CN113616563B - 一种工业***提取物组合物脂质体及其制备方法与应用 - Google Patents
一种工业***提取物组合物脂质体及其制备方法与应用 Download PDFInfo
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Abstract
本发明公开了一种工业***提取物组合物脂质体及其制备方法与应用。该工业***提取物组合物脂质体包括以下按质量百分含量计的原料:0.1‑5%积雪草提取物,0.1‑5%马齿苋提取物,0.1‑5%芍药提取物,0.1‑5%工业***提取物,1‑10%氢化卵磷脂,1‑10%氢化蓖麻油,0.1‑2%椰油基‑磺基甜菜碱,1‑5%的0.5%HA玻尿酸,1‑10%甘油,0.5‑5%大豆卵磷脂,0.5‑10%海藻糖,0.5‑2%维生素E,余量为去离子水。其具有稳定性高、溶解性好、抗炎、舒敏、祛痘和保湿修复的特性,其中的活性成分可以突破皮肤屏障,改善效果显著,具有良好的应用前景。
Description
技术领域
本发明具体涉及一种工业***提取物组合物脂质体及其制备方法与应用。
背景技术
完整的皮肤屏障能够抵御外界细菌、刺激物、紫外线进入,同时具有保湿、抑菌及调节抗炎作用;反之皮肤屏障受损无法抵御外界的刺激物或细菌进入皮肤,保湿功能明显下降,无法有效抑制细菌的生长。敏感肌肤其根本原因在于皮肤屏障受损,进而引发自身***修复不完善,经表皮去离子水分丢失加大,破坏细胞间平衡最终导致皮肤抵抗力下降,容易出现干燥、过敏、细菌感染、湿疹皮炎、红血丝、痤疮等皮肤疾病,严重影响日常的生活质量。
工业***提取物是从天然绿色植物工业***花、叶、茎、籽中提取出的混合物。目前,人们已从***植株中分离出了百余种物质,主要含***素类化合物,其主要活性成分为***二酚(CBD)。因具有独特的消炎和对损伤细胞的修复作用,***二酚越来越受到人们的重视。此外工业***提取物还含有多种不饱和脂肪酸、植物甾醇等。药理研究表明工业***提取物具有保湿、抗炎、舒缓镇痛、抑菌等作用;能够修复肌肤屏障;改善皮炎、痤疮、皮脂溢;此外可显著减少脸颊皮脂含量和红斑,维持肌肤稳态的同时显著改善皮肤过敏。
但是,工业***提取物为油溶性材料,其水溶性较低,且性状不稳定,容易受到光照、温度、湿度等的影响,将其直接应用于产品中具有储存成本高,货架周期短等特点,这使得工业***提取物的使用受到了限制。因此,亟需开发一种以舒敏、祛痘、保湿修复功效为核心的稳定性高、溶解性好、易透皮吸收的工业***提取物相关产品。
发明内容
为了克服现有技术存在的缺点与不足,本发明的第一目的在于提供一种工业***提取物组合物脂质体。
本发明的第二目的在于提供通过上述工业***提取物组合物脂质体的制备方法。
本发明的第三目的在于提供通过上述工业***提取物组合物脂质体的应用。
本发明的目的通过如下技术方案实现:
一种工业***提取物组合物脂质体,包括以下按质量百分含量计的原料:
0.1-5%积雪草提取物,0.1-5%马齿苋提取物,0.1-5%芍药提取物,0.1-5%工业***提取物,1-10%氢化卵磷脂,1-10%氢化蓖麻油,0.1-2%椰油基-磺基甜菜碱,1-5%的0.5%HA玻尿酸,1-10%甘油,0.5-5%大豆卵磷脂,0.5-10%海藻糖,0.5-2%维生素E,余量为去离子水。
优选地,所述的工业***提取物组合物脂质体包括以下按质量百分含量计的原料:
0.5-2%积雪草提取物,0.5-3%马齿苋提取物,0.1-3%芍药提取物,0.1-3%工业***提取物,4-6%氢化卵磷脂,4-6%氢化蓖麻油,0.5-2%椰油基-磺基甜菜碱,1-5%的0.5% HA玻尿酸,4-6%甘油,0.8-2%大豆卵磷脂,1-3%海藻糖,1-2%维生素E,余量为去离子水。
更优选地,所述的工业***提取物组合物脂质体包括以下按质量百分含量计的原料:
0.5%积雪草提取物,1%马齿苋提取物,2%芍药提取物,3%工业***提取物,5%氢化卵磷脂,4%氢化蓖麻油,1.5%椰油基-磺基甜菜碱,4%的0.5%HA玻尿酸,4%甘油,0.8%大豆卵磷脂,2%海藻糖,1.5%维生素E,余量为去离子水。
上述工业***提取物组合物脂质体的制备方法,包括以下步骤:
步骤一:将氢化卵磷脂、氢化蓖麻油、大豆卵磷脂、维生素E在45-60℃混合均匀,得到组分A;
步骤二:将去离子水、海藻糖、0.5%HA玻尿酸、甘油、椰油基-磺基甜菜碱、工业***提取物、芍药提取物、马齿苋提取物、积雪草提取物在45-60℃混合均匀,得到组分B;
步骤三:将A组分和B组分混合均匀后进行均质处理;
步骤四:使用挤出设备,将得到的溶液依次通过0.6μm、0.45μm和0.22μm的聚碳酸酯膜进行过滤挤出,最终得到均匀、稳定的组合物脂质体。
优选地,所述步骤一和步骤二中混合温度为50-60℃。
更优选地,所述步骤一和步骤二中混合温度为50℃。
优选地,所述步骤三中均质处理的压力为20000-30000PSI,8-10次循环。
更优选地,所述步骤三中均质处理的压力为20000PSI。
本发明与现有技术相比具备以下优点:
(1)本发明将油溶性原材料工业***提取物包裹于脂质体组合物中,提高了工业***提取物的水溶性和稳定性,解决了工业***提取物难溶于水、稳定性差等问题,提高了其产品的货架周期;
(2)本发明的工业***提取物组合物脂质体选取亲脂性材料,更有利用产品吸收,提高了工业***的生物利用率,与未包裹的工业***提取物相比,本发明工业***提取物组合物脂质体具有更为显著的作用,如抑菌、抗炎、改善皮肤屏障,减少经皮水分的流失,改善皮肤发红或者红血丝等;
(3)本发明所用材料天然无公害,不会对人体和环境产生不利影响;
(4)本发明提供的工业***提取物组合物脂质体兼顾舒敏、祛痘、保湿修复和杀菌等多种功效,并且各种提取物的各组分之间还具有协同的功效,使各组分的作用发挥到最大。
(4)本发明的工业***提取物组合物脂质体制备方法简单,产品稳定易得,有利于大规模机械化生产。
具体实施方式
下面对本发明作进一步的说明,但不以任何方式对本发明加以限制,基于本发明教导所作的任何变换或替换,均属于本发明的保护范围。
除非另有定义,本发明中所使用的所有科学和技术术语具有与本发明涉及技术领域的技术人员通常理解的相同的含义。
下述实施例和对比例中:
工业***提取物购自元贝贝生物科技有限公司,货号为YBB-1152;
积雪草提取物购自山西宏达植物化工有限公司,货号为JXC-191028;
马齿苋提取物购自西安佰斯特生物科技有限公司,货号为best206;
芍药提取物购自陕西富特科生物科技有限公司,货号为F0157S;
水解透明质酸钠购自华熙生物,货号为4d00。
实施例1
一种工业***提取物组合物脂质体(工业***提取物含量为3%),以质量分数计,包含成分如下表1所示:
表1配方
具体制备方法如下:
步骤一:将氢化卵磷脂、氢化蓖麻油、大豆卵磷脂、、维生素E在45-60℃混合均匀,得到组分A;
步骤二:将去离子水、海藻糖、0.5%HA玻尿酸、甘油、椰油基-磺基甜菜碱、工业***提取物、芍药提取物、马齿苋提取物、积雪草提取物在45-60℃混合均匀,得到组分B;
步骤三:将A组分和B组分混合均匀后通过超高压微射流均质器,均质压力为20000PSI,8-10次循环。
步骤四:使用挤出设备,将得到的溶液依次通过0.6μm、0.45μm和0.22μm的聚碳酸酯膜进行过滤,最终得到均匀、稳定的脂质体组合物。
实施例2
一种工业***提取物组合物脂质体(工业***提取物含量为3%),以质量分数计,包含成分如下表2所示:
表2配方
具体制备方法与实施例1相同。
实施例3
一种工业***提取物组合物脂质体(工业***提取物含量为3%),以质量分数计,包含成分如下表3所示:
表3配方
具体制备方法与实施例1相同。
对比例1
本对比例组合物脂质体组分中不包括芍药提取物、马齿苋提取物、积雪草提取物,所含工业***提取物的质量百分含量为3%,其它同实施例2。
具体制备方法参考实施例1。
对比例2
本对比例组合物脂质体组分中不包括工业***提取物,所含芍药提取物质量百分含量为2%、马齿苋提取物质量百分含量为1%、积雪草提取物质量百分含量为0.5%,其它同实施例2。
具体制备方法参考实施例1。
效果实施例1
金黄色葡萄球菌抑菌活性研究
1、试验材料:
实施例1~3和对比例1制备得到的组合物脂质体,对比例2制备得到的不含工业***提取物组合物脂质体。
2、试验方法:
菌种活化:将冻存的金黄色葡萄球菌(ATCC 27217)接种至液体培养基中,用封口膜封口后放入厌氧盒。放入一次性厌氧袋,于37℃恒温细菌培养箱中厌氧培养48h。用接种环蘸取少许菌液,以平板划线法涂布于固体琼脂平板,倒置放入厌氧盒中,并放入新的一次性厌氧袋,于37℃恒温细菌培养箱中厌氧培养48h。
菌液制备:于固体琼脂平板上挑取单菌落于15mL液体培养基中,用封口膜封口后放入厌氧盒。放入一次性厌氧袋,于37℃恒温细菌培养箱中厌氧培养48h。
牛津杯法步骤:将活化的菌悬液离心,沉淀用无菌生理盐去离子水重悬至菌浓度约107CFU/mL;取100μL菌悬液涂布于固体琼脂平板上,用镊子夹取无菌牛津杯放至培养基表面,轻轻按压使牛津杯与培养基完全接触(每个平板放置3个牛津杯),向牛津杯中加入200μL样品。将平板放入厌氧培养盒中,培养7天后观察抑菌圈大小,测定抑菌圈直径。实验用无菌去离子水作阴性及空白对照。结果如下表4所示。
表4样品稀释倍数及抑菌结果
分析表5可以看出,本发明实施例1-3所制备的含工业***提取物组合物脂质体,均表现出明显的抑制金黄色葡萄球菌的作用。尤其是与对比例1与对比例2相比,实施例2制备得到的脂质体抑菌效果更突出。可以预测本发明实施例制得的含工业***提取物组合物脂质体可以更有效地祛痘,预防痘肌和痤疮等肌肤问题。
效果实施例2
对2,4—二硝基氯苯(DNCB)所致小鼠Ⅳ型***反应的治疗作用
1、试验材料:
实施例1~3和对比例1制备得到的含工业***提取物组合物脂质体,对比例2制备得到的不含工业***提取物组合物脂质体。
2、试验方法:
取小鼠40只,随机分为5组,每组8只:空白组、本发明实施例1~3、对比例1~2制备得到的组合物脂质体组、氢化可的松乳膏组。
实验第1天,各组每只小鼠皮下注射3.5%DNCB-丙酮油溶液0.04mL致敏。实验第7天,于每只小鼠右耳正反两面均涂上1%DNCB-丙酮油溶液0.02mL进行试验。实验第8天,空白组各小鼠右耳分别外涂75%乙醇溶液,其余组分别涂对应的药物,每天2次,连续4天。最后一次涂抹后24小时处死小鼠,从左右耳分别用6mm打孔器取下耳片,在分析天平上称重,以两耳片重量之差作为Ⅳ型***反应强度。在HE染色切片下观察耳片病例改变,光镜下用网格目测微尺计数每mm2的炎性细胞数(包括单一核细胞和多形核白细胞)。结果如下表5所示。
表5各药物对DNCB致小鼠Ⅳ型***反应的影响
分析表6可以看出,本发明实施例1-3所制备的含工业***提取物组合物脂质体对皮炎模型小鼠的耳肿胀具有明显抑制作用,尤其是实施例2制备得到的工业***脂质体组合物治疗效果更突出,且作用显著优于对比例1与对比例2。此外本发明实施例1-3所制备的含工业***提取物组合物脂质体可明显减少皮肤受损部位炎性细胞浸润,与仅包裹工业***的脂质体相比具有更为显著的抗炎作用。说明本发明脂质体具有更显著的舒缓,抗过敏功效。
上述实施例为本发明较佳的实施方式,但本发明的实施方式并不受上述实施例的限制,其他的任何未背离本发明的精神实质与原理下所作的改变、修饰、替代、组合、简化,均应为等效的置换方式,都包含在本发明的保护范围之内。
Claims (3)
1.一种工业***提取物组合物脂质体,其特征在于:包括以下按质量百分含量计的原料:
0.5%积雪草提取物,1%马齿苋提取物,2%芍药提取物,3%工业***提取物,5%氢化卵磷脂,4%氢化蓖麻油,1.5%椰油基-磺基甜菜碱,4%浓度为0.5%的玻尿酸,4%甘油,0.8%大豆卵磷脂,2%海藻糖,1.5%维生素E,余量为去离子水。
2.权利要求1所述的工业***提取物组合物脂质体的制备方法,其特征在于:包括以下步骤:
步骤一:将氢化卵磷脂、氢化蓖麻油、大豆卵磷脂、维生素E在45-60℃混合均匀,得到组分A;
步骤二:将去离子水、海藻糖、浓度为0.5%的玻尿酸、甘油、椰油基-磺基甜菜碱、工业***提取物、芍药提取物、马齿苋提取物、积雪草提取物在45-60℃混合均匀,得到组分B;
步骤三:将A组分和B组分混合均匀后进行均质处理;
步骤四:使用挤出设备,将得到的溶液依次通过0.6μm、0.45μm和0.22μm的聚碳酸酯膜进行过滤挤出,最终得到均匀、稳定的组合物脂质体。
3.根据权利要求2所述的工业***提取物组合物脂质体的制备方法,其特征在于:
所述步骤一和步骤二中混合温度为50-60℃;
所述步骤三中均质处理的压力为20000-30000PSI,8-10次循环。
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