Preparation and Characterization of Gatifloxacin-Loaded Polyacrylonitrile Nanofiber for the Management of Dry Eye Infection,Journal of Pharmaceutical Innovation

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Preparation and Characterization of Gatifloxacin-Loaded Polyacrylonitrile Nanofiber for the Management of Dry Eye Infection
Journal of Pharmaceutical Innovation ( IF 2.7 ) Pub Date : 2022-05-09 , DOI: 10.1007/s12247-022-09650-0
Dipak Kumar Sahu ₁ , Deepak Pradhan ₁ , Jitu Halder ₁ , Prativa Biswasroy ₁ , Biswakanth Kar ₁ , Goutam Ghosh ₁ , Goutam Rath _{1,

2}

Affiliation

Purpose

Dry eye can cause an increased risk of ocular infection due to loss of corneal epithelial integrity and changes to tear film homeostasis. Polymeric nanofibers with unique physicochemical and biological properties have attracted a lot of attention due to the improved in vivo performance of their conventional ocular formulations. The purpose of this present exposition was to assess the in vitro and in vivo efficacy of gatifloxacin (GAF)-loaded polyacrylonitrile (PAN) nanofiber in dry eye conditions.

Methods

The nanofibers were characterized for morphology, drug entrapment, swelling behavior, drug release, oxygen permeability, biodegradability, antimicrobial potential, and sterility. Draize test, in vivo antibacterial activity, corneal healing characteristics, and tear quality profiles were also used to determine in vivo safety and efficacy.

Results

Experimental findings suggested that electrospinning at defined conditions (applied voltage of 18 kV, flow rate of 0.5 mL/h, and tip to collector distance of 10 cm) produced smooth and continuous nanofibers with an average diameter of 480 nm. High drug entrapment of 95% combined with swelling indices of around 180% increased the controlled drug delivery capability of the prepared formulation. A slow degradation rate of 3±0.75% ensured a long-term cumulative drug release of 90% within 16 days. The inhibition diameter of the optimized formulation was found to be 15 ± 0.31 mm for E. coli and 13 ± 0.26 mm for S. aureus. Furthermore, after 3 days in an experimental dry eye animal model, the drug-loaded nanofiber showed better antibacterial activity, corneal healing, and tear film stability than the commercial eye drop.

Conclusion

Overall, the study concluded that the GAF-loaded PAN nanofiber has good application prospects in the treatment of dry eye due to its safety and controlled drug release profile.

Graphical Abstract

中文翻译：

用于治疗干眼感染的加替沙星负载聚丙烯腈纳米纤维的制备和表征

目的

由于角膜上皮完整性的丧失和泪膜稳态的改变，干眼症会增加眼部感染的风险。具有独特理化和生物学特性的聚合物纳米纤维由于其常规眼部制剂的体内性能得到改善而引起了广泛关注。本次博览会的目的是评估加替沙星 (GAF) 负载的聚丙烯腈 (PAN) 纳米纤维在干眼症中的体外和体内功效。

方法

对纳米纤维的形态、药物截留、溶胀行为、药物释放、透氧性、生物降解性、抗菌潜力和无菌性进行了表征。Draize 测试、体内抗菌活性、角膜愈合特性和泪液质量曲线也用于确定体内安全性和有效性。

结果

实验结果表明，在规定的条件下（施加电压为 18 kV，流速为 0.5 mL/h，尖端到收集器的距离为 10 cm）静电纺丝可以产生平均直径为 480 nm 的光滑连续纳米纤维。95% 的高药物包埋率和约 180% 的溶胀指数增加了所制备制剂的受控药物递送能力。3±0.75%的缓慢降解率确保了16天内90%的长期累积药物释放。发现优化配方的抑制直径对大肠杆菌为 15 ± 0.31 mm，对金黄色葡萄球菌为 13 ± 0.26 mm. 此外，在实验性干眼动物模型中 3 天后，载药纳米纤维显示出比市售滴眼液更好的抗菌活性、角膜愈合和泪膜稳定性。