Advanced Postsynthetic Modification of COF: Elevating Hydrophilicity for Efficient Doxorubicin Delivery

IF 4.7 Q2 MATERIALS SCIENCE, BIOMATERIALS

ACS Applied Bio Materials Pub Date : 2025-05-02 DOI:10.1021/acsabm.5c0043610.1021/acsabm.5c00436

Parvin Asadi*, Nazanin Mokhtari, Saeid Asghari, Hyeonji Rha, Ghadamali Khodarahmi, Hanieh Jalali, Amit Sharma*, Mohammad Dinari* and Jong Seung Kim*,

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引用次数: 0

Abstract

Covalent organic frameworks (COFs) show great potential as drug delivery systems (DDSs) due to their customizable structures, stability, and capacity for pore surface functionalization. However, their natural hydrophobicity limits their dispersion in water, posing challenges for biological applications. We address this issue by initially reducing a COF (Az-COF) to an amine-linked form (Az-AL-COF) and subsequently sulfonating it to obtain Az-AL-SO₃H-COF, a water-dispersible derivative. Water contact angle (WCA) analysis confirmed increased hydrophilicity across the series of 84.5, 61.2, and 54.7° for Az-COF, Az-AL-COF, and Az-AL-SO₃H-COF, respectively. Using doxorubicin (Dox) as a model drug, the modified COFs exhibited pH-sensitive drug release, with greater release at acidic pH (5.6) compared to neutral pH (7.4). Cytotoxicity assays revealed that Az-AL-SO₃H-COF was biocompatible with normal cells (MCF-10) while effectively suppressing the growth of cancer cells (MDA-MB-231). The Dox-loaded sulfonated COF (Dox@Az-AL-SO₃H-COF) showed selective cytotoxicity against cancer cells, highlighting its potential as a pH-responsive, biocompatible DDS for cancer treatment.

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COF的高级合成后修饰：提高阿霉素高效递送的亲水性

共价有机框架（COFs）由于其可定制的结构、稳定性和孔表面功能化能力而显示出巨大的潜力作为药物递送系统（dds）。然而，它们的天然疏水性限制了它们在水中的分散，给生物应用带来了挑战。我们首先将COF （Az-COF）还原为胺连接形式（Az-AL-COF），然后将其磺化以获得Az-AL-SO3H-COF，这是一种水分散衍生物。水接触角（WCA）分析证实，Az-COF、Az-AL-COF和Az-AL-SO3H-COF的亲水性分别提高了84.5°、61.2°和54.7°。以阿霉素（Dox）为模型药物，修饰的COFs表现出pH敏感的药物释放，在酸性pH（5.6）下比中性pH（7.4）下释放更大。细胞毒性实验表明，Az-AL-SO3H-COF与正常细胞（MCF-10）具有生物相容性，同时能有效抑制癌细胞（MDA-MB-231）的生长。负载dox的磺化COF （Dox@Az-AL-SO3H-COF）显示出对癌细胞的选择性细胞毒性，突出了其作为ph响应性，生物相容性的癌症治疗DDS的潜力。

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来源期刊

ACS Applied Bio Materials Chemistry-Chemistry (all)

CiteScore

9.40

自引率

2.10%

发文量

464

期刊介绍： ACS Applied Bio Materials is an interdisciplinary journal publishing original research covering all aspects of biomaterials and biointerfaces including and beyond the traditional biosensing, biomedical and therapeutic applications. The journal is devoted to reports of new and original experimental and theoretical research of an applied nature that integrates knowledge in the areas of materials, engineering, physics, bioscience, and chemistry into important bio applications. The journal is specifically interested in work that addresses the relationship between structure and function and assesses the stability and degradation of materials under relevant environmental and biological conditions.