Abstract
Purpose: Conventional topical dosage forms face with some challenges like low intraocularbioavailability, which could be overcome by application of novel drug delivery systems.Therefore, this study was conducted to prepare azithromycin (AZM)-loaded chitosan/polyvinylalcohol/polyvinyl pyrrolidone (CS/PVA-PVP) nanofibers with the prolonged antibacterialactivity by electrospinning method. Methods: After preparation of nanofibers, they were characterized in terms of physicochemicaland morphological properties. In vitro and in vivo release of the drug from nanofibers wereevaluated using microbial assay against the Micrococcus luteus. Antibacterial efficacy of thenanofibers was assessed. The ophthalmic irritation test was also performed. MTT test wascarried out to evaluate cytotoxicity of the formulations. Results: All the formulations were found to be stable with uniform thickness, weight, and drugcontent. Nanofibers had a diameter range from 119 ± 29 to 171 ± 39 nm. The inserts were nonirritantand non-toxic to the rabbits’ eye. Based on the obtained results, the crosslinked AZMnanofibers showed slower and more controlled drug release in tear fluid compared to the noncrosslinkedones, within 184 hours. Conclusion: Our results revealed that the prepared nanofibers could be considered as suitableand non-invasive inserts for the prolonged ophthalmic delivery of AZM.
Highlights
Topical dosage forms have always been the most common route of administration for t ophthalmic anti-infective agents.[1]
The nanofibers could be more beneficial by addition of other polymers like polyvinyl alcohol (PVA), polyvinyl pyrrolidone (PVP), and polyethylene terephthalate (PET) to CS compared to pure CS
This addition could lead to a significant decrease in fiber diameter of electrospun CS/PVP mixed fibers attributing to an increase in solution conductivity.[24,25] e Glutaraldehyde (GA) is a strong crosslinker due to high activity of aldehyde groups, which could interact with amino groups of proteins
Summary
All the formulations were found to be stable with uniform thickness, weight, and drug content. Nanofibers had a diameter range from 119±29 to 171±39 nm. The inserts were nonirritant and non-toxic to the rabbits҆ eye. Based on the obtained results, the crosslinked AZM nanofibers showed slower and more controlled drug release in tear fluid compared to the noncrosslinked ones, within 184 h
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