CN102327199A - 包含具有双壳结构的纳米结构体的化妆品成分 - Google Patents
包含具有双壳结构的纳米结构体的化妆品成分 Download PDFInfo
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- CN102327199A CN102327199A CN2010106156462A CN201010615646A CN102327199A CN 102327199 A CN102327199 A CN 102327199A CN 2010106156462 A CN2010106156462 A CN 2010106156462A CN 201010615646 A CN201010615646 A CN 201010615646A CN 102327199 A CN102327199 A CN 102327199A
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Abstract
本发明公开一种化妆品成分,包括:水溶性生理活性成分核;核壳,为了包覆上述核而包含聚乙二醇-聚己内酯-聚乙二醇(PEG-PCL-PEG)三嵌段共聚物;纳米结构体,为了包覆上述核壳而以包含磷脂质或其衍生物的外部壳所构成。通过上述化妆品成分,可提高对氧化、光、热等脆弱的活性成分的稳定性、可将粒子大小制备成纳米水平,表现出高的经皮渗透率,可将各种除皱、美白生理活性成分等稳定地胶囊化的化妆品成分。
Description
技术领域
本发明涉及一种具有双壳结构的纳米结构体的化妆品成分,所述双壳结构是在制造将改善各种皱纹、美白的生理活性成分等稳定地胶囊化而制备的化妆品成分时非常有用的。
背景技术
功能性化妆品,是指具有皮肤美白效果、皮肤除皱改善效果、美黑或防紫外线等效果的产品。将作为上述产品的原料的视黄醇、维生素A、维生素C等的有效成分露出到光和热、空气的情形下,会导致稳定性的降低,由于皮肤的低吸收率而相对费用表现出低的效果。
由此,为解决上述问题而进行了制造如下高功能性化妆品的研究。即,通过使得用于化妆品的视黄醇、维生素A、维生素C等的不稳定物质趋于稳定,从外部条件保护生理活性成分,提高皮肤亲和性,使得皮肤吸收变得容易。
作为制造这样的高功能性化妆品的前提条件,有如下技术:可实现化妆品的功能的、确认了效果的高功能性生理活性材料的开发、可证明在皮肤的生理活性物质的功效的评价技术;可实现化妆品的功能而向所需部位准确传递生理活性物质的功能的技术等。因此,最终为了在所需部位实现持续开发中的高功能性生理活性材料的功能,最重要的核心课题是向皮肤内所需部位的正确传递(active targeting)。因此迫切需要一种适合皮肤且安全的材料的载体(carrier)和能透过皮肤的脂质膜等而安全/稳定地传递高功能性生理活性物质的技术的开发。
为解决这样的问题的生体亲和型生分解性高分子的开发,在乳剂粒子的稳定化研究和经皮渗透型载体研究中作为关注的对象,但因为化妆品产业的特性上的原因而需要表面化学、生命工学、皮肤科学、纳米工学、高分子工学、化学工学等相关领域的共同注目和技术开发,因此很多成果都处于未实现的状态。
发明内容
本发明的目的在于提供一种包含可稳定地包覆生理活性成分、具有纳米水平的粒子大小而使得相对皮肤的吸收率提高的纳米结构体,且可用作各种功能性化妆品的化妆品成分。
本发明是以如下方式实现的。本发明的化妆品成分,包括:
水溶性生理活性成分核;
核壳,为了包覆上述核而包含聚乙二醇-聚己内酯-聚乙二醇(Poly(ethylene glycol)-Polycaprolactone-Poly(ethyleneglycol),PEG-PCL-PEG)三嵌段共聚物;
纳米结构体,为了包覆上述核壳而以包含磷脂质或其衍生物的外部壳所构成。
根据本发明的纳米结构体,可提高对氧化、光、热等脆弱的活性成分的稳定性、可将粒子大小制备成纳米水平,表现出高的经皮渗透率,可将各种除皱、美白的生理活性成分等稳定地胶囊化的化妆品成分。
附图说明
图1是表示根据本发明的纳米结构体的结构的立体剖视图。
图2是表示在实施例1中制备的乳剂的粒子大小分布图,(a)为核壳,(b)为外部壳,(c)为纳米结构体的粒子大小分布。
图3是表示实施例1及比较例1的乳剂的皮肤浸透结果的图表。
在图1~图3中,10:纳米结构体,11:水溶性生理活性成分核
12:核壳,13:外部壳,A:核壳和外部壳之间的空间。
具体实施方式
本发明涉及一种为解决在乳剂(emulsion)、面霜(cream)、精华液(essence)、眼霜(eye cream)、底霜(make-up base)、粉底(foundation)等化妆品成分中使用具有多种功能的活性成分时的安全问题,揭示了以双层结构的壳所构成的纳米结构体,其大小以纳米水平制备,确保了进一步促进经皮渗透的效果。
图1是表示根据本发明的纳米结构体的结构的立体剖视图。
参照图1,纳米结构体10是由如下结构构成:
水溶性生理活性成分核11;
核壳12,为了围绕及包覆上述核11而包含聚乙二醇-聚己内酯-聚乙二醇(Poly(ethylene glycol)-Polycaprolactone-Poly(ethyleneglycol),PEG-PCL-PEG)三嵌段共聚物;
外部壳13,为了包覆上述核壳12而包含磷脂质或其衍生物。
上述水溶性生理活性成分核11是可进入多种化妆品剂型的粒子内的生理活性成分,可使用对化妆品赋予一定效果或功能的已知的大部分已验证的生理活性材料。
特别是,作为不稳定的生理活性材料,可以是用于如下化妆品组成的生理活性成分:美白剂、胶原合成促进剂、除皱剂、皮肤障壁(skin barrier)强化剂、抗老化剂、保湿剂等。
代表性的有,作为具有美白效果的生理活性成分可包含如下水溶性成分:AA2G(抗坏血酸葡糖苷,Ascorbic Acid 2-Glucoside)、维生素C(抗坏血酸,Ascorbic acid)、烟酰胺(Niacinamid)、熊果苷(Arbutin)、桑白皮(Morus alba Linne)提取物、构树提取物(Broussonetia kazinoki)、抗坏血酸磷酸酯镁(Magnesium Ascorbyl Phosphate)等。并且,作为除皱效果的活性成分可包含如下水溶性成分:羟脯胺酸(Hydroxyproline)、成长因子(EGF、FGF、IGF等)、肽(peptide)、N-乙酰葡糖胺(N-acetylglucosamine)等。
核壳12包含PEG-PCL-PEG三嵌段共聚物,这样的三嵌段共聚物是由亲水性的聚乙二醇(Polyethyleneglycol;PEG)A-嵌段、疏水性的聚己内酯(Polycaprolactone;PCL)B-嵌段。上述三嵌段共聚物是具有分子量比为PEG∶PCL∶PEG优选为1∶1∶1~1∶5∶1,更为优选为1∶2∶1~1∶3∶1的ABA-型三嵌段共聚物,优选为具有1500~20000g/mol的平均分子量、结晶化温度(Tc)为10~40℃的生物降解性共聚物。
上述三嵌段共聚物具有结晶型,从而在作为化妆品剂型制备时配向在乳剂表面而形成薄的薄膜,通过具有亲水性的A-嵌段和具有疏水性的B-嵌段的组合而同时具有自行装配性能(self-assembly)的两亲型表面活性剂(amphiphilic surfactant)和乳化剂的特性。由此,在乳化工序中容易吸附及配向在乳剂粒子的表面,形成薄膜而稳定化粒子内的不稳定的有效成分,经皮渗透(transdermal penetration)时因乳剂粒子的结构特性而使得更容易吸收、透过脂质双层(lipid double layer),可增加所需的化妆品的功能。
上述三嵌段共聚物可直接制备使用或者可购买使用市场上销售的物品。这样的三嵌段共聚物的功能可根据多种共聚物的嵌段设计而不同,可以是两亲型表面活性剂的功能、经皮吸收促进剂的功能、提高乳剂稳定性的功能、提高不稳定的生理活性成分的粒子内的稳定性的功能等多种功能。
特别是,在本发明中使用外部壳13制备具有纳米水平的粒子大小的纳米结构体10。在韩国发明专利公开第2008-105249号中,利用三嵌段共聚物包覆活性成分的粒子的情形下,粒子大小为17~20μm的微米水平,考虑到粒子大小越小皮肤渗透度越大,可预测以纳米水平制备粒子的情形下可进一步提高经皮吸收率。由此,在本发明中,通过以磷脂质进一步对包覆了生理活性成分核11的核壳12的过程中使用超高压乳化系统,将现有的微米水平的粒子纳米化成纳米水平。
纳米结构体10的外部壳13,包含磷脂质或其衍生物,且围绕核壳12地包覆。
磷脂质与皮肤的脂质成分类似,且具有优秀的扩散性、防止重新凝聚性及皮肤亲和力,因分散性的提高而使得颜色鲜明度提高的功能,特别是可有效防止皮肤干燥感的功能。可使用的磷脂质,优选从大豆或卵黄中提取的天然的饱和蛋黄素(lecithin)。这样的天然的饱和蛋黄素包含,卵磷脂(Phosphatidylcholine)23~95重量%,磷脂酰乙醇胺(Phosphatidylethanolamine)20重量%以下。并且,可使用蛋黄素的成分的卵磷脂(phosphatidylcholine)、溶血磷脂酰胆碱(lysophosphatidylcholine)、磷脂酰乙醇胺(Phosphatidylethanolamine)等的不饱和胆碱类、丝氨酸(serine)类、乙醇胺类化合物及它们的氢添加物形态的衍生物等。上述磷脂质占全部纳米结构体组成中的0.5~15.0重量%。如果该含量不足上述范围,则不能制备纳米水平的粒子。
与此相反地,如果超过上述范围,因原料及剂型上的黏度太高,且不能很好地分散及溶解,不能进行使用一般剂型或高压乳化机(微射流,Microfluidizer)的超高压乳化,因此不能实现剂型的制备。通过本发明的试验例1对粒子大小进行检测,发现在膦脂质含量不足时可制备数十微米水平的粒子。
进一步,作为外部壳13,可使用与磷脂质一起使用的补助乳化剂,此时,上述补助乳化剂可以是阴离子型、阳离子型、非离子型或者阳性离子类乳化剂,根据所使用的磷脂质含量及构成成分而使用相对磷脂质含量的0.5~5倍,优选使用1~3倍的比率,作为一例,可单独或混用聚甘油-10-五羟基硬脂酸盐(polyglyceryl-10-pentahydroxy stearate)、聚甘油-2-异硬脂酸盐(polyglyceryl-2-isostearate)、聚甘油-2-油酸盐(polyglyceryl-2-oleate)、聚甘油-3-二异硬脂酸盐(polyglyceryl-3-diisostearate)等的聚甘油类和鲸蜡基二甲基硅氧烷共聚醇(Cetyl Dimechicone Copolyol)、二甲基硅氧烷共聚醇(Dimechicone Copolyol)等的硅类。
并且,如图1所示,核壳12和外部壳13之间的空间A可进一步增加油溶性活性成分。这样的油溶性活性成分可使用前述的具有改善皱纹及美白效果的成分。
作为代表性的,具有美白性的生理化学成分可使用如下油溶性成分:油溶性甘草、维生素C乙基醚(Ethyl Ascorbyl Ether)、α-甜没药萜醇(α-Bisabolol)等。并且,作为具有除皱效果的活性成分有,维生素A(retinol)及其衍生物(例如,维生素A棕榈酸酯(Retinyl Palmitate))、腺苷(adenosine)等。
这样的油溶性活性成分的添加,可以通过对水溶性生理活性成分核11进行包覆的工序中添加到油中,或者后续的通过外部壳13的包覆工序中添加。
根据本发明的优选实施例中,核壳组成设为占全部100重量%,其中包括:
1)水溶性生理活性成分占0.1~5.0重量%;
2)油占50~70.0重量%;
3)三嵌段共聚物占0.5~20.0重量%;及
4)剩余为水。
根据本发明的纳米结构体组成设为占全部100重量%,其中包括:
1)包覆有水溶性生理活性成分核的核壳占0.5~20重量%;
2)油状部:
(1)油占0.5~10.0重量%;
(2)油溶性生理活性成分占5.0重量%以下的乳状部;及
3)水状部:
(1)磷脂质占0.5~15.0重量%;
(2)多元醇占10.0~60.0重量%;
(3)水溶性生理活性成分占5.0重量%以下;及
(4)剩余为水。
上述油,以可溶解生理活性成分和表面活性剂的方式使用该领域中常规使用的油。作为代表性的有:聚癸烯(polydecene)及石蜡油(paraffinoil)等的碳氢化合物类油;酯类合成油;硅油;动植物性油;羟乙基化酯(ethoxylated alkyl ester)油;胆固醇;胆固醇硫酸酯(CholesterylSulfate);诸如植物鞘氨醇(Phytosphingosine)、鞘氨醇(sphingosine)的鞘脂类(Sphingolipid);;由C10~40的脂肪醇、辛酸/癸酸甘油三酯(caprylic/capric triglyceride)、神经酰胺(ceramide)及它们的混合物所组成的组中选择的一种。并且,除了油外,还可添加,碳氢化合物;由月桂酸(lauric acid)、肉豆蔻酸(myristic acid)、棕闾酸(palmiticacid)、硬脂酸(stearic acid)、油酸(oleic acid)、亚油酸(linoleicacid)及它们的混合物所组成的组中选择的一种脂肪酸。
上述水是蒸馏水,优选使用脱离子蒸馏水。
对于上述多元醇,本发明中并不特别限定,可以使用公知的多元醇。作为一例,由丙二醇(propyleneglycol)、二丙二醇(propyleneglycol)、丁二醇(butylene glycol)、甘油(glycerin)、甲基丙醇(methylpropanol)、3-甲基-1,3-丁二醇(Isopreneglycol)、戊基乙二醇(pentylene glycol)及它们的混合物所构成的组中选择的一种。更为优选为使用丁二醇、或甘油,最优选为使用丁二醇。
此外,根据需要还可以包括该领域公知的溶剂或添加剂。上述溶剂是用于溶解油溶性成分而使用的,可以使用甲醇(methanol)、乙醇、丙醇、丁醇即它们的混合溶剂。并且,作为添加剂可使用防腐剂、pH调节剂、表面活性剂、防氧化剂、紫外线阻断剂、颜料、染料、香料、稳定化剂、增黏剂等,该领域普通技术人员可适当选择。
对于根据本发明的纳米结构的制备方法,本发明中并不进行特别限定,可使用常规使用的乳化方法,优选使用高压乳化方法。
具体说明是通过如下方法制备的。
S1)将水溶性生理活性成分及三嵌段共聚物溶解于净化水后,与油混合而制备活性成分以核包覆的核壳结构。
S2)制备油、及溶解有选择性的油溶性生理活性成分的乳状部、磷脂质、多元醇、在水中溶解有选择性的水溶性生理活性成分的水状部。
S3)在上述水状部混合S1)的核壳组成及S2)的乳状部后通过超高压乳化工序制备。
上述溶解是通过常规方法进行,根据需要进行搅拌或在50~80℃、优选为65~75℃条件下加热进行。
乳化可在常规的混合机(作为一例,使用乳化均质机)进行,优选为以2000~4000rpm、更为优选为以3000rpm的速度搅拌3~10分钟,从而获得一次乳化生成物。
将通过乳化而获得的乳化生成物冷却到50~60℃后,通过高压型均质机或高压乳化机以500bar、优选为以1000~2500bar处理3次而制备纳米结构体。
这样制备的纳米结构体,具有纳米水平的粒子,制备成乳化成分形态。包含水溶性生理活性成分的核的粒子大小为80~110nm,包含磷脂质的外部壳为300~350nm,上述以外部壳包覆核的纳米结构体的粒子大小为300~500nm,优选具有390~460nm(如图2所示)。具有这样的粒子大小范围的纳米结构体,与现有的微细乳化粒子相比而制备成纳米水平,在适用于皮肤时相对增加与皮肤的接触面积,提高经皮渗透率及经皮吸收面积。
并且,考虑到皮肤角质层的各细胞之间的脂质之间的缝隙为约50nm,和乳化粒子的乳化膜具有柔韧性而根据本发明的纳米结构体的情形下具有皮肤细微乳化粒子容易吸收及扩散到细胞之间的脂质内的优点。
即,根据本发明的纳米结构体制备成平均粒径为纳米水平,由此以与皮肤的接触面积的增加及细胞间脂质中的渗透及扩散此2个途径,提高了构成核的去皱、美白等的功能优秀的生理活性成分的经皮吸收率。
这样的纳米结构可直接用作化妆品成分,并可应用为各种功能性化妆品。
用作化妆品成分的情形下,上述纳米结构体的含量相对全部化妆品成分总量的0.001~30.0重量%,优选为0.1~5.0重量%。在上述纳米结构体含量未满上述范围的情形下对于起效存在问题,与此相反地,如超过上述范围时随着含量增加的效果的增加不明显,降低剂型的稳定性的问题。
本发明的化妆品成分可以制备成公知的任何一种剂型,可剂型化为溶液、悬浮液、乳剂、糊状物(paste)、胶、面霜(cream)、乳液(lotion)、粉末(powder)、肥皂(soap)、含表面活性剂的清洁剂(cleansing)、油、粉末粉底、乳剂粉底、蜡粉底(wax foundation)及喷雾形(spray)等。
并且,各剂型的成分可包含对该剂型的制剂化所需的各种基质和添加物,在不降低该效果的范围内可包含如下公知成分来制备:非离子表面活性剂、硅聚合物(silicon polymer)、体质颜料、香料、防腐剂、杀菌剂、氧化稳定剂、有机溶剂、离子型或非离子型增黏剂(viscosity agent)、柔软剂、防氧化剂、自由基清除剂、不透明剂、稳定剂、润肤剂(emollient)、硅、α-羟基酸(alpha hydroxy acid)、消泡剂、保湿剂、维生素、昆虫驱避剂(Insect repellant)、香料、保存剂、表面活性剂、消炎剂、P物质(Substance P)、填充剂、聚合体、燃料(fuel)、碱性化剂或酸性化剂、或者着色剂等。
【实施例】
以下,为便于理解本发明揭示优选实施例及比较例。但是,本发明的实施例可以进行各种形态的变形,下述实施例是为更容易理解本发明而提供的,本发明的保护范围并不限于下述实施例。本发明的下述各叔叔里是为了对本技术领域的普通技术人员进行更完整的说明而提供的。
实施例1~2及比较例1~5
(1)核壳的制造
准备了下表1所示的组成及含量。
将水状部和油状部分别加热到50℃而完全溶解后,在上述水状部中慢慢投入油状部,并通过均质机以2000rpm速度乳化3分钟,从而制备了包含一次核壳的乳化液。此时,三嵌段共聚物的PEG∶PCL∶PEG比例为1∶2∶1,分子量为1000g/mol的PEG和1000g/mol的PCL而制备而成的制品(使用了韩国发明专利公开第2008-0105249号中揭示的方法)。
【表1】
核壳组成
(2)纳米结构体的制造
准备下表2所示的组成及含量来制备包覆上述核壳的纳米结构体。
将上述水状部和油状部加热到70℃而完全溶解后,在水状部中慢慢投入油状部,并通过均质机以3000rpm速度乳化5分钟。将所制备的乳化液的温度降低到45℃后,将在上述(1)制备的乳化液渐渐滴下而以2000rpm混合5分钟后,使用高压乳化机(微射流,Microfluidizer)以1000bar/3cycles进行而制备分散有纳米结构体的乳剂。
【表2】
试验例1:粒子大小的检测
对所获得的纳米结构体的粒子尺寸通过动态光散射仪(Dynamic LightScattering;DLS)进行检测,其结果如下图2所述。图2是表示实施例1中制备的乳剂粒子大小的分布图,(a)核壳、(b)外部壳、(c)纳米结构体的粒子大小分布。如图2所示,粒子大小分布表示为,核壳的情形下约为80~110nm,外部壳的情形下约为300~350nm,根据本发明的纳米结构体的情形下为390~460nm。此时,观察图3的(c)时,未包覆的一部分核壳在约90nm被观察,通过过滤去除了此核壳。
与此相比较,比较例1的乳剂的情形下的粒子大小约为15μm,比较例2的乳剂(韩国发明专利公开第2007-105249号)的情形下的粒子大小约为18μm水平相比较,可知道通过本发明实现纳米水平的制备。
此外,在比较例3及比较例4的乳剂也是制备了微米水平的粒子(10~30μm)。
特别是,在比较例5的情形下,因蛋黄素过量而提高了黏度,由此导致不能制备乳剂成分。
试验例2:皮肤渗透促进效果的评价
使用改进型Franz扩散池(Modified Franz diffusion cell)对利用生分解性三嵌段共聚物的纳米结构体的药物放出量进行了检测。对从老鼠身上采集的4cm2的采集皮肤适用了利用包含AA2G的生分解性三嵌段共聚物的纳米结构体和包含AA2G的一般乳剂,将提取皮肤固定于供体(donor)和受体相(receptor phase)之间后,作为受体相使用在实验前事先以37℃加热而准备的pH7.4的磷酸缓冲液。此时,壳的体积为11ml,实验中以温度为37℃±0.5℃、搅拌速度为600rpm的方式维持了规定时间。通过微量吸液管(Micropipette)以每20分钟准确采集1ml的方式采集5个小时,通过HPLC分别检测AA2G浓度,所获得的结果如图3所示。
图3是表示实施例1及比较例1的乳剂的皮肤渗透结果的图表。如图3所示,根据本发明所制备的纳米结构体可实现在短时间内浸透到皮肤,确认了在皮肤涂布200分钟后皮肤吸收速度约为4.5倍,加快了吸收速度。
试验例3:稳定性提高的评价
将在上述实施例及比较例中所制备的成分在25℃、5℃,cycle、45℃烤箱中分别保管1个月,对相的稳定性进行了肉眼观察。此时,“cycle”是指在25℃、5℃、cycle、45℃分别循环6个小时,◎是表示“非常好”,○表示“好”,Δ表示“稍微变差”,×表示“非常差”。
【表3】
45℃ | cycle | 25℃ | 5℃ | |
实施例1 | ◎ | ◎ | ◎ | ◎ |
实施例2 | ◎ | ◎ | ◎ | ◎ |
比较例1 | ○ | ○ | ○ | ○ |
比较例2 | ○ | ○ | ○ | ○ |
比较例3 | ○ | ○ | ○ | ○ |
比较例4 | ○ | Δ | ○ | ○ |
比较例5 | ○ | ○ | Δ | Δ |
如上表3所示,根据本发明的实施例及比较例的成分在比较高温及低温的情形下也具有优秀的分散稳定性。
以下,为便于理解本发明而提供优选剂型例。但是如下剂型例仅为更容易理解本发明而提供,本发明的内容并不限于剂型例。
剂型例1:柔软化妆水(皮肤乳液)
如下表4所示,通过常规方法制备了柔软化妆水。
【表4】
成分 | 含量(重量%) |
实施例1的纳米结构体 | 2.0 |
甘油(glycerin) | 5.0 |
1,3-丁二醇(1,3-Butylene glycol) | 3.0 |
PEG 1500 | 1.0 |
尿囊素(allantoin) | 0.1 |
DL-泛醇(dl-panthenol) | 0.3 |
EDTA-2Na | 0.02 |
二苯酮-9(Benzophenone-9) | 0.04 |
透明质酸钠(sodium hyaluronate) | 5.0 |
乙醇(ethanol) | 10.0 |
辛基十二醇聚醚-16(Octyldodeceth-16) | 0.2 |
山梨酸盐20(sorbate 20) | 0.2 |
Unicide-U13 | 0.01 |
蒸馏水 | 残量 |
合计 | 100 |
剂型例2:收敛化妆水
如下表5所示,通过常规方法制备了收敛化妆水。
【表5】
成分 | 含量(重量%) |
实施例1的纳米结构体 | 2.0 |
甘油(glycerin) | 2.0 |
1,3-丁二醇(1,3-Butylene glycol) | 2.0 |
尿囊素(allantoin) | 0.2 |
DL-泛醇(dl-panthenol) | 0.2 |
EDTA-2Na | 0.02 |
二苯酮-9(Benzophenone-9) | 0.04 |
透明质酸钠(sodium hyaluronate) | 3.0 |
乙醇(ethanol) | 15.0 |
山梨酸盐20(sorbate 20) | 0.3 |
金缕梅(witch hazel)提取物 | 2.0 |
柠檬酸(citric acid) | 微量 |
Unicide-U13 | 0.01 |
蒸馏水 | 残量 |
合计 | 100 |
剂型例3:营养化妆水
如下表6所示,通过常规方法制备了营养化妆水。
【表6】
成分 | 含量(重量%) |
实施例1的纳米结构体 | 2.0 |
甘油硬脂酸酯SE(Glyceryl Stearate SE) | 1.5 |
硬脂醇(stearyl Alcohol) | 1.5 |
羊毛脂(lanolin) | 1.5 |
聚山梨醇酯60(Polysorbate 60) | 1.3 |
山梨醇硬脂酸酯(sorbitan stearate) | 0.5 |
硬化植物油 | 1.0 |
矿物油 | 5.0 |
角鲨烯(squalane) | 3.0 |
三辛酸甘油酯(trioctanoin) | 2.0 |
二甲聚硅氧烷(dimethicone) | 0.8 |
盐酸生育酚酯(Tocopherol acetate) | 0.5 |
聚羧乙烯(carboxyvinyl polymer) | 0.12 |
甘油(glycerin) | 5.0 |
1,3-丁二醇(1,3-Butylene glycol) | 3.0 |
透明质酸钠(sodium hyaluronate) | 5.0 |
三乙醇胺(Triethanolamine) | 0.12 |
Unicide-U13 | 0.02 |
蒸馏水 | 残量 |
合计 | 100 |
剂型例4:营养霜
如下表7所示,通过常规方法制备了营养霜。
【表7】
剂型例5:按摩霜
如下表8所示,通过常规方法制备了按摩霜。
【表8】
剂型例6:精华液
如下表9所示,通过常规方法制备了精华液。
【表9】
成分 | 含量(重量%) |
实施例1的纳米结构体 | 0.3 |
甘油(glycerin) | 10.0 |
内胺盐(Betaine) | 5.0 |
PEG 1500 | 2.0 |
尿囊素(allantoin) | 0.1 |
DL-泛醇(dl-panthenol) | 0.3 |
EDTA-2Na | 0.02 |
二苯酮-9(Benzophenone-9) | 0.04 |
羟乙基纤维素(hydroxyethyl cellulose) | 0.1 |
透明质酸钠(sodium hyaluronate) | 8.0 |
聚羧乙烯(carboxyvinyl polymer) | 0.2 |
三乙醇胺(Triethanolamine) | 0.18 |
辛基十二碳醇(Octyldodecanol) | 0.3 |
辛基十二醇聚醚-16(Octyldodeceth-16) | 0.4 |
乙醇 | 6.0 |
Unicide-U13 | 0.01 |
蒸馏水 | 残量 |
合计 | 100 |
剂型例7:洁肤霜
如下表10所示,通过常规方法制备了洁肤霜。
【表10】
成分 | 含量(重量%) |
实施例1的纳米结构体 | 0.3 |
聚乙烯醇(polyvinyl alcohol) | 15.0 |
纤维素胶(cellulose gum) | 0.15 |
甘油(glycerin) | 3.0 |
PEG 1500 | 2.0 |
DL-泛醇(dl-panthenol) | 0.4 |
尿囊素(allantoin) | 0.1 |
甘草酸单铵盐(Ammonium Glycyrrhizinate) | 0.3 |
烟酰胺(nicotinamide) | 0.5 |
乙醇(ethanol) | 6.0 |
PEG 40硬化蓖麻油(castor oil) | 0.3 |
Unicide-U13 | 0.02 |
蒸馏水 | 残量 |
合计 | 100 |
【产业上的实用性】
根据本发明的纳米结构体可以适用于所有化妆品,即,乳液、面霜、眼霜、除皱相关产品、美白相关产品、线相关产品、底霜、粉底、嘴唇用等多种化妆品成分。
Claims (12)
1.一种化妆品成分,包括:
水溶性生理活性成分核;
核壳,为了包覆上述核而包含聚乙二醇-聚己内酯-聚乙二醇(PEG-PCL-PEG)三嵌段共聚物;
纳米结构体,为了包覆上述核壳而以包含磷脂质或其衍生物的外部壳所构成。
2.根据权利要求1所述的化妆品成分,其中,上述水溶液生理活性成分是从AA2G(抗坏血酸葡糖苷,Ascorbic Acid 2-Glucoside)、维生素C(抗坏血酸,Ascorbic acid)、烟酰胺(Niacinamid)、熊果苷(Arbutin)、桑白皮(Morus alba Linne)提取物、构树提取物(Broussonetia kazinoki)、抗坏血酸磷酸酯镁(Magnesium Ascorbyl Phosphate)、羟脯胺酸(Hydroxyproline)、成长因子、肽(peptide)、N-乙酰葡糖胺(N-acetylglucosamine)及它们的组合所组成的组中选择的一种。
3.根据权利要求1所述的化妆品成分,其中,
上述三嵌段共聚物的结晶化温度为(Tc)10~40℃,PEG∶PCL∶PEG的比例为1∶1∶1~1∶5∶1,利用分子量为400~3000g/mol的PEG和分子量为400~3000g/mol的PCL来制备的。
4.根据权利要求1所述的化妆品成分,其中,
上述磷脂质是从大豆或卵黄中提取的天然的蛋黄素(lecithin);包含卵磷脂(phosphatidylcholine)、溶血磷脂酰胆碱(lysophosphatidylcholine )、磷脂酰乙醇胺(Phosphatidylethanolamine)的不饱和胆碱类;丝氨酸(serine)类;乙醇胺类;它们的氢添加物形态的衍生物;及它们的组合所组成的组中选择的一种。
5.根据权利要求1所述的化妆品成分,其中,
上述磷脂质占全部纳米结构体的组成中的0.5~15.0重量%。
6.根据权利要求1所述的化妆品成分,其中,
上述纳米结构体设为占全部100重量%,其中包括:
1)包覆有水溶性生理活性成分核的核壳占0.5~20重量%;
2)油状部:
(1)油占0.5~10.0重量%;
(2)油溶性生理活性成分占5.0重量%以下的乳状部;及
3)水状部:
(1)磷脂质占0.5~15.0重量%;
(2)多元醇占10.0~60.0重量%;
(3)水溶性生理活性成分占5.0重量%以下;及
(4)剩余为水。
7.根据权利要求6的化妆品成分,上述核壳组成设为占全部100重量%,其中包括:
1)水溶性生理活性成分占0.1~5.0重量%;
2)油占50~70.0重量%;
3)三嵌段共聚物占0.5~20.0重量%;及
4)剩余为水。
8.根据权利要求1所述的化妆品成分,其中,
在核壳和外部壳之间进一步包括油溶性生理活性成分。
9.根据权利要求8所述的化妆品成分,其中,上述油溶性生理活性成分是从油溶性甘草、维生素C乙基醚(Ethyl Ascorbyl Ether)、α-甜没药萜醇(α-Bisabolol)、维生素A(retinol)及其衍生物、腺苷(adenosine)及它们的组合所组成的组中选择的一种。
10.根据权利要求1所述的化妆品成分,其中,
上述纳米结构体的平均粒径为300~500nm。
11.根据权利要求1所述的化妆品成分,其中,
上述纳米结构体占全部化妆品成分总重量的0.001~30.0重量%。
12.根据权利要求1所述的化妆品成分,其中,
上述化妆品成分具有如下剂型:柔软化妆水、收敛化妆水、营养化妆水、营养霜、按摩霜、精华液或洁肤霜。
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US20120015011A1 (en) | 2012-01-19 |
CN102327199B (zh) | 2013-03-27 |
US8541010B2 (en) | 2013-09-24 |
KR101249716B1 (ko) | 2013-04-05 |
KR20120006722A (ko) | 2012-01-19 |
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