Preparation and antifungal activity of water-soluble graphene-based itraconazole antifungal eye drops
10.3760/cma.j.cn115989-20230428-00153
- VernacularTitle:水溶性石墨烯基伊曲康唑滴眼液的制备及其抗真菌活性
- Author:
Jingguo LI
1
;
Fengqi HAN
;
Mengyang ZHAO
;
Jijun HE
;
Zhen LIANG
;
Junjie ZHANG
Author Information
1. 河南省人民医院眼科 河南省立眼科医院，郑州 450003
- Keywords:
Antifungal agents;
Itraconazole;
Solubility;
Fungal keratitis;
Antifungal properties
- From:
Chinese Journal of Experimental Ophthalmology
2023;41(7):641-645
- CountryChina
- Language:Chinese
-
Abstract:
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.
