<br>使用 pH 敏感聚合物薄膜电控药物释放†,Nanoscale

当前位置： X-MOL 学术 › Nanoscale › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

使用 pH 敏感聚合物薄膜电控药物释放†
Nanoscale ( IF 5.8 ) Pub Date : 2018-05-15 00:00:00 , DOI: 10.1039/c8nr02602e
S Ephraim Neumann ₁ , Christian F Chamberlayne , Richard N Zare

Affiliation

允许药物在空间和时间上受控释放的药物递送系统（DDS）在药物递送领域特别受关注。这些系统为单独定制药物剂量创造了机会，并通过将初始药物剂量定位到感兴趣的器官来减少副作用。我们提出了一种生物可吸收纳米复合膜形式的电响应 DDS，它在低电压（<−2 V）下工作。该方法基于在电极表面以电化学方式产生局部pH变化，以诱导用作载体材料的pH敏感聚合物溶解。我们之前使用聚（甲基丙烯酸甲酯-共-甲基丙烯酸）（共-PMMA）共聚物进行了这一概念验证，该共聚物在商业上以Eudragit S100（EGT）的形式销售。然而，由于 EGT 在 pH 值高于 7 时可溶，因此实验在等渗盐水溶液（pH ∼ 6.4）中进行。在这项工作中，我们合成了具有多种单体比例的共聚PMMA，以将共聚物的溶解度转移到更高的pH值，并开发了一种可以在生理相关条件下使用的聚合物。通过显示具有不同参数（如大小、疏水性和pKa _）的不同药物分子的受控释放，证明了该系统的通用性。荧光素（一种亲水性模型化合物）、美洛昔康（一种疏水性抗关节炎药物）、姜黄素（一种具有抗癌治疗潜力的小分子）和胰岛素（一种用于治疗低血糖的多肽激素）都可以按需释放，且泄漏最小。所达到的载药量为共聚物重量的~32 wt%。

"点击查看英文标题和摘要"

Electrically controlled drug release using pH-sensitive polymer films†

Drug delivery systems (DDS) that allow spatially and temporally controlled release of drugs are of particular interest in the field of drug delivery. These systems create opportunities for individually tailored doses of drugs to be administered as well as reduce side effects by localizing the initial drug dose to the organ of interest. We present an electroresponsive DDS in the form of a bioresorbable nanocomposite film which operates at low voltages (<−2 V). The method is based on electrochemically generating local pH changes at an electrode surface to induce dissolution of a pH-sensitive polymer, which is used as the carrier material. We previously demonstrated this proof-of-concept using a poly(methyl methacrylate-co-methacrylic acid) (co-PMMA) copolymer commercially marketed as Eudragit S100 (EGT). However, as EGT is soluble at a pH above 7, experiments were performed in isotonic saline solutions (pH ∼ 6.4). In this work, we have synthesized co-PMMA with a variety of monomer ratios to shift the solubility of the copolymer to higher pH values, and developed a polymer that can be used under physiologically relevant conditions. The generalizability of this system was demonstrated by showing controlled release of different drug molecules with varying parameters like size, hydrophobicity, and pK_a. Fluorescein, a hydrophilic model compound, meloxicam, a hydrophobic anti-arthritic medication, curcumin, a small molecule with anti-cancer therapeutic potential, and insulin, a polypeptide hormone used in the treatment of hypoglycemia, could all be released on demand with minimal leakage. The drug loading achieved was ∼32 wt% by weight of the co-polymer.

更新日期：2018-05-15

点击分享查看原文

点击收藏

公开下载

阅读更多本刊新发论文本刊介绍/投稿指南