Purpose

The success of the treatment of lung diseases with minimized side effects depends on the optimum design of microparticulate systems for pulmonary delivery that provide local delivery of drugs. This study aims to develop and evaluate optimized drug delivery systems against cystic fibrosis for pulmonary delivery.

Methods

Lysozyme, an antimicrobial peptide, was used as an alternative drug to conventional antibiotics. Since lysozyme is a water-soluble drug, lysozyme-loaded microparticles were prepared using the water-in-oil-in-water (w₁/o/w₂) double emulsion solvent evaporation method. Polycaprolactone (PCL) was chosen as a polymer due to its biocompatible and biodegradable properties. Designed microparticles were optimized utilizing 2⁴ full factorial experimental design based on desired response factors including particle size and encapsulation efficiency (%EE).

Results and conclusion

Optimized formulation was found to display particle size of 8.75 ± 0.04 µm and %EE of 65.15 ± 0.00%. Results of SEM analysis have shown the spherical structure of microparticles with a smooth surface. Optimized microparticles were found to exhibit sustained release for up to 35 days after initial burst release. Mean median aerodynamic diameter (MMAD) and fine particle fraction (FPF) values were found to be 5.44 ± 0.19 μm and 50.99 ± 2.89%, respectively. These results demonstrated that optimized PCL microparticles can be used for pulmonary delivery of lysozyme.

中文翻译：

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用于肺部递送的载有溶菌酶的聚 (ε-己内酯) 微粒的设计、优化和表征

目的

以最小化的副作用治疗肺部疾病的成功取决于提供局部药物递送的肺部递送微粒系统的优化设计。本研究旨在开发和评估针对肺递送的囊性纤维化优化的药物递送系统。

方法

溶菌酶是一种抗菌肽，被用作传统抗生素的替代药物。由于溶菌酶是水溶性药物，因此使用水包油包水(w ₁ /o/w ₂ )双乳液溶剂蒸发法制备负载溶菌酶的微粒。聚己内酯 (PCL) 因其生物相容性和可生物降解的特性而被选为聚合物。基于所需的响应因素，包括粒径和包封效率 (%EE)，利用 2 ^{4全因子实验设计优化设计的微粒。}

结果和结论

发现优化的配方显示出 8.75 ± 0.04 µm 的粒径和 65.15 ± 0.00% 的 %EE。SEM分析的结果显示了具有光滑表面的微粒的球形结构。发现优化的微粒在初始突释后表现出长达 35 天的持续释放。平均空气动力学直径 (MMAD) 和细颗粒分数 (FPF) 值分别为 5.44 ± 0.19 μm 和 50.99 ± 2.89%。这些结果表明，优化的 PCL 微粒可用于溶菌酶的肺部递送。