Solulan C24- and Bile Salts-Modified Niosomes for New Ciprofloxacin Mannich Base for Combatting Pseudomonas-Infected Corneal Ulcer in Rabbits

Pharmaceuticals

卷:15

Mahmoud Elrehany¹  Rania Alaaeldin¹  Mohamed Abdel-Aziz²  Hossam Moharram³  Raafat M. A. Abdallah³  Mohamed A. Abdelgawad⁴  Gamal El-Din A. Abuo-Rahma⁵  Islam M. Abdel-Rahman⁵  Alaa M. Hayallah⁶  Soad A. Mohamed⁷  Hamdy Abdelkader⁷  Zeinab Fathalla⁸  Mohammed M. Ghoneim⁹ 

[1] Department of Biochemistry, Faculty of Pharmacy, Deraya University, New-Minia 61519, Minya, Egypt;

[2] Department of Medicinal Chemistry, Faculty of Pharmacy, Minia University, Minia 61519, Minya, Egypt;

[3] Department of Ophthalmology, Faculty of Medicine, Minia University, Minia 61519, Minya, Egypt;

[4] Department of Pharmaceutical Chemistry, College of Pharmacy, Jouf University, Sakaka 72341, Al Jawf, Saudi Arabia;

[5] Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Deraya University, New-Minia 61519, Minya, Egypt;

[6] Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71515, Asyut, Egypt;

[7] Department of Pharmaceutics, Faculty of Pharmacy, Deraya University, New-Minia 61519, Minya, Egypt;

[8] Department of Pharmaceutics, Faculty of Pharmacy, Minia University, Minia 61519, Minya, Egypt;

[9] Department of Pharmacy Practice, College of Pharmacy, AlMaarefa University, Ad Diriyah 13713, Ar Riyad, Saudi Arabia;

关键词: ciprofloxacin mannich base;    keratitis;    corneal ulcer;    gene expression;    antibiotic resistance;   

DOI  :  10.3390/ph15010044

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown