Design, Optimization, and Characterization of Lysozyme-Loaded Poly(ɛ-Caprolactone) Microparticles for Pulmonary Delivery

IF 2.7 4区医学 Q2 PHARMACOLOGY & PHARMACY Journal of Pharmaceutical Innovation Pub Date : 2022-05-20 DOI:10.1007/s12247-022-09648-8

Burcu Devrim Gökberk, Nilhan Erdinç

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Abstract

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.

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肺输送溶菌酶负载聚己内酯微颗粒的设计、优化和表征

【摘要】目的以最小的副作用治疗肺部疾病的成功取决于微颗粒肺给药系统的优化设计，以提供局部给药。本研究旨在开发和评估针对囊性纤维化肺给药的优化药物给药系统。方法采用抗菌肽菌酶作为常规抗生素的替代药物。由于溶菌酶是一种水溶性药物，因此采用水包油包水(w1/o/w2)双乳液溶剂蒸发法制备了载菌酶微粒。聚己内酯(PCL)由于其生物相容性和可生物降解的特性而被选择作为聚合物。采用24全因子实验设计，以粒径和包封效率(%EE)为期望响应因子，对设计的微颗粒进行优化。结果与结论优化后的配方粒径为8.75±0.04µm, EE为65.15±0.00%。SEM分析结果表明，微颗粒呈球形结构，表面光滑。优化后的微颗粒在初始爆发释放后可持续释放长达35天。空气动力学直径(MMAD)和细颗粒分数(FPF)的平均值中值分别为5.44±0.19 μm和50.99±2.89%。这些结果表明，优化后的PCL微颗粒可用于溶菌酶的肺部递送。

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来源期刊

Journal of Pharmaceutical Innovation PHARMACOLOGY & PHARMACY-

CiteScore

3.70

自引率

3.80%

发文量

审稿时长

>12 weeks

期刊介绍： The Journal of Pharmaceutical Innovation (JPI), is an international, multidisciplinary peer-reviewed scientific journal dedicated to publishing high quality papers emphasizing innovative research and applied technologies within the pharmaceutical and biotechnology industries. JPI''s goal is to be the premier communication vehicle for the critical body of knowledge that is needed for scientific evolution and technical innovation, from R&D to market. Topics will fall under the following categories: Materials science, Product design, Process design, optimization, automation and control, Facilities; Information management, Regulatory policy and strategy, Supply chain developments , Education and professional development, Journal of Pharmaceutical Innovation publishes four issues a year.