CN103169983A - 多酚类化合物(药物)缓释方法 - Google Patents
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Abstract
本发明公开了一种新的层层组装药物释放技术。利用多酚类化合物(药物)分子作为氢键给体与聚N-乙烯基吡喏烷酮等氢键受体进行基于氢键的层层组装，直接将药物组装(附载)到层层组装膜中。由于氢键的可逆性，组装膜在水中逐渐解离，从而释放出药物。
Description
技术领域
本发明涉及多酚类化合物，特别是多酚类药物的缓释技术，属于生物医药技术领域。
背景技术
多酚类化合物具有很强的抗氧化作用。研究表明它们具有防止衰老的作用，并能预防许多常见疾病。作为抗氧化剂，它们能有效地保护细胞和人体中重要的化学分子，如DNA、蛋白质、酶等免受自由基的破坏，同时防止活性原子对人体组织的损坏。多酚还能阻碍一些肿瘤生长所需酶的作用，使一些促进肿瘤生长的物质失活，因此具有抗肿瘤的功效。以茶多酚为代表的多酚类药物的药理作用包括：(1)强烈的消除有害自由基的作用；(2)抗衰老作用：(3)抗辐射作用；(4)对癌细胞的抑制作用；(5)抗菌、杀菌作用；(6)对艾滋病病毒的抑制作用，等。
层层组装方法是一种制备高分子薄膜的组装方法。如果两种高分子之间具有可以相互作用的基团，当基片在这两种高分子溶液中交替浸泡的时候，就可以将这两种高分子组装到基片上。两种高分子之间的相互作用可为静电力、氢键、共价键、疏水相互作用、电荷转移相互作用等等。层层组装膜已被用于药物控释。一种方法是用层层组装方法制备微胶囊，并将药物包埋在微胶囊的囊芯中。药物通过构成囊壁的层层组装膜扩散而被释放。通过调节层层组装膜的可渗透性能可控制药物释放速度。这里层层组装膜主要起到扩散屏障的作用。第二种方法是将药物通过吸附附载到层层组装膜中，药物通过扩散而释放。第三种方法是药物与可降解高分子组装成层层组装膜，通过可降解高分子的降解，达到释放药物的目的。
发明内容
本发明提出一种新的层层组装药物释放技术。本发明利用多酚类化合物(药物)分子作为氢键给体与聚N-乙烯基吡喏烷酮等氢键受体进行基于氢键的层层组装，直接将药物组装(附载)到层层组装膜中。由于氢键的可逆性，这样的组装膜在水中将会逐渐解离，从而释放出药物。(图1)
本发明中的多酚类化合物为具有多个苯酚基团的任意化合物，特别是具有药理作用的多酚类药物，以及具有保健作用的天然多酚化合物，如茶多酚等。
本发明中作为氢键受体的高分子包括聚N-乙烯基吡咯烷酮、聚环氧乙烷、环氧乙烷-环氧丙烷共聚物、聚乙二醇等合成高分子，以及羟丙基纤维素等天然高分子。
附图说明
图1、多酚类化合物或药物作为氢键给体的层层组装膜在水溶液中的解离。随着膜的解离，多酚类化合物或药物被释放。
图2、不同层数的聚N-乙烯基吡喏烷酮/单宁酸层层自组装膜的紫外-可见吸收光谱。
图3、单宁酸在不同pH值的0.050M磷酸缓冲溶液中的释放动力学。
具体实施方式
下面结合附图和实施例对本发明作进一步说明。但本发明并不限于下列实施例。
实施例1
洁净基片(石英、玻璃或抛光硅片)在0.1wt％聚N-乙烯基吡喏烷酮溶液中浸泡10分钟，水洗4分钟，然后在0.1wt％单宁酸溶液中浸泡10分钟，再水洗4分钟。重复这一交替组装过程即得到聚N-乙烯基吡喏烷酮/单宁酸层层自组装膜。
用紫外光谱仪测定上述自组装膜的紫外-可见光谱，如图2所示。组装膜在278nm处的吸收随组装层数的增加而增加。
将上述自组装膜浸泡在不同pH值的0.050M磷酸缓冲溶液中。单宁酸的释放动力学如图3所示。
实施例2
洁净基片(石英、玻璃或抛光硅片)在0.1wt％聚N-乙烯基吡喏烷酮溶液中浸泡10分钟，水洗4分钟，然后在0.1wt％儿茶素溶液中浸泡10分钟，再水洗4分钟。重复这一交替组装过程即得到聚N-乙烯基吡喏烷酮/儿茶素层层自组装膜。
用紫外光谱仪测定上述自组装膜的紫外-可见光谱，组装膜的紫外吸收随组装层数的增加而增加。将上述自组装膜浸泡在不同pH值的0.050M磷酸缓冲溶液中，儿茶素的释放动力学与实施例1类似。
实施例3
洁净基片(石英、玻璃或抛光硅片)在0.1wt％聚N-乙烯基吡喏烷酮溶液中浸泡10分钟，水洗4分钟，然后在0.1wt％花青素溶液中浸泡10分钟，再水洗4分钟。重复这一交替组装过程即得到聚N-乙烯基吡喏烷酮/花青素层层自组装膜。
用紫外光谱仪测定上述自组装膜的紫外-可见光谱，组装膜的紫外吸收随组装层数的增加而增加。将上述自组装膜浸泡在不同pH值的0.050M磷酸缓冲溶液中，花青素的释放动力学与实施例1类似。
Claims (3)
1.一种多酚类化合物，特别是多酚类药物的缓释方法，其特征在于将多酚类化合物作为氢键给体与氢键受体进行层层组装，利用氢键可逆性进行药物释放。
2.如权利要求1所述的多酚类化学物，包括任意的含多个苯酚基团的化合物。
3.如权利要求1所述的氢键受体，包括聚N-乙烯基吡咯烷酮、聚环氧乙烷、环氧乙烷-环氧丙烷共聚物、聚乙二醇等合成高分子，以及羟丙基纤维素等天然高分子。
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105582547A (zh) * | 2016-02-29 | 2016-05-18 | 南开大学 | 一种持续恒速释放药物的药物载体 |
| CN114191568A (zh) * | 2021-12-15 | 2022-03-18 | 山东大学 | 一种基于多酚的凝聚层颗粒制备方法 |
| CN114250053A (zh) * | 2021-12-30 | 2022-03-29 | 山东大学 | 一种多酚-聚乙二醇基低共熔胶粘剂的制备和使用方法 |
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2011
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105582547A (zh) * | 2016-02-29 | 2016-05-18 | 南开大学 | 一种持续恒速释放药物的药物载体 |
| CN114191568A (zh) * | 2021-12-15 | 2022-03-18 | 山东大学 | 一种基于多酚的凝聚层颗粒制备方法 |
| CN114191568B (zh) * | 2021-12-15 | 2023-10-20 | 山东大学 | 一种基于多酚的凝聚层颗粒制备方法 |
| CN114250053A (zh) * | 2021-12-30 | 2022-03-29 | 山东大学 | 一种多酚-聚乙二醇基低共熔胶粘剂的制备和使用方法 |
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