Purpose

The purpose of the present work was to develop levofloxacin-flurbiprofen coloaded PLGA (LEV-FLU-PLGA) nanoparticles with surface modification using chitosan to attain mucoadhesion for the treatment of bacterial conjunctivitis.

Method

Polymeric nanoparticles were prepared by nanoprecipitation method and evaluated for parameters like particle size, PDI, zeta potential, entrapment efficiency (%), in vitro drug release, ex vivo permeation studies, microbial assay against Staphylococcus aureus and ocular tolerance using Hen’s egg test-chorioallantoic membrane (HET-CAM). Furthermore, surface of optimized PLGA nanoparticle formulation was modified by coating with chitosan.

Results

LEV-FLU-PLGA nanoparticles demonstrated particle size of 166.1 nm with PDI of 0.137 and zeta potential of − 16.8 mV. The entrapment efficiency was found to be 39.37% for levofloxacin (LEV) and 48.33% for flurbiprofen (FLU), whereas for surface-modified nanoparticles, it was found to be 42.05% for LEV and 45.26% for FLU. LEV-FLU chitosan-coated PLGA nanoparticles showed an increase in particle size, i.e., 333.6 nm with PDI of 0.319 and an inversion of zeta potential to 37.67 mV. The developed nanosystems showed sustained release and improved eye permeability. Microbiological studies showed equivalent zone of inhibition to that of marketed formulation. HET-CAM assay revealed the non-irritant nature of drug-loaded PLGA nanoparticles; however, chitosan-coated PLGA nanoparticles were found to be moderately irritating owing to the acidic nature of formulation.

Conclusion

The nanoparticulate system provides prolonged drug release making it a promising alternative to conventional dosage forms. It reduces systemic effects of locally acting drugs, improving therapeutic efficacy and patient compliance.

中文翻译：

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共负载表面修饰的 PLGA 纳米颗粒用于持续眼部递送左氧氟沙星和氟比洛芬

 目的

本工作的目的是开发左氧氟沙星-氟比洛芬共载 PLGA (LEV-FLU-PLGA) 纳米颗粒，并使用壳聚糖进行表面修饰，以获得粘膜粘附力，用于治疗细菌性结膜炎。

 方法

采用纳米沉淀法制备聚合物纳米颗粒，并使用鸡蛋测试-绒毛膜尿囊法评估粒径、PDI、zeta 电位、包封率 (%)、体外药物释放、离体渗透研究、金黄色葡萄球菌微生物测定和眼部耐受性等参数膜（HET-CAM）。此外，优化的PLGA纳米粒子配方通过壳聚糖涂层进行表面修饰。

 结果

LEV-FLU-PLGA 纳米粒子的粒径为 166.1 nm，PDI 为 0.137，zeta 电位为 − 16.8 mV。左氧氟沙星 (LEV) 和氟比洛芬 (FLU) 的包封率为 39.37%，氟比洛芬 (FLU) 的包封率为 48.33%，而表面修饰纳米颗粒的 LEV 和 FLU 的包封率为 42.05% 和 45.26%。 LEV-FLU 壳聚糖包被的 PLGA 纳米粒子显示出粒径增加，即 333.6 nm，PDI 为 0.319，zeta 电位反转至 37.67 mV。开发的纳米系统表现出持续释放和改善的眼睛渗透性。微生物学研究表明抑制区与市售制剂相当。 HET-CAM 测定揭示了载药 PLGA 纳米颗粒的无刺激性；然而，由于制剂的酸性性质，壳聚糖包被的 PLGA 纳米粒子被发现具有中等刺激性。

 结论

纳米颗粒系统提供延长的药物释放，使其成为传统剂型的有前途的替代品。它减少局部作用药物的全身效应，提高治疗效果和患者依从性。