Experimental Science
Preparation and antifungal activity of water-soluble graphene-based itraconazole antifungal eye drops
Li Jingguo, Han Fengqi, Zhao Mengyang, He Jijun, Liang Zhen, Zhang Junjie
Published 2023-07-10
Cite as Chin J Exp Ophthalmol, 2023, 41(7): 641-645. DOI: 10.3760/cma.j.cn115989-20230428-00153
Abstract
ObjectiveTo prepare water-soluble graphene-based itraconazole antifungal eye drops and evaluate its antifungal activity against Fusarium solani.
MethodsBy 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.
ResultsScanning 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.
ConclusionsGO-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