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Fluconazole conjugated-gold nanorods as an antifungal nanomedicine with low cytotoxicity against human dermal fibroblasts
RSC Advances ( IF 3.9 ) Pub Date : 2020-7-8 , DOI: 10.1039/d0ra00297f Khawla M Hamad 1 , Nouf N Mahmoud 2 , Sabaa Al-Dabash 2 , Luma A Al-Samad 2 , Maha Abdallah 3 , Amal G Al-Bakri 3
RSC Advances ( IF 3.9 ) Pub Date : 2020-7-8 , DOI: 10.1039/d0ra00297f Khawla M Hamad 1 , Nouf N Mahmoud 2 , Sabaa Al-Dabash 2 , Luma A Al-Samad 2 , Maha Abdallah 3 , Amal G Al-Bakri 3
Affiliation
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Herein, a nanotechnology-based approach was adopted to develop a facile and effective nanoplatform for the treatment of superficial fungal infections. Gold nanorods (GNR) functionalized with thiolated poly ethylene glycol (PEG-SH) or thiolated PEGylated cholesterol (Chol-PEG-SH) moieties were conjugated with Fluconazole and loaded into poloxamer 407 hydrogel. The obtained nanocomplexes; PEG-Fluc-GNR and Chol-Fluc-GNR were characterized by optical spectroscopy, hydrodynamic size and effective surface charge. The anti-fungal activity of the nanocomplexes was investigated by estimating the minimum inhibitory concentration (MIC) and the percentage reduction of fungal viable count against Candida (C.) albicans. PEG-Fluc-GNR and Chol-Fluc-GNR resulted in 5-fold and 14-fold reduction in MIC of GNR, and in 9-fold and 12-fold reduction in MIC of Fluconazole, respectively. The average log-reduction of the viable fungal cells upon treatment with the nanocomplexes was 5 log cycles, and it ranged from 1.3–3.7 log cycles when loaded into poloxamer 407 hydrogel. Transmission electron microscope imaging of the treated C. albicans revealed an enhanced uptake of the nanoparticles into the fungus's cell wall within the first 120 min of exposure. The nanocomplexes demonstrated low cytotoxicity towards human dermal fibroblasts which represent the human skin dermal cells. Conjugating Fluconazole with GNR is a promising approach for the effective treatment of superficial fungal infections.
中文翻译：
氟康唑共轭金纳米棒作为一种抗真菌纳米药物，对人皮肤成纤维细胞具有低细胞毒性
在此，采用基于纳米技术的方法开发了一种用于治疗浅表真菌感染的简便有效的纳米平台。用硫醇化聚乙二醇 (PEG-SH) 或硫醇化聚乙二醇化胆固醇 (Chol-PEG-SH) 部分功能化的金纳米棒 (GNR) 与氟康唑缀合并加载到泊洛沙姆 407 水凝胶中。得到的纳米复合物；PEG-Fluc-GNR和Chol-Fluc-GNR通过光谱学、流体动力学尺寸和有效表面电荷表征。通过估计最小抑制浓度 (MIC) 和对白色念珠菌( C. ) albicans的真菌活计数减少百分比来研究纳米复合物的抗真菌活性. PEG-Fluc-GNR 和 Chol-Fluc-GNR 分别导致 GNR 的 MIC 降低 5 倍和 14 倍，氟康唑的 MIC 降低 9 倍和 12 倍。用纳米复合物处理后活真菌细胞的平均对数减少为 5 个对数循环，当加载到泊洛沙姆 407 水凝胶中时，其范围为 1.3-3.7 个对数循环。处理过的白色念珠菌的透射电子显微镜成像显示，在暴露的前 120 分钟内，纳米颗粒被增强吸收到真菌的细胞壁中。纳米复合物对代表人皮肤真皮细胞的人真皮成纤维细胞表现出低细胞毒性。氟康唑与 GNR 的结合是一种有效治疗浅表真菌感染的有前景的方法。
更新日期：2020-07-08
中文翻译：
氟康唑共轭金纳米棒作为一种抗真菌纳米药物，对人皮肤成纤维细胞具有低细胞毒性
在此，采用基于纳米技术的方法开发了一种用于治疗浅表真菌感染的简便有效的纳米平台。用硫醇化聚乙二醇 (PEG-SH) 或硫醇化聚乙二醇化胆固醇 (Chol-PEG-SH) 部分功能化的金纳米棒 (GNR) 与氟康唑缀合并加载到泊洛沙姆 407 水凝胶中。得到的纳米复合物；PEG-Fluc-GNR和Chol-Fluc-GNR通过光谱学、流体动力学尺寸和有效表面电荷表征。通过估计最小抑制浓度 (MIC) 和对白色念珠菌( C. ) albicans的真菌活计数减少百分比来研究纳米复合物的抗真菌活性. PEG-Fluc-GNR 和 Chol-Fluc-GNR 分别导致 GNR 的 MIC 降低 5 倍和 14 倍，氟康唑的 MIC 降低 9 倍和 12 倍。用纳米复合物处理后活真菌细胞的平均对数减少为 5 个对数循环，当加载到泊洛沙姆 407 水凝胶中时，其范围为 1.3-3.7 个对数循环。处理过的白色念珠菌的透射电子显微镜成像显示，在暴露的前 120 分钟内，纳米颗粒被增强吸收到真菌的细胞壁中。纳米复合物对代表人皮肤真皮细胞的人真皮成纤维细胞表现出低细胞毒性。氟康唑与 GNR 的结合是一种有效治疗浅表真菌感染的有前景的方法。
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