Department of Medicinal Chemistry, School of Pharmacy, Shiraz University of Medical Sciences, Shiraz, Iran.
Department of Quality Control of Drug Products, School of Pharmacy, Shiraz University of Medical Sciences, Shiraz, Iran.
Colloids Surf B Biointerfaces. 2021 Sep;205:111823. doi: 10.1016/j.colsurfb.2021.111823. Epub 2021 May 6.
Multi-walled carbon nanotubes (MWCNTs) can be applied for pH-sensitive delivery of anticancer drugs. Due to the importance of 5-fluorouracil (5-FU) in different tumor therapy regimens, it has been widely used in different pH dependent drug delivery systems. To investigate the pH effects on loading (and release) of 5-FU on (and from) the functionalized MWCNTs and propose the optimum condition for drug delivery, both macroscopic and microscopic studies were carried out using chromatography and molecular dynamic simulation at different conditions. For both levels of studies, different analytical approaches were performed to assess the validity of the methods. The experimental results revealed that 5-FU has more binding affinity to the surface of the nanocarrier at physiological pH (pH = 7.4) and showed more release at acidic conditions (pH = 5.0). Meanwhile it has been observed that basic pH (pH = 9.0) can lead to a dramatic decrease effect on loading of the drug. The results of this study can be used to suggest the optimum pH levels for nanocarbon based formulations of 5-FU in cancer therapy.
多壁碳纳米管（MWCNTs）可用于 pH 敏感的抗癌药物传递。由于氟尿嘧啶（5-FU）在不同肿瘤治疗方案中的重要性，它已被广泛应用于不同的 pH 依赖性药物传递系统中。为了研究 pH 对功能化 MWCNTs 上（和从）5-FU 的加载（和释放）的影响，并提出药物传递的最佳条件，我们在不同条件下使用色谱法和分子动力学模拟进行了宏观和微观研究。在这两个研究水平上，我们都采用了不同的分析方法来评估方法的有效性。实验结果表明，5-FU 在生理 pH（pH=7.4）下对纳米载体表面具有更强的结合亲和力，在酸性条件（pH=5.0）下具有更强的释放能力。同时，我们还观察到碱性 pH（pH=9.0）会对药物的加载产生显著的抑制作用。本研究的结果可用于建议癌症治疗中基于纳米碳的 5-FU 制剂的最佳 pH 值水平。
