Preparation and antifungal activity of water-soluble graphene-based itraconazole antifungal eye drops

Authors: Li Jingguo,  Han Fengqi,  Zhao Mengyang,  He Jijun,  Liang Zhen,  Zhang Junjie
DOI: 10.3760/cma.j.cn115989-20230428-00153
Published 2023-07-10
Cite as Chin J Exp Ophthalmol, 2023, 41(7): 641-645.

Abstract                               [Download PDF] [Read Full Text]

Objective

To prepare water-soluble graphene-based itraconazole antifungal eye drops and evaluate its antifungal activity against Fusarium solani.

Methods

By oxidative modification of graphene and modification of polymer materials, water-soluble graphene oxide-modified polyethylene glycol (GO-PEG) composites were prepared.The composites were characterized by scanning electron microscopy, zeta potential, and Raman spectroscopy.The antifungal drug itraconazole was loaded onto the GO-PEG vector by solvent evaporation method, and itraconazole eye drops were obtained.The drug loading of itraconazole eye drops was measured using a UV and visible spectrophotometer.The antifungal effect in vitro was assessed by the microdilution method and light microscopy.

Results

Scanning electron microscopy showed that GO-PEG had a two-dimensional nanosheet structure and many wrinkles.The zeta potential of GO-PEG was -42.40 mV.Raman spectroscopy showed that the ID/IG of GO-PEG was 1.003.Using the water-soluble GO-PEG vector, a maximum itraconazole concentration of 10 mg/ml was achieved with a 10 000-fold increase in apparent solubility (10 mg/ml vs 0.001 mg/ml). The antifungal results showed that the minimum inhibitory concentration of itraconazole eye drops against Fusarium solani was approximately 1.88 μg/ml, but the GO-PEG vector has no significant antifungal activity against Fusarium solani.

Conclusions

GO-PEG achieves effective loading and solubilization of itraconazole, demonstrating an in vitro inhibitory effect on Fusarium solani.

Key words:

Antifungal agents; Itraconazole; Solubility; Fungal keratitis; Antifungal properties

Contributor Information

Li Jingguo

Department of Ophthalmology, Henan Province People’s Hospital, Henan Eye Hospital, Zhengzhou 450003, China

Han Fengqi

Department of Ophthalmology, Henan Province People’s Hospital, Henan Eye Hospital, Zhengzhou 450003, China

Zhao Mengyang

Department of Ophthalmology, Henan Province People’s Hospital, Henan Eye Hospital, Zhengzhou 450003, China

He Jijun

Department of Ophthalmology, Henan Province People’s Hospital, Henan Eye Hospital, Zhengzhou 450003, China

Liang Zhen

Department of Ophthalmology, Henan Province People’s Hospital, Henan Eye Hospital, Zhengzhou 450003, China

Zhang Junjie

Department of Ophthalmology, Henan Province People’s Hospital, Henan Eye Hospital, Zhengzhou 450003, China

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