Zero-order release of polyphenolic drugs from dynamic, hydrogen-bonded LBL films.
Zero-order release of polyphenolic drugs from dynamic, hydrogen-bonded LBL films.
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DOI：
10.1039/c5sm02186c
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发表时间：
2016-01
期刊：
影响因子：
3.4
通讯作者：
Ya-nan Zhao;Jianjun Gu;Siyu Jia;Ying Guan;Yongjun Zhang
中科院分区：
文献类型：
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作者：
Ya-nan Zhao;Jianjun Gu;Siyu Jia;Ying Guan;Yongjun Zhang
能够以恒定速率或遵循零级动力学释放药物的药物载体可以导致对血浆药物浓度的最佳控制。在这里，我们证明了零级释放多酚类药物，包括单宁酸，表没食子儿茶素没食子酸酯，原花青素，和茶黄素-3 '-没食子酸酯，可以实现使用氢键层层膜作为药物载体。以多酚类药物为氢供体，聚乙二醇（PEG）为氢受体制备了该膜。由于药物和PEG以可逆的动态氢键结合，因此膜在水溶液中逐渐崩解，从而将药物释放到介质中。此外，由于PEG聚合物具有窄的分子量分布，因此膜以恒定速率崩解并释放多酚药物。除了允许零级释放之外，这里开发的药物载体还提供了多种调节药物释放速率的方法。药物释放速率随PEG分子量的减小而增大。更重要的是，可以使用外部刺激来调节释放速率。增加pH或温度导致加速药物释放，而盐的加入延迟药物释放。
Drug carriers capable of releasing drugs at a constant rate, or following zero-order kinetics, can lead to the best control of plasma drug concentration. Here we demonstrated that zero-order release of polyphenolic drugs, including tannic acid, epigallocatechin gallate, proanthocyanidins, and theaflavin-3'-gallate, could be achieved using hydrogen-bonded layer-by-layer films as the drug carrier. The films were fabricated using the polyphenolic drugs as hydrogen donors and polyethylene glycol (PEG) as the hydrogen acceptor. Because the drugs and PEG are bonded with reversible, dynamic hydrogen bonds, the films disintegrate gradually in aqueous solutions, and thus release the drugs into the media. Furthermore, because the PEG polymers have a narrow molecular weight distribution, the films disintegrate and release the polyphenolic drugs at a constant rate. Besides allowing for zero-order release, the drug carrier developed here also provides various ways to tune the drug release rate. The drug release rate increases with decreasing molecular weight of PEG. More importantly, the release rate could be tuned using external stimuli. Increasing the pH or temperature results in accelerated drug release, while the addition of salt retards the drug release.