A novel pH-responsive drug carrier for the delivery of specific Docetaxel (DTX) administration is developed based on a zeolitic imidazolate framework (ZIF-8). Aminating the surface of ZIF-8 is allowed for the conjugation of folic acid (FA). Several spectroscopic studies characterized the newly fabricated DTX-encapsulated folic acid-embedded ethylene diamine (ED) ZIF-8 nanocomposites (DTX/FA@ED-ZIF-8). It has excellent chemical stability and high drug-loading efficiency. DTX from the folic acid-embedded aminated ZIF-8 (FA@ED-ZIF-8) is three-fold more efficient under acidic pH (5.0) than in physiological settings (pH 7.4), according to in vitro drug release tests. DTX/FA@ED-ZIF-8 exhibited cytotoxicity of 76.8% in an MTT experiment conducted in A549 and H1299 cells. Cell morphological and nuclear staining were investigated in the fabricated samples to support the MTT experiments. Further, the apoptosis mode of cell death was examined using Annexin V-FITC and PI by flow cytometry. These findings indicate that FA@ED-ZIF-8 holds great potential as a drug carrier for precise dosing.

Graphical abstract

中文翻译：

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叶酸包埋的胺化药物封装沸石咪唑酯框架的制备作为有前景的肺癌药物递送系统

基于沸石咪唑酯框架 (ZIF-8)，开发了一种新型 pH 响应性药物载体，用于输送特定的多西紫杉醇 (DTX)。胺化 ZIF-8 的表面可以与叶酸 (FA) 结合。多项光谱研究对新制备的 DTX 封装叶酸包埋乙二胺 (ED) ZIF-8 纳米复合材料 (DTX/FA@ED-ZIF-8) 进行了表征。具有优良的化学稳定性和较高的载药效率。根据体外药物释放测试，来自叶酸嵌入的胺化 ZIF-8 (FA@ED-ZIF-8) 的 DTX 在酸性 pH (5.0) 下的效率是生理环境 (pH 7.4) 下的三倍。在 A549 和 H1299 细胞中进行的 MTT 实验中，DTX/FA@ED-ZIF-8 显示出 76.8% 的细胞毒性。在制作的样品中研究了细胞形态学和核染色以支持 MTT 实验。此外，使用Annexin V-FITC和PI通过流式细胞术检查细胞死亡的凋亡模式。这些发现表明 FA@ED-ZIF-8 作为精确给药的药物载体具有巨大的潜力。

图形概要