CN114028265A - 一种超分子包埋水杨酸及其制备方法 - Google Patents
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Abstract
本发明涉及一种超分子包埋水杨酸及其制备方法。该超分子包埋水杨酸，按浓度百分比计，包括35%的水杨酸、45%的糊精以及20%的芝麻氨基酸。其中，糊精为超分子环糊精。该超分子包埋水杨酸的制备方法，包括以下步骤：(1)制备水杨酸溶液：(2)制备糊精水溶液；（3）制备芝麻氨基酸水溶液；(4)将水杨酸溶液、糊精水溶液以及芝麻氨基酸水溶液混合，此时水杨酸，糊精以及芝麻氨基酸在混合水溶液中浓度百分比计分别为35%、45%、20%，超声处理5min，静置90min后得超分子包埋水杨酸溶液。相比于现有技术中的水杨酸，本发明的超分子包埋水杨酸利用包裹技术解决了水杨酸难溶于水的问题，使得水杨酸能够稳定缓慢析出，不会对皮肤产生刺激。
Description
技术领域
本发明属于水杨酸技术领域，具体涉及一种超分子包埋水杨酸及其制备方法。
背景技术
水杨酸，又被称为邻羟基苯甲酸，是一种脂溶性的有机酸。水杨酸用途广泛，例如，可作为碱量法及碘量法滴定的标准试剂；在橡胶工业中用作防焦剂及生产紫外线吸收剂和发泡剂；在某些弱酸性电解液中作为添加剂，也可用作电镀或化学镀的络合剂；可作为化妆品防腐剂使用；作为医药工业的原料，用于制备阿斯匹林、水杨酸钠、水杨酰胺、止痛灵、水杨酸苯酯、血防-67等药物；在临床试验上可用来降低糖尿病患者长期并发心脏病的风险；水杨酸被广泛应用于外用涂抹类药物中，在许多皮肤护理产品中都使用水杨酸，可起到软化角质、杀菌、治疗粉刺等作用。水杨酸微溶于水，易溶于酒精，在皮肤护理产品中常加入大量酒精溶解水杨酸。但是酒精挥发快，当产品涂在皮肤上，酒精快速挥发，水杨酸从产品中析出来，水杨酸刺激性较强，对皮肤造成刺激。
发明内容
为了解决上述技术问题，本发明提供了一种超分子包埋水杨酸及其制备方法，该超分子包埋水杨酸利用包裹技术解决了水杨酸难溶于水的问题，使得水杨酸能够稳定缓慢析出，不会对皮肤产生刺激。
本发明的一种超分子包埋水杨酸的技术方案是：
一种超分子包埋水杨酸，按浓度百分比计，包括35%~45%的水杨酸、40%~50%的糊精以及20%~30%的芝麻氨基酸。
作为对上述技术方案的进一步改进，所述水杨酸的浓度为35%，所述糊精的浓度为45%，所述芝麻氨基酸的浓度为20%。
作为对上述技术方案的进一步改进，所述环糊精为超分子环糊精。
本发明的一种超分子包埋水杨酸的制备方法的技术方案是：
一种超分子包埋水杨酸的制备方法，包括以下步骤：
(1)制备水杨酸溶液：
(2)制备糊精水溶液；
(3)制备芝麻氨基酸水溶液；
(4)将水杨酸溶液、糊精水溶液以及芝麻氨基酸水溶液混合，此时水杨酸，糊精以及芝麻氨基酸在混合水溶液中浓度百分比计分别为35%~45%、40%~50%、20%~30%，超声处理5min，静置90min后得超分子包埋水杨酸溶液。
作为对上述技术方案的进一步改进，所述水杨酸的浓度为35%，所述糊精的浓度为45%，所述芝麻氨基酸的浓度为20%。
作为对上述技术方案的进一步改进，所述环糊精为超分子环糊精。
本发明提供了一种超分子包埋水杨酸及其制备方法，相比于现有技术，其有益效果在于：
本发明的超分子包埋水杨酸在水系溶剂中均具有良好的溶解性，通过超分子环糊精包裹可以降低水杨酸引起的刺激性，同时还能起到缓释的作用，使得功效更持久。同时，制本发明的超分子包埋水杨酸制备时，反应条件温和且操作简便，合成步骤简洁，后处理方便，制得的水杨酸包裹率高。相比于现有技术中的水杨酸，本发明的超分子包埋水杨酸利用包裹技术解决了水杨酸难溶于水的问题，使得水杨酸能够稳定缓慢析出，不会对皮肤产生刺激。
附图说明
图1是本发明的超分子包埋水杨酸制备方法的流程图；
图2是本发明的超分子包埋水杨酸稳定性测试结果图；
图3是本发明的超分子包埋水杨酸刺激性测试结果图；
图4是本发明的超分子包埋水杨酸抑制5-α还原酶活性测试结果图；
图5是本发明的超分子包埋水杨酸剥落角质测试结果图；
图6是本发明的超分子包埋水杨酸抑制痤疮测试结果图；
图7是本发明的超分子包埋水杨酸帮助恢复皮肤屏障测试结果图一；
图8是本发明的超分子包埋水杨酸帮助恢复皮肤屏障测试结果图二。
具体实施方式
下面结合附图及具体实施方式对本发明作进一步详细描述：
实施例一：
本发明提供了一种超分子包埋水杨酸，按浓度百分比计，包括35%的水杨酸、45%的糊精以及20%的芝麻氨基酸。其中，糊精为超分子环糊精。
本发明还提供了一种超分子包埋水杨酸，包括以下步骤：
(1)制备水杨酸溶液：
(2)制备糊精水溶液；
(3)制备芝麻氨基酸水溶液；
(4)将水杨酸溶液、糊精水溶液以及芝麻氨基酸水溶液混合，此时水杨酸，糊精以及芝麻氨基酸在混合水溶液中浓度百分比计分别为35%、45%、20%，超声处理5min，静置90min后得超分子包埋水杨酸溶液。
实施例二：
本发明提供了一种超分子包埋水杨酸，按浓度百分比计，包括35%的水杨酸、40%的糊精以及25%的芝麻氨基酸。其中，糊精为超分子环糊精。
本发明还提供了一种超分子包埋水杨酸，包括以下步骤：
(1)制备水杨酸溶液：
(2)制备糊精水溶液；
(3)制备芝麻氨基酸水溶液；
(4)将水杨酸溶液、糊精水溶液以及芝麻氨基酸水溶液混合，此时水杨酸，糊精以及芝麻氨基酸在混合水溶液中浓度百分比计分别为35%、40%、25%，超声处理5min，静置90min后得超分子包埋水杨酸溶液。
实施例三：
本发明的超分子包埋水杨酸稳定性测试：
为了描述，将本发明的超分子包埋水杨酸命名为Narsai20。如图2所示，本发明的超分子包埋水杨酸在-4℃~45℃具有良好的稳定性。
本发明的超分子包埋水杨酸刺激性测试：
分别配置浓度为0.25%、0.5%、0.75%、1%、1.25%的水杨酸溶液和Narsai20溶液，分别进行刺激性测试。测试结果如图3所示，相比于未包裹的水杨酸，本发明的超分子包裹水杨酸对皮肤的刺激性极低。
本发明的超分子包埋水杨酸抑制5-α还原酶活性测试：
取来自于人诱导多能干细胞的皮脂细胞培养，通过10μm睾酮在第7天诱导脂质生成。在第7、8、9天使用Narsai20进行处理，并在第11天进行DHT定量分析。
5-α还原酶活性诱导睾酮带写为二氢睾酮（DHT），DHT会导致皮脂异常。非那雄胺是一种著名的5-α还原酶抑制剂，能够显著降低DHT的合成。
由图4可以看出，1%的Narsai20能显著性抑制DHT合成，反映了Narsai20能够显著抑制5-α还原酶活性的活性。
本发明的超分子包埋水杨酸剥落角质测试：
使用1%的Narsai20或者含有1%的水杨酸容易热处理培养的人表皮角质形成细胞，室温下分别培养细胞10分钟、20分钟、30分钟和40分钟，收集培养孔中的培养基，计算脱落的细胞数量。
结果如图5所示，随着时间推移，Narsai20的剥脱功效逐渐加强，并且可以与1%浓度的水杨酸相比。
本发明的超分子包埋水杨酸抑制痤疮测试：
分别配置浓度为0.5%、1%、2%的超分子包埋水杨酸，在105CFU/ml痤疮丙酸杆菌培养基上，评估Narsai20处理48小时候的痤疮丙酸杆菌增殖情况。从图6可以看出，本发明的超分子包埋水杨酸能够有效抑制痤疮丙酸杆菌的增殖。
本发明的超分子包埋水杨酸帮助恢复皮肤屏障测试：
丝聚蛋白是维持完整的皮肤屏障功能和表皮水化功能的关键蛋白之一，丝聚蛋白的缺失可以导致屏障功能缺损、皮肤干燥以及瘙痒。组织激肽释放酶存在于颗粒层的细胞和角质层的细胞间隙中，可以使桥粒及桥黏素裂解，组织激肽释放酶的数量增加或者功能加强时，桥粒水解加速，使上皮角质细胞出现脱落异常，同时角质层的修复也出现异常，从而导致屏障的功能异常。
根据图7、图8可知，0.05%~3%的包裹水氧酸Narsai20可增加体外培养角质形成细胞的丝聚蛋白表达，抑制组织激肽释放酶表达，因此可能具有促进皮肤屏障功能恢复的作用。
以上所述仅为本发明的较佳实施例，并不用以限制本发明，凡在本发明的精神和原则之内，所作的任何修改、等同替换、改进等，均应包含在本发明的保护范围之内。
Claims (6)
1.一种超分子包埋水杨酸，其特征在于，按浓度百分比计，包括35%~45%的水杨酸、40%~50%的糊精以及20%~30%的芝麻氨基酸。
2.根据权利要求1所述的超分子包埋水杨酸，其特征在于，所述水杨酸的浓度为35%，所述糊精的浓度为45%，所述芝麻氨基酸的浓度为20%。
3.根据权利要求2所述的超分子包埋水杨酸，其特征在于， 所述环糊精为超分子环糊精。
4.一种超分子包埋水杨酸的制备方法，其特征在于，包括以下步骤：
(1)制备水杨酸溶液：
(2)制备糊精水溶液；
(3)制备芝麻氨基酸水溶液；
(4)将水杨酸溶液、糊精水溶液以及芝麻氨基酸水溶液混合，此时水杨酸，糊精以及芝麻氨基酸在混合水溶液中浓度百分比计分别为35%~45%、40%~50%、20%~30%，超声处理5min，静置90min后得超分子包埋水杨酸溶液。
5.根据权利要求4所述的超分子包埋水杨酸的制备方法，其特征在于，所述水杨酸的浓度为35%，所述糊精的浓度为45%，所述芝麻氨基酸的浓度为20%。
6.根据权利要求4所述的超分子包埋水杨酸的制备方法，其特征在于，所述环糊精为超分子环糊精。
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