Abstract
Keratitis is a global health issue that claims the eye sight of millions of people every year. Dry eye, contact lens wearing and refractive surgeries are among the most common causes. The resistance rate among fluoroquinolone antibiotics is >30%. This study aims at formulating a newly synthesized ciprofloxacin derivative (2b) niosomes and Solulan C24-, sodium cholate- and deoxycholate-modified niosomes. The prepared niosomal dispersions were characterized macroscopically and microscopically (SEM) and by percentage entrapment efficiency, in vitro release and drug release kinetics. While the inclusion of Solulan C24 produced something discoidal-shaped with a larger diameter, both cholate and deoxycholate were unsuccessful in forming niosomes dispersions. Conventional niosomes and discomes (Solulan C24-modified niosomes) were selected for further investigation. A corneal ulcer model inoculated with colonies of Pseudomonas aeruginosa in rabbits was developed to evaluate the effectiveness of keratitis treatment of the 2b-loaded niosomes and 2b-loaded discomes compared with Ciprocin® (ciprofloxacin) eye drops and control 2b suspension. The histological documentation and assessment of gene expression of the inflammatory markers (IL-6, IL1B, TNFα and NF-κB) indicated that both 2b niosomes and discomes were superior treatments and can be formulated at physiological pH 7.4 compatible with the ocular surface, compared to both 2b suspension and Ciprocin® eye drops.
Highlights
Bacterial keratitis is a primary cause of corneal blindness [1]
Previous studies on ciprofloxacin indicated that the encapsulation of ciprofloxacin in liposomes has been more effective and reduced the treatment period against Bacillus anthracis [23]
These findings contradict our previous findings upon using a water-soluble drug [25]; the results indicate that both sodium cholate and deoxycholate are poor membrane additives when used with a poorly soluble drug like 2b
Summary
Bacterial keratitis is a primary cause of corneal blindness [1]. Bacterial keratitis could progress rapidly and can cause ocular damage such as irreversible corneal melt, endophthalmitis and lead to loss of vision [1,2]. Diseases that can be associated with corneal neovascularization include inflammatory disorders, corneal graft rejection after transplantation, infectious keratitis, contact lens-related hypoxia, alkali burns, stromal ulceration or limbal stem cell deficiency [3]. The contagions responsible for bacterial keratitis are surprisingly alike worldwide; the predominance of each microbial etiology changes according to many factors including patients’ general health, the nature of precursor optical trauma resulting from from surgery or lesions, environmental factors and the type of the pathogen [2].
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