CN116459170A - 一种脂质体组合物及其在化妆品中的应用 - Google Patents
一种脂质体组合物及其在化妆品中的应用 Download PDFInfo
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- CN116459170A CN116459170A CN202310594403.2A CN202310594403A CN116459170A CN 116459170 A CN116459170 A CN 116459170A CN 202310594403 A CN202310594403 A CN 202310594403A CN 116459170 A CN116459170 A CN 116459170A
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- liposome composition
- active ingredient
- liposome
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- 229940115478 isopropyl lauroyl sarcosinate Drugs 0.000 claims abstract description 16
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- 229940045898 sodium stearoyl glutamate Drugs 0.000 claims abstract description 15
- KDHFCTLPQJQDQI-BDQAORGHSA-M sodium;(4s)-4-amino-5-octadecanoyloxy-5-oxopentanoate Chemical compound [Na+].CCCCCCCCCCCCCCCCCC(=O)OC(=O)[C@@H](N)CCC([O-])=O KDHFCTLPQJQDQI-BDQAORGHSA-M 0.000 claims abstract description 15
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
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Abstract
本发明涉及一种新型脂质体组合物及其在化妆品中的应用,所述脂质体组合物包含活性成分、硬脂酰谷氨酸钠和月桂酰肌氨酸异丙酯。
Description
技术领域
本发明涉及一种新型脂质体组合物及其在化妆品中的应用,所述脂质体组合物包含活性成分、硬脂酰谷氨酸钠和月桂酰肌氨酸异丙酯的组合。
背景技术
在化妆品领域中,有些活性成分具有溶解性低、刺激性高、难以透皮吸收的特点,这严重限制了它们的应用。为解决这一问题,现有技术开发了用脂质体包裹负载这些活性成分的技术。
脂质体最早是1965年由Bangham等作为生物模型提出来的,是以卵磷脂、胆固醇等作为膜材形成的具有封闭囊泡结构的载体,其中亲水基团位于膜的表面和脂溶性基团位于膜的中间,每层膜之间具有一定空间,可以包封疏水性药物。脂质体作为一种新型载体,具有稳定性好、靶向性强、可延缓释放、无免疫毒性等特点。20世纪80年代,脂质体主要应用于医药行业,后因其独特的性能逐渐被应用于化妆品领域中。
然而,常见的脂质体存在一系列的问题,包括活性成分负载量低、稳定性差等,这些问题极大限制了其在化妆品中的应用。现有技术的脂质体一般仅能负载低于5%的活性成分,例如,在CN104983591B中,活性物β-胡萝卜素的负载量为0.1-1%;在CN201510400196.8中,抗皱保湿活性物的负载量为0.4-1.5%。
因此,在化妆品领域中,需要一种新型的脂质体组合物,其可解决脂质体对活性成分的负载量低、在正常储存条件下和在化妆品配方中不稳定的问题。
附图的简要说明
图1-10分别是脂质体A-J的冷冻电子显微镜照片。
图11-20分别是脂质体A-J的显微镜照片。
发明内容
本发明人经研究发现,硬脂酰谷氨酸钠和月桂酰肌氨酸异丙酯的组合在提高活性成分在脂质体中的负载量和稳定性方面发挥了明显的协同作用。
因此,一方面,本发明涉及硬脂酰谷氨酸钠和月桂酰肌氨酸异丙酯的组合在脂质体组合物中的用途,其中所述硬脂酰谷氨酸钠和月桂酰肌氨酸异丙酯的组合可提高活性成分在脂质体中的负载量和稳定性。
另一方面,本发明涉及一种脂质体组合物,其包含活性成分、硬脂酰谷氨酸钠和月桂酰肌氨酸异丙酯。
所述硬脂酰谷氨酸钠是一种乳化剂,月桂酰肌氨酸异丙酯是一种脂质,它们都是已知的化合物,其均可商购获得,例如,硬脂酰谷氨酸钠可购自BASF,月桂酰肌氨酸异丙酯可购自味之素株式会社。
在所述脂质体组合物中,硬脂酰谷氨酸钠的含量为约0.1-3%,优选约0.3-2%;月桂酰肌氨酸异丙酯的含量为约1-20%,优选约3-15%,更优选约5-10%;所述含量均基于所述脂质体组合物的总重量。
所述活性成分待负载在脂质体组合物中,其是化妆品中已知的和包括例如花榈木树皮提取物、白藜芦醇、姜黄素、神经酰胺、苯乙基间苯二酚、视黄醇、甘草类黄酮、光果甘草根提取物、槲皮素、槲皮苷、黄芩苷、黄芩素、水飞蓟素、山奈酚、泛醌、芦荟苦素、光甘草定、五羟黄酮、四氢胡椒碱、紫檀芪、橙皮苷、积雪草苷、水杨酸和阿魏酸等。在本发明的脂质体组合物中,优选的活性成分包括苯乙基间苯二酚、白藜芦醇和花榈木树皮提取物。
所述脂质体组合物通常还包含多元醇、助乳化剂、膜修饰剂和水等,以及还可以进一步包含其它的脂质和乳化剂等。
所述多元醇包括但不限于二元醇和三元醇,例如1,2-戊二醇、异戊二醇、甘油、1,3-丁二醇、双丙甘醇和1,3-丙二醇、山梨醇。优选地,所述多元醇选自1,2-戊二醇、1,3-丁二醇和1,3-丙二醇。所述多元醇的含量是本领域已知的,其通常为约1-20%,优选约7-15%,基于所述脂质体组合物的总重量。
所述助乳化剂是化妆品中常用的助乳化剂,其可选自甘油脂肪酸酯(例如,甘油硬脂酸酯SE、甘油肉豆蔻酸酯、甘油十一碳烯酸酯和单硬脂酸甘油酯)、L-赖氨酸、聚乙烯醇或海藻酸钠,磷脂类乳化剂(例如卵磷脂、氢化卵磷脂、羟基化卵磷脂、溶血卵磷脂、氢化溶血卵磷脂)等。优选的助乳化剂选自单硬脂酸甘油酯、氢化卵磷脂和卵磷脂。
所述膜修饰剂是化妆品中常用的那些,包括但不限于甾醇类,例如植物混合甾醇、β-谷甾醇、胆甾醇、菜油甾醇、谷甾烷醇、麦角甾醇和豆甾醇。优选地,所述膜修饰剂包括植物混合甾醇和β-谷甾醇。所述膜修饰剂含量是本领域已知的,其通常为约0.1-2%,优选约0.2-1%,基于所述脂质体组合物的总重量。
所述其它的脂质是化妆品中常用的那些,包括但不限于酯类,例如鲸蜡醇乙基己酸酯、棕榈酸乙基己酯、肉豆蔻酸异丙酯、辛酸/癸酸甘油三酯、碳酸二辛酯、椰油醇-辛酸酯/癸酸酯、单硬脂酸甘油酯;醇类,例如辛基十二醇、山嵛醇、鲸蜡醇和硬脂醇等;烃类,例如异十六烷和氢化聚异丁烯等。优选地,所述其它的脂质选自棕榈酸乙基己酯、肉豆蔻酸异丙酯、辛酸/癸酸甘油三酯、单硬脂酸甘油酯、山嵛醇和硬脂醇。所述其它的脂质的含量是本领域已知的,其通常为约10-30%,优选约15-25%,基于所述脂质体组合物的总重量。
所述其它的乳化剂是化妆品中常用的乳化剂,其可选自非离子乳化剂,例如葡糖苷类乳化剂(例如鲸蜡硬脂基葡糖苷),聚醚类乳化剂(例如硬脂醇聚醚-21),聚甘油类乳化剂(例如聚甘油-3甲基葡糖二硬脂酸酯);阴离子型乳化剂,例如羧酸盐(例如硬酯酰谷氨酸钠、硬脂酰乳酸钠等),硫酸酯盐(例如鲸蜡硬脂醇硫酸酯钠),磷酸酯盐(例如鲸蜡醇磷酸酯钾、硬脂醇磷酸酯)等。优选地,所述其它的乳化剂选自鲸蜡硬脂基葡糖苷、硬脂醇聚醚-21、聚甘油-3甲基葡糖二硬脂酸酯。所述其它的乳化剂含量是本领域已知的,其通常为约0.5-7%,优选约1-4%,基于所述脂质体组合物的总重量。
再一方面,本发明提供一种制备上述脂质体组合物的方法,其包括如下步骤:
a.在60-90℃、优选75-85℃的温度下,混合多元醇、硬脂酰谷氨酸钠、助乳化剂和水,得到均匀的混合物A;
b.在60-90℃、优选75-85℃的温度下,预混合月桂酰肌氨酸异丙酯、膜修饰剂、助乳化剂,然后将活性成分加入其中并在搅拌下进行进一步混合,得到均匀的混合物B;
c.在搅拌下,将混合物A和混合物B进行混合,得到均匀的混合物C;和
d.采用高压微射流均质机处理混合物C,得到脂质体组合物,其中高压微射流均质机的压力为约10,000-30,000psi,优选约20,000-30,000psi,和循环次数为约2-5次,优选约3次。
在上述步骤a中,还可以进一步加入其它的乳化剂以有助于得到均匀的混合物A。为了加快混合,可在搅拌下进行所述混合,搅拌的速度可为约100-1000rpm,优选约300-800rpm。
在上述步骤b中,所述搅拌的速度可为约100-1000rpm,优选约200-500rpm,更优选约300-400rpm,搅拌时间可为约10-30min,优选约20-30min。在预混合中,为了加快混合,可在搅拌下进行所述预混合,搅拌的速度可为约100-1000rpm,优选约300-800rpm。
在上述步骤c中,所述搅拌的速度可为约500-1000rpm,优选约700-900rpm,搅拌时间可为约5-10min,优选约8-10min。所述步骤c一般在常温下进行。
上述步骤d通常在常温下进行。
本发明的制备方法由于采用高压微射流技术,借助高速撞击、剪切和空化作用达到了均质和细化的目的,具有操作简便、清洁安全、易于连续化生产和可获得稳定的脂质体组合物的优点。
本发明的脂质体组合物通常为淡黄色泛蓝光的均匀液体,具有约100-500nm、优选约100-300nm、更优选约100-200nm和最优选100-120nm的粒径。本发明的脂质体组合物具有良好的稳定性,其粒径能长期保持稳定,例如,所述脂质体组合物在常温下可稳定至少一年,至少两年,或至少三年。
与现有技术的脂质体相比,本发明的脂质体组合物可以显著包含(负载)更多的活性成分。例如,本发明的脂质体组合物中可以负载大于5%、优选约5-35%、更优选约5-30%和最优选约15-25%的活性成分,基于脂质体组合物的总重量。而且,本发明的脂质体组合物中活性成分的包封率为大于70%、优选大于80%、更优选大于90%、甚至优选大于95%,基于负载的活性成分的总重量。
本发明的脂质体组合物作为中间体用于化妆品组合物中,以提供可有效利用的活性成分。本发明的脂质体组合物具有良好的稳定性,而且粒径能长期保持稳定,这对于其随后用于化妆品组合物中和因此充分发挥活性成分的功效而言是非常重要的。
又一方面,本发明提供一种化妆品组合物,其包含上述脂质体组合物。通常,所述脂质体组合物在化妆品组合物中的含量为约3-20%,优选约5-15%,基于所述化妆品组合物的总重量。
所述化妆品组合物可以是任何剂型的化妆品组合物,例如保湿液、精华、乳液、面霜、粉底、防晒乳霜、喷雾等。
除了所述脂质体组合物外,所述化妆品组合物还任选地包含化妆品中常用的成分,其包括但不限于润肤剂、保湿剂、皮肤调理剂等活性组分,稀释剂、分散剂、溶剂或载体等媒介物,表面活性剂,乳化剂、增稠剂、防腐剂、香料、pH调节剂等辅料,这些是本领域技术人员已知的,且可根据需要具体选择其类型和用量。
本发明的化妆品组合物可通过本领域已知的任何合适的方法制备。例如,可使用化妆品领域中常用的溶解槽、乳化锅、分散器、输送泵等设备,根据本领域已知的工艺,进行制备。例如,可首先将水溶性物质投入水相溶解釜,将油溶性物质投入油相溶解釜,分别将两个釜的温度加热至大约80℃,其中对于易结块的原料,可先用分散器将其预分散;待溶解完成后,将油相和水相递送至乳化锅中,进行均质乳化约5-15min;乳化完成后,将料体温度降至45℃,加入脂质体组合物并搅拌5min。继续降温至室温,任选地,加入香精、防腐剂等,并视需要调节产物的pH;待相关检测指标合格后,可灌装出货。以上制备工艺仅仅是例举性的,本领域技术人员可根据剂型要求进行增减或调整,从而制备得到喷雾、乳液、膏、霜或凝胶等各种剂型。
实施例
以下结合实施例,对本发明进行进一步详细说明。
实施例1:制备本发明的脂质体组合物和对照脂质体组合物
在该实施例中,制备了具有下述配方的本发明的脂质体组合物和对照脂质体组合物。
表1
表1’
成分(重量%) | 脂质体F | 脂质体I | 脂质体J |
硬脂酰谷氨酸钠 | 0.8 | 0.8 | 0.8 |
月桂酰肌氨酸异丙酯 | 15 | 15 | 15 |
氢化卵磷脂 | 5 | 5 | 5 |
丙二醇 | 10 | 10 | 10 |
辛酸/癸酸甘油三酯 | 25 | 25 | 25 |
甘油硬脂酸酯 | 1.5 | 1.5 | 1.5 |
植物甾醇类 | 0.5 | 0.5 | 0.5 |
花榈木树皮提取物 | 20 | 0 | 0 |
山奈酚 | 0 | 20 | 0 |
二氢燕麦酰基邻氨基苯甲酸 | 0 | 0 | 20 |
水 | 22.5 | 22.5 | 22.5 |
上述脂质体组合物制备工序如下:
a.称取丙二醇、硬脂酰谷氨酸钠、氢化卵磷脂和去离子水,在75℃和500rpm下搅拌混合20min,得到A相;
b.称取月桂酰肌氨酸异丙酯、植物甾醇类、辛酸/癸酸甘油三酯和单硬脂酸甘油酯,在75℃和500rpm下混合10min,然后将活性成分(花榈木树皮提取物或白藜芦醇或苯乙基间苯二酚等)加入其中并继续搅拌混合10min,得到B相;
c.在室温(和800rpm的搅拌下,混合A相和B相,得到混合液C;
d.然后将混合液C加入高压微射流均质机,在20000psi的压力下循环3次,得到上述脂质体组合物。
实施例2:测试脂质体组合物中的活性成分负载量和包封率
采用乙醇稀释后紫外吸光光度法测试负载量。具体地,取100uL的脂质体组合物用乙醇稀释10000倍,制成样品。采用同样的方法制作对照品(无活性成分),并使用超声分散机充分分散,然后将样品通过0.22μm的滤膜过滤,测试样品在紫外下的吸光值并与标准曲线对照,计算出脂质体组合物中的活性成分的负载量p(Wt%),其计算方法如下:
负载量p=[脂质体组合物中活性成分的量Wt/载体中活性成分的总量Wz]×100%
采用超滤离心法测定脂质体的包封率。具体地,精密称取400uL脂质体组合物并放入超滤离心管中,使用高速冷冻离心机,在10000rpm下离心30min;离心结束后,取超滤离心管下层滤液并放入10mL容量瓶中,通过HPLC测定滤液中的花榈木树皮提取物或白藜芦醇或苯乙基间苯二酚等活性成分的含量(Wf),同时计算400uL脂质体组合物中的所述活性成分的总含量(Wt),和根据下式计算包封率(EE):
包封率(EE)计算方法为:EE=(Wt-Wf)/Wt*100%。
结果如下表所示。
表2
表2’
成分(重量%) | 脂质体F | 脂质体I | 脂质体J |
负载量p(g/100g) | 19.47 | 9.48 | 8.98 |
包封率(%) | 96.44 | 73.24 | 64.63 |
实施例3:测试脂质体组合物的稳定性
在常温下放置脂质体组合物脂质体。一年后肉眼可观察到,对照脂质体A-C和I-M有肉眼可见的晶体析出且明显分层,而本发明的脂质体D-H的颜色无明显变化,没有晶体析出和分层。
经激光粒度仪测试,各脂质体样品的粒径均低于200nm,在约100-120nm的范围内。
在冷冻电子显微镜下观察,对照脂质体A-C和I-J在视野内已经基本无规则圆形存在,偶有不规则椭圆形大颗粒存在;而本发明的脂质体D-H的颗粒依然呈初始状态下的规则圆形;参见附图1-10。
在显微镜下观察,对照脂质体A-C和I-J有较多且较大晶体颗粒析出,程度逐步减弱,而本发明的脂质体D-H中的晶体没有明显析出,参见附图10-20。
以上所述实施例的技术方案是本发明优选实施方式,在不脱离本发明原理的前提下还可以进行若干改进和变换,这些改进和变化也应视为在本发明的保护范围内。
Claims (15)
1.硬脂酰谷氨酸钠和月桂酰肌氨酸异丙酯的组合在脂质体组合物中的用途。
2.根据权利要求1所述的用途,其中硬脂酰谷氨酸钠在所述脂质体组合物中的含量为0.1-3%,优选0.3-2%;月桂酰肌氨酸异丙酯在所述脂质体组合物中的含量为1-20%,优选3-15%,更优选5-10%;基于所述脂质体组合物的总重量。
3.根据权利要求1或2所述的用途,其中所述脂质体组合物包含选自下述的活性成分:花榈木树皮提取物、白藜芦醇、姜黄素、神经酰胺、苯乙基间苯二酚、视黄醇、甘草类黄酮、光果甘草根提取物、槲皮素、槲皮苷、黄芩苷、黄芩素、水飞蓟素、山奈酚、泛醌、芦荟苦素、光甘草定、五羟黄酮、四氢胡椒碱、紫檀芪、橙皮苷、积雪草苷、水杨酸和阿魏酸。
4.根据权利要求3所述的用途,其中所述脂质体组合物包含选自下述的活性成分:苯乙基间苯二酚、白藜芦醇和花榈木树皮提取物。
5.一种脂质体组合物,其包含活性成分、硬脂酰谷氨酸钠和月桂酰肌氨酸异丙酯。
6.根据权利要求5所述的脂质体组合物,其中硬脂酰谷氨酸钠的含量为0.1-3%,优选0.3-2%;月桂酰肌氨酸异丙酯的含量为1-20%,优选3-15%,更优选5-10%;基于所述脂质体组合物的总重量。
7.根据权利要求5所述的脂质体组合物,其中所述活性成分选自花榈木树皮提取物、白藜芦醇、姜黄素、神经酰胺、苯乙基间苯二酚、视黄醇、甘草类黄酮、光果甘草根提取物、槲皮素、槲皮苷、黄芩苷、黄芩素、水飞蓟素、山奈酚、泛醌、芦荟苦素、光甘草定、五羟黄酮、四氢胡椒碱、紫檀芪、橙皮苷、积雪草苷、水杨酸和阿魏酸。
8.根据权利要求7所述的脂质体组合物,其中所述活性成分选自苯乙基间苯二酚、白藜芦醇和花榈木树皮提取物。
9.根据权利要求5-8任一项所述的脂质体组合物,其包含大于5%、优选5-35%、更优选5-30%和最优选15-25%的活性成分,基于所述脂质体组合物的总重量。
10.根据权利要求9所述的脂质体组合物,其中所述脂质体组合物中活性成分的包封率为大于70%、优选大于80%、更优选大于90%、甚至大于95%,基于负载的活性成分的总重量。
11.根据权利要求5-10任一项所述的脂质体组合物,其具有100-500nm、优选100-300nm、更优选100-200nm和最优选100-120nm的粒径。
12.根据权利要求5-11任一项所述的脂质体组合物,其还包含多元醇、助乳化剂、膜修饰剂和水。
13.一种制备权利要求12所述的脂质体组合物的方法,其包括如下步骤:
a.在60-90℃、优选75-85℃的温度下,混合多元醇、硬脂酰谷氨酸钠、助乳化剂和水,得到均匀的混合物A;
b.在60-90℃、优选75-85℃的温度下,预混合月桂酰肌氨酸异丙酯、膜修饰剂、助乳化剂,然后将活性成分加入其中并在搅拌下进行进一步混合,得到均匀的混合物B;
c.在搅拌下,将混合物A和混合物B进行混合,得到均匀的混合物C;和
d.采用高压微射流均质机处理混合物C,得到脂质体组合物。
14.一种化妆品组合物,其包含权利要求5-12任一项所述的脂质体组合物。
15.根据权利要求14所述的化妆品组合物,其中所述脂质体组合物在化妆品组合物中的含量为3-20%,优选5-15%,基于所述化妆品组合物的总重量。
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