CN115227590A - 一种协同抗衰老阳离子脂质体及其制备方法与应用 - Google Patents
一种协同抗衰老阳离子脂质体及其制备方法与应用 Download PDFInfo
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Abstract
本发明公开了一种协同抗衰老阳离子脂质体及其制备方法与应用，所述脂质体包含活性成分、脂质膜材和包衣材料，其中活性成分包括白藜芦醇和肌肽，脂质膜材包括磷脂和胆固醇，包衣材料为壳聚糖及改性壳聚糖。将白藜芦醇和肌肽分别包封于脂质体双分子层中和腔内，搅拌下将脂质体加入壳聚糖及改性壳聚糖水溶液中，室温孵育即得。本发明首次同时负载白藜芦醇与肌肽，二者协同发挥抗衰老作用，壳聚糖及改性壳聚糖包衣既可以减少活性成分的泄漏，又具有缓释作用。本产品稳定性好、成本低、操作简单、安全性高，抗衰老效果强，可直接作为化妆品使用或者添加到化妆品中使用。
Description
技术领域
本发明涉及化妆品技术领域，具体涉及一种协同抗衰老阳离子脂质体及其制备方法与应用。
背景技术
皮肤，作为机体与外界环境直接接触的第一道屏障，参与并维持整个机体与外界环境的统一，使机体内各组织器官免受外界机械性、物理性、化学性或生物性刺激。然而，随着时间流逝和外界环境的不断损伤，皮肤抵御能力逐渐减弱，一系列皮肤问题由此产生，例如：粗糙、暗沉、皱纹和松弛等，这些特征集中体现为皮肤衰老，这是一个是多因素、多机制、复杂的慢性过程。
随着人类社会发展和生活水平的提升，人们对皮肤状态的重视程度和对美的追求也不断提高，皮肤细腻有弹性、纹理清晰无皱纹成为了大家的期待，因此，皮肤衰老成为了急需解决的焦点问题，以抗衰老为主导作用的化妆品也越来越受到人们的欢迎。
白藜芦醇(Resveratrol)，来源于葡萄、虎杖、桑葚等植物，是一种抗氧化活性很强的蒽醌萜类多酚物质。肌肽(Carnosine)是由β-丙氨酸和L-组氨酸组成的二肽，有着很强的抗糖化功效，将二者联用可从不同角度发挥协同抗衰老作用，效果更强。
脂质体是磷脂分散于水相时，分子疏水尾部聚在一起，避开水相，而亲水头部暴露于水相，形成的具有双分子层结构的封闭囊泡。根据其结构特征，可将脂溶性药物分散于磷脂双分子层的疏水夹层中提高难溶性药物的溶解度，将水溶性药物包于双分子层内核，实现同时包载脂溶性和水溶性成分，且脂质体具有良好的生物相容性和生生物安全性，已成为纳米递药系统中极受关注的热点。但传统脂质体尚存在易泄漏、稳定性差等缺点。通过对脂质体进行包衣可有效提高脂质体稳定性，这对抗衰老脂质体化妆品的开发具有重要意义。
发明内容
本发明的目的是提供一种壳聚糖及改性壳聚糖修饰的白藜芦醇和肌肽共载脂质体的制备方法，以解决现有技术不足。本发明首次验证白藜芦醇和肌肽联用的协同抗衰老效果，同时将二者负载于脂质体，不仅有效地提高了白藜芦醇溶解性，且较小的粒径使其更易穿过皮肤。壳聚糖，作为一种天然多糖，包裹于脂质体外，不但可防止药物泄漏，且其自身带有的正电荷能增加与带负电荷皮肤的亲和力，使整体与皮肤的结合更紧密，与此同时，壳聚糖的促渗作用也增加了脂质体的透皮深度。
为了实现上述技术目的，本发明的技术方案如下：
本发明通过实验证实了白藜芦醇和肌肽联用的协同抗衰老效果。
本发明提供一种协同抗衰老阳离子脂质体，所述脂质体包括药物活性成分、脂质膜材和包衣材料，其中药物活性成分包括白藜芦醇和肌肽，脂质膜材包括磷脂和胆固醇，包衣材料为壳聚糖及改性壳聚糖。
本发明提供上述脂质体的制备方法，包括如下步骤：
(1)将配方比例的磷脂、胆固醇和白藜芦醇溶解在有机溶剂中，除去溶剂后加入溶有配方比例肌肽的水溶液，充分水化，均一粒径，得到白藜芦醇和肌肽共载脂质体。
(2)在磁力搅拌下，将脂质体加入壳聚糖或改性壳聚糖水溶液中，室温孵育。得到修饰后的白藜芦醇和肌肽共载脂质体。
本发明的壳聚糖或改性壳聚糖修饰的白藜芦醇和肌肽共载脂质体，是一种粒径在约130nm的正电荷脂质体。
与现有技术相比，本发明取得的有益技术效果：
验证了白藜芦醇和肌肽联用的协同抗衰老效果。
解决了白藜芦醇溶解度低和稳定性差的问题。
制备的脂质体稳定性好、与皮肤亲和力强、渗透效果好且具有缓释的功能。
方法成本低、操作简单、反应条件温和、生物安全性高。
附图说明
图1-6分别是本发明实施例1制得产品SOD、MDA、HYP、GSH、CAT和AGEs指标测定结果图。
具体实施方式
下面将本发明实施例中的技术方案作进一步清楚、完整地描述，但这些实施例并不限制本发明的保护范围。
实施例1
分别称取蛋黄卵磷脂200mg、胆固醇50mg和白藜芦醇20mg，使其质量比为20：5：2，置茄形瓶中，加入20mL无水乙醇，充分溶解，40℃旋转蒸发1小时至溶剂挥发完全，再加入20mL肌肽水溶液(0.5mg/mL)，充分水化1小时，将得到的脂质体混悬液用脂质体挤出器(100nm膜)反复挤压，得白藜芦醇和肌肽共载脂质体。
按白藜芦醇和肌肽共载脂质体溶液与壳聚糖水溶液体积比为1：2，在磁力搅拌器搅拌下，将白藜芦醇和肌肽共载脂质体逐滴加入壳聚糖水溶液中，室温孵育2小时，得到壳聚糖修饰的白藜芦醇和肌肽共载脂质体。
实施例2
分别称取大豆卵磷脂200mg、胆固醇40mg和白藜芦醇20mg，使其质量比为10：2：1，置茄形瓶中，加入20mL乙醚，充分溶解，40℃旋转蒸发2小时至溶剂挥发完全，再加入20mL肌肽水溶液(1mg/mL)，充分水化2小时，将得到的脂质体混悬液用高压匀质机匀质，得到白藜芦醇和肌肽共载脂质体。
按白藜芦醇和肌肽共载脂质体溶液与邻苯二酚壳聚糖水溶液体积比为1：2，在磁力搅拌器搅拌下，将白藜芦醇和肌肽共载脂质体逐滴加入邻苯二酚壳聚糖水溶液中，室温孵育2小时，得到邻苯二酚壳聚糖修饰的白藜芦醇和肌肽共载脂质体。
实施例3
分别称取氢化卵磷脂200mg、胆固醇40mg和白藜芦醇15mg，使其质量比为40：8：3，置茄形瓶中，加入20mL氯仿，充分溶解，40℃旋转蒸发1小时至溶剂挥发完全，再加入20mL肌肽水溶液(0.33mg/mL)，充分水化1小时，将得到的脂质体混悬液用超滤膜过滤，得到白藜芦醇和肌肽共载脂质体。
按白藜芦醇和肌肽共载脂质体溶液与巯基壳聚糖水溶液体积比为1：2，在磁力搅拌器搅拌下，将白藜芦醇和肌肽共载脂质体逐滴加入巯基壳聚糖水溶液中，室温孵育2小时，得到巯基壳聚糖修饰的白藜芦醇和肌肽共载脂质体。
实施例4
分别称取蛋黄卵磷脂150mg、胆固醇50mg和白藜芦醇20mg，使其质量比为15：5：2，置茄形瓶中，加入20mL甲醇，充分溶解，40℃旋转蒸发1小时至溶剂挥发完全，再加入20mL肌肽水溶液(2mg/mL)，充分水化1小时，将得到的脂质体混悬液用脂质体挤出器(100nm膜)反复挤压，得到白藜芦醇和肌肽共载脂质体。
按白藜芦醇和肌肽共载脂质体溶液与邻苯二酚壳聚糖水溶液体积比为1：2，在磁力搅拌器搅拌下，将白藜芦醇和肌肽共载脂质体逐滴加入邻苯二酚壳聚糖水溶液中，室温孵育2小时，得到邻苯二酚壳聚糖修饰的白藜芦醇和肌肽共载脂质体。
实施例5
分别称取大豆卵磷脂200mg、胆固醇60mg和白藜芦醇20mg，使其质量比为10：3：1，置茄形瓶中，加入20mL乙腈，充分溶解，40℃旋转蒸发1小时至溶剂挥发完全，再加入20mL肌肽水溶液(3mg/mL)，充分水化1小时，将得到的脂质体混悬液用超滤膜过滤，得到白藜芦醇和肌肽共载脂质体。
按白藜芦醇和肌肽共载脂质体溶液与壳聚糖水溶液体积比为1：2，在磁力搅拌器搅拌下，将白藜芦醇和肌肽共载脂质体逐滴加入壳聚糖水溶液中，室温孵育2小时，得到壳聚糖修饰的白藜芦醇和肌肽共载脂质体。
药物包封率检测：
采用高效液相色谱法检测实施例1得到的脂质体中白藜芦醇和肌肽含量。
检测结果显示，实施例1中，白藜芦醇包封率分别为79.6％，肌肽包封率分别为71.5％，药物包封效果良好。
功效测试：
35只白色雌性豚鼠，清洁级，鼠龄6-8周，体重280±20g，随机分成对照组，模型组，白藜芦醇组，肌肽组，混合药物组，脂质体组，邻苯二酚壳聚糖脂质体组，每组5只，用脱毛膏脱去背部表面毛发，暴露皮肤，除空白组，给予UVA和UVB联合照射7天，继续以低剂量照射并给药处理，21天后，剪取背部皮肤组织，加生理盐水制成10％组织混悬液，用衰老相关试剂盒(SOD，AGEs，MDA)测定相关指标含量。检测结果显示，抗衰老效果由强到弱为：邻苯二酚壳聚糖脂质体组>脂质体组>混合药物组>肌肽组>白藜芦醇组，这证明了两种药物在体内的协同效果，同时在赋予药物剂型和剂型改良后效果更佳，以上证明邻苯二酚壳聚糖修饰的白藜芦醇和肌肽共载脂质体是值得被开发的产品。
Claims (10)
1.一种协同抗衰老阳离子脂质体，其特征在于，所述脂质体的活性成分为白藜芦醇和肌肽，脂质膜材为磷脂和胆固醇，包衣材料为壳聚糖及改性壳聚糖。
2.根据权利要求1所述的一种协同抗衰老阳离子脂质体，其特征在于，所述药物活性成分白藜芦醇和肌肽质量比为1：10～10：1，优选2：1。
3.根据权利要求1所述的一种协同抗衰老阳离子脂质体，其特征在于，所述磷脂、胆固醇、白藜芦醇和肌肽质量比为3～20：1～6：0.5～2：0.3～1，优选为20：5：2：1。
4.根据权利要求1所述的一种协同抗衰老阳离子脂质体，其特征在于，脂质膜材可选用蛋黄卵磷脂、大豆卵磷脂、氢化卵磷脂、合成磷脂和胆固醇。
5.根据权利要求1所述的一种协同抗衰老阳离子脂质体，其特征在于，包衣材料可选用壳聚糖、邻苯二酚壳聚糖和巯基壳聚糖中的一种或多种。
6.权利要求2-5任一项所述抗衰老阳离子脂质体的制备方法，其特征在于，所述方法可采用薄膜分散法、薄膜超声法和薄膜分散-高压均质法。
7.根据权利要求6所述制备方法，其特征在于，包括以下步骤：
(1)按配方比例称取磷脂、胆固醇和白藜芦醇，加入至有机溶剂中，除去溶剂后，按照配方比例加入肌肽水溶液，充分水化，粒径均化，得负载白藜芦醇和肌肽的脂质体；
(2)将步骤(1)得到的脂质体，在磁力搅拌下，按体积比为1：1～1：5加入至壳聚糖或改性壳聚糖水溶液，室温孵育2小时。
8.根据权利要求7所述制备方法，其特征在于，步骤(1)中所述有机溶剂可选用无水乙醇、乙醚、氯仿、乙腈和甲醇中的任意一种或多种。
9.根据权利要求7所述制备方法，其特征在于，步骤(1)中均一粒径选用脂质体挤出器、高压均质或超滤膜过滤。
10.根据权利要求1所述的一种协同抗衰老阳性脂质体，其特征在于，将脂质体应用于化妆品，包括直接使用或添加至水、乳液、喷雾、面膜、精华和膏霜。
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