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氟康唑共轭金纳米棒作为一种对人皮肤成纤维细胞具有低细胞毒性的抗真菌纳米药物。

Fluconazole conjugated-gold nanorods as an antifungal nanomedicine with low cytotoxicity against human dermal fibroblasts.

作者信息

Hamad Khawla M, Mahmoud Nouf N, Al-Dabash Sabaa, Al-Samad Luma A, Abdallah Maha, Al-Bakri Amal G

机构信息

Amman Academy Amman 11821 Jordan.

Faculty of Pharmacy, Al-Zaytoonah University of Jordan Amman 11733 Jordan

出版信息

RSC Adv. 2020 Jul 8;10(43):25889-25897. doi: 10.1039/d0ra00297f. eCollection 2020 Jul 3.

DOI:10.1039/d0ra00297f
PMID:35518580
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9055348/
Abstract

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 () . 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 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.

摘要

在此,采用了一种基于纳米技术的方法来开发一种简便有效的纳米平台,用于治疗浅表真菌感染。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)与氟康唑共轭,并负载到泊洛沙姆407水凝胶中。通过光谱学、流体动力学尺寸和有效表面电荷对所得纳米复合物(PEG-Fluc-GNR和Chol-Fluc-GNR)进行了表征。通过估计最小抑菌浓度(MIC)和针对()的真菌活菌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分别使GNR的MIC降低了5倍和14倍,使氟康唑的MIC降低了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个对数周期,当负载到泊洛沙姆407水凝胶中时,其范围为1.3 - 3.7个对数周期。对处理后的(此处原文缺失具体内容)进行透射电子显微镜成像显示,在暴露的前120分钟内,纳米颗粒对真菌细胞壁的摄取增加。纳米复合物对代表人类皮肤真皮细胞的人皮肤成纤维细胞表现出低细胞毒性。将氟康唑与GNR共轭是有效治疗浅表真菌感染的一种有前景的方法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0b02/9055348/af461373507b/d0ra00297f-f6.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0b02/9055348/af461373507b/d0ra00297f-f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0b02/9055348/6e9a0d6f2add/d0ra00297f-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0b02/9055348/0e41b954edff/d0ra00297f-f2.jpg
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