂酸硬脂酯、油酸癸酯、蓖麻油酸鲸蜡酯、月桂酸异硬脂酯、肉豆蔻酸异十三烷基酯,棕榈酸辛酯、辛酯硬脂酸酯、硬脂酸异鲸蜡酯、油酸异癸酯、油酸辛基十二烷基酯、亚油酸辛基十二烷基酯、异硬脂酸异丙酯、2-乙基己酸鲸蜡硬脂酯、2-乙基己酸硬脂酯、异硬脂酸己酯、乙二醇二辛酸酯、乙二醇二油酸酯、丙二醇二癸酸酯、二(辛基、癸酸)丙二醇、丙二醇二辛酸酯、新戊二醇二癸酸酯、新戊基二辛酸酯乙二醇、甘油三辛酸酯、甘油三十一酸酯、甘油三异棕榈酸酯、甘油三异硬脂酸酯、辛基十二烷基酯新戊酸酯、辛酸异硬脂酯、异壬酸辛酯、新癸酸己酯癸基、新癸酸辛基十二烷基酯、异硬脂酸异鲸蜡酯、异硬脂酸异硬脂酯、异硬脂酸辛基癸酯、聚甘油油酸酯、聚甘油异硬脂酸酯、柠檬酸三异鲸蜡酯、柠檬酸三异烷基酯、柠檬酸三异辛酯、乳酸月桂酯、乳酸肉豆蔻酯、乳酸鲸蜡酯、乳酸辛基癸酯、柠檬酸三乙酯、柠檬酸乙酰基三乙酯、柠檬酸乙酰基三丁酯、柠檬酸三辛酯、二苹果酸异硬脂酸酯、羟基硬脂酸2-乙基己酯、琥珀酸二2-乙基己酯、己二酸二异丁酯、二异丙基癸二酸酯、癸二酸二辛酯、胆固醇硬脂酸酯、胆甾醇异硬脂酸酯、胆甾醇羟基硬脂酸酯、胆甾醇油酸酯、二氢胆甾醇油酸酯、植醇异硬脂酸酯、植醇油酸酯、12-硬脂酰羟基硬脂酸异鲸蜡酯、12-硬脂酰羟基硬脂酰硬脂酸酯、12-硬脂酰羟基硬脂酸酯异硬脂酸酯等。
烃油可以为角鲨烯、液体石蜡、α-烯烃低聚物、异链烷烃、纯地蜡、石蜡、液体异链烷烃、聚丁烯、微晶蜡、凡士林等。
硅油可以为聚甲基硅氧烷、甲基苯基硅氧烷、甲基环聚硅氧烷、八甲基聚硅氧烷、十甲基聚硅氧烷、十二甲基环硅氧烷、二甲基硅氧烷/甲基十六烷氧基硅氧烷共聚物、二甲基硅氧烷/甲基硬脂氧基硅氧烷共聚物、烷基改性硅油、氨基改性硅油等。
氟油可以为全氟聚醚等。
动物油或植物油可以为鳄梨油、杏仁油、橄榄油、芝麻油、米糠油、鸟花油、大豆油、玉米油、菜籽油、杏仁油、棕榈仁油、棕榈油、蓖麻油、葵花籽油、葡萄籽油、棉籽油、椰子油、库库伊坚果油、小麦胚芽油、米胚芽油、乳木果油、月见草油、马克达米亚坚果油、绣线菊油、蛋黄油、牛油、马油、貂油、橙酒椰油、荷荷芭油、小烛树油发蜡、卡纳瓦发蜡、液体羊毛脂、硬化蓖麻油等。
保湿剂可以为水溶性低分子保湿剂、脂溶性分子保湿剂、水溶性高分子、脂溶性高分子等。
水溶性低分子保湿剂可以为丝氨酸、谷氨酰胺、山梨糖醇、甘露醇、吡咯烷酮甲酸钠、甘油、丙二醇、1,3-丁二醇、乙二醇、聚乙二醇B(聚合度n=2以上)、聚丙二醇(聚合度n=2以上)、聚甘油B(聚合度n=2以上)、乳酸、乳酸盐等。
脂溶性分子保湿剂可以为胆固醇、胆固醇酯等。
水溶性高分子可以为羧乙烯基聚合物、聚天冬氨酸酯、黄芪胶、黄原胶、甲基纤维素、羟甲基纤维素、羟乙基纤维素、羟丙基纤维素、羧甲基纤维素、水溶性甲壳质、壳聚糖、糊精等。
脂溶性高分子可以为聚乙烯吡咯烷酮/二十碳烯共聚物、聚乙烯吡咯烷酮/十六碳烯共聚物、硝基纤维素、糊精脂肪酸酯、聚合物有机硅等。
润肤剂可以为长链酰基谷氨酸胆固醇酯、羟基硬脂酸胆固醇酯、12-羟基硬脂酸、硬脂酸、松香酸、羊毛脂脂肪酸胆固醇酯等。
表面活性剂可以为非离子表面活性剂、阴离子表面活性剂、阳离子表面活性剂、两性表面活性剂等。
非离子表面活性剂可以为自乳化单硬脂酸甘油酯、丙二醇脂肪酸酯、甘油脂肪酸酯、聚甘油脂肪酸酯、脱水山梨糖醇脂肪酸酯、POE(聚氧乙烯)脱水山梨糖醇脂肪酸酯、POE脱水山梨糖醇脂肪酸酯、POE甘油脂肪酸酯、POE烷基酯、POE脂肪酸酯、POE氢化蓖麻油、POE蓖麻油、POE/POP(聚氧乙烯/聚氧丙烯)共聚物、POE/POP烷基醚、聚醚改性有机硅、月桂酸链烷醇酰胺、烷基氧化胺、氢化大豆磷脂等。
阴离子表面活性剂可以为脂肪酸皂、α-酰基磺酸盐、烷基磺酸盐、烷基烯丙基磺酸盐、烷基萘磺酸盐、烷基硫酸盐、POE烷基醚硫酸盐、烷基酰胺硫酸盐、烷基磷酸盐、POE烷基磷酸三盐、烷基酰胺磷酸盐、烷酰基烷基牛磺酸盐、N-酰基氨基酸盐、POE烷基醚羧酸盐、烷基磺基琥珀酸盐、烷基磺基乙酸钠、酰化水解胶原肽盐、全氟烷基磷酸酯等。
阳离子表面活性剂可以为烷基三甲基氯化铵、硬脂基三甲基氯化铵、硬脂基三甲基溴化铵、鲸蜡硬脂基三甲基氯化铵、二硬脂基二甲基氯化铵、硬脂基二甲基苄基氯化铵、二十二烷基三甲基溴化铵、苯扎氯铵、二硬脂酸乙氨基乙酰胺、硬脂酸二甲氨基丙酰胺、羊毛脂衍生物季铵盐等。
两性表面活性剂可以为羧基甜菜碱型、酰胺甜菜碱型、磺基甜菜碱型、羟基磺基甜菜碱型、酰胺磺基甜菜碱型、磷酸甜菜碱型、氨基羧酸盐型、咪唑啉衍生物型、酰胺胺型等。
有机和无机颜料可以为硅酸、无水硅酸、硅酸镁、滑石、绢云母、云母、高岭土、孟加拉土、粘土、膨润土、镀钛云母、氯氧化铋、氧化锆、氧化镁、氧化锌、氧化钛、氧化铝、硫酸钙、硫酸钡、硫酸镁、碳酸钙、碳酸镁、氧化铁、群青、氧化铬、氢氧化铬、炉甘石及其复合物等无机颜料;聚酰胺、聚酯、聚丙烯、聚苯乙烯、聚氨酯、乙烯基树脂、尿素树脂、酚醛树脂、氟树脂、硅树脂、丙烯酸树脂、三聚氰胺树脂、环氧树脂、聚碳酸酯树脂、二乙烯基苯/苯乙烯共聚物、丝粉、纤维素、CI颜料黄、CI颜料橙等有机颜料及这些的无机颜料和有机颜料的复合颜料等。
有机粉末可以为硬脂酸钙等金属皂;鲸蜡酸锌钠、月桂酸锌和月桂酸钙等烷基磷酸金属盐;N-月桂酰-β-丙氨酸钙、N-月桂酰-β-丙氨酸锌、N-月桂酰甘氨酸钙等酰基氨基酸的多价金属盐;N-月桂酰牛磺酸钙、N-棕榈酰牛磺酸钙等酰胺磺酸的多价金属盐;N-ε-月桂酰-L-赖氨酸、N-ε-棕榈酰基嗪、N-α-谷酰鸟氨酸、N-α-月桂酰精氨酸、N-α-硬化牛肉脂肪酸酰基精氨酸等N-酰基碱性氨基酸;N-月桂酰甘氨酰甘氨酸等;α-氨基辛酸、α-氨基月桂酸等α-氨基脂肪酸;聚乙烯、聚丙烯、尼龙、聚甲基丙烯酸甲酯、聚苯乙烯、二乙烯基苯-苯乙烯共聚物、四氟乙烯等。
紫外线吸收剂可以为对氨基苯甲酸、对氨基苯甲酸乙酯、对氨基苯甲酸戊酯、对氨基苯甲酸辛酯、乙二醇水杨酸酯、水杨酸苯酯、水杨酸辛酯、水杨酸苄酯、水杨酸丁苯酯、水杨酸高薄荷酯、肉桂酸苄酯、参数毒肉桂酸-2-乙氧基乙基、对甲氧基肉桂酸辛酯、二对甲氧基肉桂酸单-2-乙基己烷甘油酯、对甲氧基肉桂酸异丙酯、二异丙基-二异丙基肉桂酸酯混合物、尿刊酸、尿刊酸乙酯、羟基甲氧基二苯甲酮、羟基甲氧基二苯甲酮磺酸及其盐、二羟基甲氧基二苯甲酮、二羟基甲氧基二苯甲酮二磺酸钠、二羟基二苯甲酮、四羟基二苯甲酮、4-叔丁基-4'-甲氧基二苯甲酰甲烷、2,4,6-三苯胺基-p-(碳-2'-乙基己基-1'-氧基)-1,3,5-三嗪、2-(2-羟基-5-甲基苯基)苯并三唑等。
杀菌剂可以为扁柏酚、三氯生、三氯羟基二苯醚、葡萄糖酸氯己定、苯氧乙醇、间苯二酚、异丙基甲基苯酚、甘菊环、水杨酸、锌绿硫酮、苯扎氯铵、光敏剂301号、单硝基钠、十一碳烯酸等。
抗氧化剂可以为丁基羟基苯甲醚、没食子酸丙酯、山梨酸等。
pH调节剂可以为柠檬酸、柠檬酸钠、苹果酸、苹果酸钠、富马酸、富马酸钠、琥珀酸、琥珀酸钠、氢氧化钠、磷酸氢二钠等。
醇类可以为鲸蜡醇等高级醇。
并且,此外能够添加的配合成分并不局限于此,并且,上述任何成分也可以在不损害本发明的目的及效果的范围内配合,相对于总重量,优选地,可以配合0.01重量百分比~5重量百分比,更优选地,可配合0.01重量百分比~3重量百分比。
本发明的化妆品组合物可以为溶液、乳液、粘稠混合物等形状。
包含在本发明的化妆品组合物的成分作为有效成分,除上述提取物之外,可以包括化妆品通常利用的成分,例如,稳定剂、增溶剂、维生素、颜料及香料等通常的辅助剂及载体。
在本发明的化妆品组合物剂型为糊剂、霜剂或凝胶的情况下,作为载体成分,可以利用动物纤维、植物纤维、蜡、石蜡、淀粉、曲棘胶、纤维素衍生物、聚乙二醇、有机硅、膨润土、二氧化硅、滑石粉或氧化锌等。
在本发明的化妆品组合物剂型为粉末或喷雾剂的情况下,作为载体成分,可以利用乳糖、滑石粉、二氧化硅、氢氧化铝、硅酸钙或聚酰胺粉末,尤其,在喷雾剂的情况下,可追加包括氯氟烃、丙烷/丁烷或二甲醚等推进剂。
在本发明的化妆品组合物剂型为溶液或乳液的情况下,作为载体成分,可利用溶剂、溶剂化剂或乳化剂,例如,水、乙醇、异丙醇、碳酸乙酯、乙酸乙酯、苯甲醇、苯甲酸苄酯、丙二醇、1,3-丁二醇油、甘油脂肪族酯、聚乙二醇或脱水山梨糖醇脂肪酸酯。
在本发明的化妆品组合物剂型为悬浮液的情况下,作为载体成分,可利用水、乙醇或丙二醇等液体稀释剂、乙氧基化异硬脂醇、聚氧乙烯山梨糖醇酯和聚氧乙烯山梨糖醇酯等悬浮剂、微晶纤维素、偏氢氧化铝、膨润土、琼脂或曲棘胶等。
在本发明的化妆品制剂为含有表面活性剂的清洁剂的情况下,作为载体成分,可利用脂肪醇硫酸盐、脂肪醇醚硫酸盐、磺基琥珀酸单酯、羟乙基磺酸盐、咪唑啉鎓衍生物、甲基牛磺酸盐、肌氨酸盐、脂肪酸酰胺醚硫酸盐、烷基酰氨基甜菜碱、脂肪醇、脂肪酸甘油酯、脂肪酸二乙醇酰胺、植物油、亚麻酸衍生物或乙氧基化甘油脂肪酸酯等。
在本发明的一实例中,与仅作为有效成分包含硫糖铝的组合物及包含两个成分的组合物(硫糖铝及果聚糖及硫糖铝及乙酰化透明质酸钠)相比,本发明的皮肤再生用化妆品组合物的特征在于,增加作为坚固地固定表皮和真皮来向皮肤赋予稳定性的基底膜的结构成分的层粘连蛋白332(层粘连蛋白5)的表达,由此,可以促进因暴露于紫外线等而导致的皮肤损伤部位的再生,增加作为表皮与真皮的稳定附着必要的半桥粒的结构成分的XVII型胶原蛋白的表达,增加作为调节线粒体的氧化磷酸化的转录共同活性因子的过氧化物酶体增殖物激活受体γ辅激活因子-1α的基因转录水平,增加作为增加皮肤屏障的发达和维持所必要的结构蛋白质的丝聚蛋白的表达,减少因紫外线而增加的白细胞介素-6的蛋白质表达等皮肤弹性改善效果、皱纹改善效果、皮肤保湿效果、皮肤屏障强化效果或皮肤损伤改善效果优秀,本发明的化妆品组合物的协同效果得到认证。
简单说明本发明的特征及优点如下:
(a)本发明提供包含(i)硫糖铝(sucralfate)、(ii)果聚糖(fructan)及(iii)透明质酸(hyaluronic acid)、其盐或其衍生物的皮肤再生用化妆品组合物。
(b)本发明提供包含(i)硫糖铝(sucralfate)、(ii)果聚糖(fructan)及(iii)透明质酸(hyaluronic acid)、其盐或其衍生物的皮肤弹性改善用化妆品组合物。
(c)本发明提供包含(i)硫糖铝(sucralfate)、(ii)果聚糖(fructan)及(iii)透明质酸(hyaluronic acid)、其盐或其衍生物的皱纹改善用化妆品组合物。
(d)本发明提供包含(i)硫糖铝(sucralfate)、(ii)果聚糖(fructan)及(iii)透明质酸(hyaluronic acid)、其盐或其衍生物的皮肤保湿用化妆品组合物。
(e)本发明提供包含(i)硫糖铝(sucralfate)、(ii)果聚糖(fructan)及(iii)透明质酸(hyaluronic acid)、其盐或其衍生物的皮肤损伤改善用化妆品组合物。
(f)在利用本发明的皮肤再生用化妆品组合物的情况下,增加因紫外线照射而减少的层粘连蛋白332(层粘连蛋白5)及XVII型胶原蛋白的蛋白质表达,由此具有坚固地结合皮肤结构的功效,增加过氧化物酶体增殖物激活受体γ辅激活因子-1α基因表达并呈现出优秀的伤口愈合(伤口愈合)效果,因此可有效地用于皮肤损伤恢复,增加丝聚蛋白的表达,由此具有强化皮肤屏障的效果,减少白细胞介素-6蛋白质的表达,由此可有效地用于皮肤舒缓。
附图说明
图1示出在成纤维细胞刮擦后处理比较例1至比较例3及实施例1的组合物之后确认伤口愈合效果的结果。
图2a示出向角质形成细胞(A431 cell)照射(irradiation)紫外线之后分别处理比较例1至比较例3及实施例1的组合物后,确认层粘连蛋白5及XVII型胶原蛋白的蛋白质表达水平的结果。
图2b示出基于图2a的蛋白质印迹结果来表示对于β-肌动蛋白(β-actin)的层粘连蛋白5及XVII型胶原蛋白的蛋白质表达比例的直方图。
图3示出向成纤维细胞照射紫外线之后分别处理比较例1至比较例3及实施例1的组合物之后,确认过氧化物酶体增殖物激活受体γ辅激活因子-1α基因的信使核糖核酸水平的结果。
图4示出向角质形成细胞(HaCaT cell)照射紫外线之后分别处理比较例1至比较例3及实施例1的组合物之后,确认白细胞介素-6蛋白质表达水平的结果。
具体实施方式
以下,通过实施例,更详细说明本发明。这些实施例仅用于更加具体说明本发明,根据本发明的主旨,本发明的范围并不局限于这些实施例对本发明所属技术领域的普通技术人员来说是显而易见的。
在整个说明书中,除非另有提及,否则为了表示特定物质的浓度而使用的“%”如下,固体/固体为(重量/重量)%,固体/液体为(重量/体积)%,液体/液体为(体积/体积)%。
实施例
准备例:组合物的制备
本发明所使用的对照组、比较例1至比较例3及实施例1的组成如以下表1准备。在表1中,HA为hyaluronic acid的缩写。以下,表1中记载的各个结构成分将纯化水用作载体,根据后述的实验例进行适当的稀释来使用。
表1
实验例1:伤口愈合(Wound healing)效果评价
在本实验例中测定了上述比较例1至比较例3和实施例1的细胞再生能力。
在24孔板(well plate)接种人类成纤维细胞(Fibroblast)并培养之后,利用SPLScarTM Scratcher来刮擦(scratch)以单一层(monolayer)培养的细胞来留下伤口并更换培养基。之后,以使比较例1至比较例3及实施例1的最终浓度达到0.05%(v/v)的方式分别在培养基进行处理并培养。将一天之后用显微镜(Leica)拍摄照片的结果呈现在图1中。
如图1所示,其结果,可以确认与比较例1至比较例3相比,本发明的实施例1处理组的细胞再生能力更为优秀。
实验例2:真皮表皮连接部强化评价
在本实验例中测定了上述比较例1至比较例3和实施例1的真皮表皮连接部强化功效。
接种作为角质形成细胞(keratinocyte)的细胞株的A431细胞并培养一天之后,在照射紫外线50mJ/cm2之后,更换无血清(serum free)培养基,以使比较例1至比较例3及实施例1的最终浓度达到0.1%(v/v)的方式在培养基进行处理并培养。以Pro-prepTM(iNtRON)收集细胞并根据制造商的方法分离蛋白质。将所分离的蛋白质定量之后,进行聚丙烯酰胺凝胶(SDS-PAGE)电泳并利用iBlot2干式转印系统(iBlot2Dry Blotting system)进行了转印(transfer)。之后,处理对层粘连蛋白332(5)(Santa Cruz(圣克鲁斯))、XVII型胶原蛋白(Thermo Fisher Scientific(赛默飞世尔科技))及β-肌动蛋白(Santa Cruz)的第一抗体之后进行了一天的反应。接着,处理小鼠辣根过氧化物酶(HRP,horseradish peroxidase)及兔辣根过氧化物酶(rabbit HRP(Bio-Rad(伯乐)))第二抗体并进行反应之后,使用AttoII化学发光成像仪(Chemi Doc)(ATTO(爱拓),Japan(日本))来实施蛋白质检测。其结果呈现在以下表2和图2a及图2b中。
表2
如表2、图2a及图2b所示,确认了在未经任何处理的对照组中,当将相对于β-肌动蛋白的层粘连蛋白5及XVII型胶原蛋白的蛋白质表达率以100%为基准时,在紫外线照射组中,层粘连蛋白5及XVII型胶原蛋白的蛋白质表达率分别减少成27.5%及40.8%。因照射紫外线而减少的层粘连蛋白5和XVII型胶原蛋白的蛋白质表达率在比较例1至比较例3中均得到了增加。
尤其,因照射紫外线而减少的层粘连蛋白5和XVII型胶原蛋白的蛋白质表达通过实施例1处理了而均显著增加,这是无法从比较例1至比较例3预期的程度,包含硫糖铝、果聚糖及乙酰化透明质酸钠的实施例1的组合物发挥出协同效果。
实验例3:皮肤再生(Skin revitalizing)评价
在本实验例中测定了上述比较例1至比较例3和实施例1的皮肤细胞活力或线粒体生物合成功效。
接种成纤维细胞(Fibroblast)并培养一天之后,照射紫外线,以使比较例1至比较例3及实施例1的最终浓度达到0.05%(v/v)的方式在培养基进行处理并培养。以QIAzolTMLysis Reagent(Qiagen(凯杰))收集细胞并根据制造商的方法分离了核糖核酸(RNA)。将所分离的核糖核酸定量之后合成互补脱氧核糖核酸(cDNA)来实施了实时聚合酶链反应(Real-Time PCR)。对于过氧化物酶体增殖物激活受体γ辅激活因子-1α及磷酸甘油醛脱氢酶(GAPDH)的引物将由CosmoGenetech(科斯莫基因科技)公司合成并使用,其序列呈现在以下表3中。实时聚合酶链反应结果呈现在以下表4和图3中。
表3
表4
区分 | PGC-1α基因表达率(%) |
对照组(未处理组) | 100.0 |
紫外线照射组 | 37.7 |
紫外线+实施例1 | 79.1 |
紫外线+比较例1 | 49.6 |
紫外线+比较例2 | 60.2 |
紫外线+比较例3 | 48.2 |
如表4和图3所示,确认与细胞活力有关的过氧化物酶体增殖物激活受体γ辅激活因子-1α的信使核糖核酸水平的结果,在未经任何处理的对照组中,当将相对于磷酸甘油醛脱氢酶的过氧化物酶体增殖物激活受体γ辅激活因子-1α的信使核糖核酸水平以为100%时,与对照组相比,在紫外线照射组中,过氧化物酶体增殖物激活受体γ辅激活因子-1α的信使核糖核酸(PGC-1αmRNA)水平大幅度减少成37.7%。在比较例1至比较例3中,因照射紫外线而大幅度减少的过氧化物酶体增殖物激活受体γ辅激活因子-1α的信使核糖核酸水平增加成48.2%至60.2%。
尤其,在实施例1中,过氧化物酶体增殖物激活受体γ辅激活因子-1α的信使核糖核酸水平显著增加成79.1%,这是无法从比较例1至比较例3的结果预期的,从而可以引导线粒体的生物合成(biogenesis)。
实验例4:保湿评价
在本实验例中测定了上述比较例1至比较例3和实施例1的皮肤保湿功效。
接种人表皮角质化细胞(HEKn cell)(Human Epidermal Keratinocytes,neonatal)并培养一天之后,以使比较例1至比较例3及实施例1的最终浓度达到0.1%(v/v)的方式在细胞进行处理并培养。以QIAzolTM Lysis Reagent(Qiagen)收集细胞并根据制造商的方法分离了核糖核酸。将所分离的核糖核酸定量后合成互补脱氧核糖核酸并为了确认丝聚蛋白的信使核糖核酸水平而实施了实时聚合酶链反应。相对于丝聚蛋白及β-肌动蛋白的引物将由CosmoGenetech公司合成并使用,其序列呈现在以下表5中。实时聚合酶链反应结果呈现在以下表6中。
表5
表6
区分 | 丝聚蛋白基因表达率(%) |
对照组(未处理组) | 100.0 |
实施例1 | 172.4 |
比较例1 | 121.0 |
比较例2 | 115.0 |
比较例3 | 138.1 |
如表6所示,确认已知作为在皮肤保湿中起到作用的代表性蛋白质的丝聚蛋白的信使核糖核酸水平的结果,与对照组相比,在比较例1至比较例3中,丝聚蛋白的信使核糖核酸水平均增加,与比较例1至比较例3相比,在实施例1中,其值显著增加。
如无法从处理比较例1至比较例3的情况预期,在处理实施例1的情况下,在丝聚蛋白的信使核糖核酸水平显著增加方面,与单独处理各个成分或处理两个成分的情况相比,本发明人员单独处理包含硫糖铝、果聚糖及乙酰化透明质酸钠的实施例1的组合物发挥出协同效果。
实验例5:皮肤舒缓评价
在本实验例中测定了上述比较例1至比较例3和实施例1的皮肤舒缓功效。
接种人永生化角质形成细胞(HaCaT cell)并培养一天之后,照射紫外线30mJ/cm2。更换无血清培养基,以使比较例1至比较例3及实施例1的最终浓度达到0.1%(v/v)的方式在细胞进行处理并培养2天。以Pro-prepTM(iNtRON)收集细胞并根据制造商的方法分离了蛋白质。将所分离的蛋白质定量之后进行聚丙烯酰胺凝胶电泳,利用iBlot2干式转印系统进行了转印(transfer)。之后,处理对白细胞介素-6(Santa Cruz)及磷酸甘油醛脱氢酶(Santa Cruz)的第一抗体后进行了一天的反应。接着,处理小鼠辣根过氧化物酶及兔辣根过氧化物酶(Bio-Rad)第二抗体并进行反应之后,使用Atto II化学发光成像仪(ATTO,Japan)来实施蛋白质检测。其结果呈现在以下表7和图4中。
表7
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如表7所示,在各个试样中确认的结果,在紫外线照射组中,当将相对于磷酸甘油醛脱氢酶的白细胞介素-6的蛋白质表达比例以100%为基准时,相比于对照组,在紫外线照射组中,白细胞介素-6蛋白质表达比例显著增加。在处理比较例1至比较例3的情况下,以照射紫外线而增加的白细胞介素-6蛋白质表达减少成75.0%至92.4%,在处理实施例1的情况下,因照射紫外线而增加的白细胞介素-6的表达显著减少成55.1%。
因照射上述紫外线而增加的白细胞介素-6的蛋白质表达通过包含硫糖铝、果聚糖及酰化透明质酸钠的实施例1的组合物显著减少的效果是无法从单独包含硫糖铝的比较例1、包含硫糖铝及果聚糖的比较例2及包含硫糖铝及乙酰化透明质酸钠的比较例3中所呈现的通过照射紫外线而增加的白细胞介素-6的减少的表达效果预期的协同效果。
制剂例
另一方面,以下记述了包含本发明的硫糖铝的皮肤再生用化妆品组合物的制剂例。只是,以下的制剂例仅用于具体说明本发明的使用例,而并非将本发明的保护范围限定在以下的制剂例,这对本发明所属技术领域的普通技术人员来说是显而易见的。
化妆品制剂例1:护肤水
将以达到2.0%(w/w)的方式溶解实施例1的物质作为原料,通过以下表8的组成如下制备护肤水。向纯化水依次投入甘油、丁二醇、丙二醇、防腐剂并搅拌溶解来制备混合液。将聚氧乙烯硬化蓖麻油加热到60℃左右并溶解之后,投入香料并溶解之后投入到上述混合液。最后,投入实施例1的2.0%水溶液、乙醇、三乙醇胺、色素并充分搅拌。
表8
化妆品制剂例2:营养乳液
将以达到2.0%(w/w)的方式溶解实施例1的物质作为原料,通过如下表9所示的组成如下制备了营养乳液。混合搅拌丙二醇、羟基聚合物、防腐剂、纯化水并加热到80℃至85℃之间并投入到制备部后使乳化机进行工作,将蜜蜡、聚山梨酯60、倍半油酸山梨坦、液体石蜡、山梨醇硬脂酸酯、亲油型单硬脂酸甘油、硬脂酸、硬脂酸甘油酯/PEG-400硬脂酸酯、三乙醇胺加热到80℃至85℃之间溶解后进行乳化。当完成乳化时,利用搅拌机进行搅拌并冷却到50℃之后,投入香料并冷却到45℃之后投入色素,在35℃的温度下投入实施例1的2.0%(w/w)水溶液并冷却到25℃。
表9
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化妆品制剂例3:面霜
将以达到2.0%(w/w)的方式溶解实施例1的物质作为原料,通过如下表10的组成如下制备了营养面霜(总100g)。混合搅拌羟基乙烯聚合物、丁二醇、甘油、纯化水并加热到80℃至85℃之间并投入到制备部之后,使乳化机进行工作,将硬脂酸、十六醇、单硬脂酸甘油酯、聚氧乙烯山梨醇单硬脂酸酯、倍半油酸山梨坦、单硬脂酸甘油酯/硬脂酸甘油脂/聚氧乙烯硬脂酸酯、发蜡、液体石蜡、辛癸酸甘油酯加热到80℃至85℃之间并溶解之后,投入三乙醇胺并进行搅拌并投入到制备部来进行乳化。当完成乳化时,利用搅拌机来进行搅拌并冷却到35℃,投入实施例1的2.0%(w/w)水溶液并冷却至25℃。
表10
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Claims (13)
1.一种组合物在皮肤再生中的用途,其特征在于,上述组合物包含(i)硫糖铝、(ii)果聚糖及(iii)透明质酸、其盐或其衍生物。
2.根据权利要求1所述的用途,其特征在于,相对于上述组合物,上述硫糖铝包含0.01%(w/v)至1.0%(w/v)。
3.根据权利要求1所述的用途,其特征在于,在上述组合物中,(i)上述硫糖铝、(ii)果聚糖及(iii)透明质酸、其盐或其衍生物的重量比为1:1:1至1:5:0.1。
4.根据权利要求1所述的用途,其特征在于,上述果聚糖为左聚糖、菊粉、梯牧草果聚糖、裸麦果糖胶或这些的组合。
5.根据权利要求1所述的用途,其特征在于,上述果聚糖为2000Da至100000kDa。
6.根据权利要求1所述的用途,其特征在于,上述透明质酸的盐或衍生物为乙酰化透明质酸钠、透明质酸钠、透明质酸钾、水解透明质酸、水解透明质酸钠、透明质酸钠交联聚合物、羟丙基三甲基氯化铵透明质酸、寡聚透明质酸或这些的组合。
7.根据权利要求1所述的用途,其特征在于,上述透明质酸、其盐或其衍生物的分子量为5000Da至1500000Da。
8.根据权利要求1所述的用途,其特征在于,上述组合物增加选自由层粘连蛋白332、XVII型胶原蛋白、过氧化物酶体增殖物激活受体γ辅激活因子-1α及丝聚蛋白组成的组中的一种以上蛋白质或编码其的基因的表达或转录。
9.根据权利要求1所述的用途,其特征在于,上述组合物减少白细胞介素-6的蛋白质或编码其的基因的表达或转录。
10.一种组合物在改善皮肤弹性中的用途,其特征在于,上述组合物包含(i)硫糖铝、(ii)果聚糖及(iii)透明质酸、其盐或其衍生物。
11.一种组合物在改善皱纹中的用途,其特征在于,上述组合物包含(i)硫糖铝、(ii)果聚糖及(iii)透明质酸、其盐或其衍生物。
12.一种组合物在皮肤保湿中的用途,其特征在于,上述组合物包含(i)硫糖铝、(ii)果聚糖及(iii)透明质酸、其盐或其衍生物。
13.一种组合物在改善皮肤损伤中的用途,其特征在于,上述组合物包含(i)硫糖铝、(ii)果聚糖及(iii)透明质酸、其盐或其衍生物。
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KR (1) | KR20240015803A (zh) |
CN (1) | CN117462447A (zh) |
WO (1) | WO2024025356A1 (zh) |
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US5908836A (en) * | 1987-12-21 | 1999-06-01 | Bar-Shalom; Daniel | Protecting skin from radiation damage using sulphated sugars |
JP2714705B2 (ja) | 1990-03-12 | 1998-02-16 | 株式会社山本製作所 | 精穀装置 |
KR100440357B1 (ko) * | 2001-10-25 | 2004-07-15 | 주식회사 바이오랜드 | 세포증식 및 피부 보습에 의한 탄력 증강 효능을 갖는레반 추출물을 함유한 화장료 조성물 |
GR1008308B (el) * | 2013-05-31 | 2014-10-02 | UNI-PHARMA ΚΛΕΩΝ ΤΣΕΤΗΣ ΦΑΡΜΑΚΕΥΤΙΚΑ ΕΡΓΑΣΤΗΡΙΑ ΑΒΕΕ με δ.τ. "UNI-PHARMA ABEE", | Τοπικες φαρμακευτικες και ιατροτεχνολογικες συνθεσεις που περιεχουν συνδυασμους σουκραλφατης, υαλουρονικου οξεος, αργινινης και ενος φυσικου ενυδατικου παραγοντα |
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2022
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- 2023-07-27 CN CN202310936329.8A patent/CN117462447A/zh active Pending
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WO2024025356A1 (ko) | 2024-02-01 |
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