Oral drug delivery has been recognized as the most common and patient acceptant drug administration. In general, an ideal drug carrier for oral drug delivery should own high drug loading capacity, good biocompatibility, and especially the feature of avoiding drug delivery in stomach (acidic conditions) and promoting the drug release in intestine (neutral conditions). Generally, most of MOFs for drug carriers exhibit the normal pH response in which the drugs are more easily released in acidic condition because of the degradation of the framework or/and the weak host-guest interactions, so they are not suitable for oral drug delivery. Herein, we design and synthesize a new nitrogen heterocycle organic ligand H₂QDDA ((2E,2′E)-3,3′-(quinoline-5,8-diyl)diacrylic acid) and use it to construct its first Zr-based MOF (termed as ZJU-802). The anionic drug encapsulated ZJU-802 exhibit an uncommonly reverse pH response due to the incorporation of N sites in which the anionic drugs can be easily released at pH 7.4 while have a negligible release at pH 2.0 due to the enhanced host-guest interactions between the framework and anionic drugs. This reversed drug release is quite suitable for oral drug delivery. Further, high anionic drug loading capacities (>40%), low cytotoxicity and good biocompatibility of ZJU-802 were fully demonstrated by ¹H NMR, MTT assay and confocal microscopy imaging.

口服药物递送已被认为是最常见和患者可接受的药物管理方式。通常，用于口服药物递送的理想药物载体应具有高的药物负载能力，良好的生物相容性，尤其是具有避免在胃中递送药物（酸性条件）和促进在肠道中释放药物（中性条件）的特征。通常，用于药物载体的大多数MOF均显示正常的pH响应，其中由于骨架的降解或/和弱的宿主-客体相互作用，药物在酸性条件下更容易释放，因此它们不适合口服药物递送。本文中，我们设计并合成了一种新的氮杂环有机配体H ₂QDDA（（2E，2'E）-3,3'-（quinoline-5,8-diyl）diacrylic acid）并用于构建其第一个基于Zr的MOF（称为ZJU-802）。包封的ZJU-802阴离子药物由于掺入了N个位点，因此表现出不常见的反向pH响应，其中N阴离子在pH 7.4时很容易释放，而在pH 2.0时由于宿主-客体之间相互作用的增强，释放量可忽略不计。骨架和阴离子药物。这种反向的药物释放非常适合口服药物输送。此外，通过¹ H NMR，MTT分析和共聚焦显微镜成像充分证明了ZJU-802的高阴离子载药量（> 40％），低细胞毒性和良好的生物相容性。