Development of a dry powder formulation for pulmonary delivery of azithromycin-loaded nanoparticles.

IF 2.9 4区 医学 Q2 PHARMACOLOGY & PHARMACY Journal of Pharmacy and Pharmaceutical Sciences Pub Date : 2024-10-14 eCollection Date: 2024-01-01 DOI:10.3389/jpps.2024.13635
Alison Tatiana Madrid Sani, Khellida Loiane V Ramos-Rocha, Michelle Alvares Sarcinelli, Marcelo Henrique da Cunha Chaves, Helvécio Vinícius Antunes Rocha, Patrícia Léo, Natália Neto Pereira Cerize, Maria Helena Ambrosio Zanin, Valker Araujo Feitosa, Carlota de Oliveira Rangel-Yagui
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引用次数: 0

Abstract

The COVID-19 pandemic has raised concern regarding respiratory system diseases and oral inhalation stands out as an attractive non-invasive route of administration for pulmonary diseases such as chronic bronchitis, cystic fibrosis, COVID-19 and community-acquired pneumonia. In this context, we encapsulated azithromycin in polycaprolactone nanoparticles functionalized with phospholipids rich in dipalmitoylphosphatidylcholine and further produced a fine powder formulation by spray drying with monohydrated lactose. Nanoparticles obtained by the emulsion/solvent diffusion-evaporation technique exhibited a mean hydrodynamic diameter around 195-228 nm with a narrow monomodal size distribution (PdI < 0.2). Nanoparticle dispersions were spray-dried at different inlet temperatures, atomizing air-flow, aspirator air flow, and feed rate, using lactose as a drying aid, resulting in a maximal process yield of 63% and an encapsulation efficiency of 83%. Excipients and the dry powder formulations were characterized in terms of morphology, chemical structure, thermal analyses and particle size by SEM, FTIR, DSC/TGA and laser light diffraction. The results indicated spherical particles with 90% at 4.06 µm or below, an adequate size for pulmonary delivery. Aerosolization performance in a NGI confirmed good aerodynamic properties. Microbiological assays showed that the formulation preserves AZM antimicrobial effect against Staphylococcus aureus and Streptococcus pneumoniae strains, with halos above 18 mm. In addition, no formulation-related cytotoxicity was observed against the human cell lines BEAS-2B (lung epithelial), HUVEC (endothelial) and HFF1 (fibroblasts). Overall, the approach described here allows the production of AZM-PCL nanoparticles incorporated into inhalable microparticles, enabling more efficient pulmonary therapy of lung infections.

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开发一种干粉制剂,用于向肺部输送阿奇霉素纳米颗粒。
COVID-19 大流行引起了人们对呼吸系统疾病的关注,而口服吸入是治疗慢性支气管炎、囊性纤维化、COVID-19 和社区获得性肺炎等肺部疾病的一种极具吸引力的非侵入性给药途径。在此背景下,我们将阿奇霉素封装在富含二棕榈酰磷脂酰胆碱的磷脂功能化聚己内酯纳米颗粒中,并通过与一水乳糖喷雾干燥进一步制备了精细粉末配方。通过乳液/溶剂扩散-蒸发技术获得的纳米粒子的平均水动力直径约为 195-228 nm,具有窄的单模粒度分布(PdI < 0.2)。使用乳糖作为干燥辅助剂,在不同的入口温度、雾化空气流量、吸气器空气流量和进料速度下对纳米粒子分散体进行喷雾干燥,结果最大工艺收率为 63%,封装效率为 83%。通过扫描电镜、傅立叶变换红外光谱、DSC/TGA 和激光衍射,对辅料和干粉制剂的形态、化学结构、热分析和粒度进行了表征。结果表明,90% 的颗粒为球形,粒径在 4.06 微米或以下,这种粒径足以用于肺部给药。在 NGI 中的气溶胶性能证实了其良好的空气动力学特性。微生物检测表明,制剂对金黄色葡萄球菌和肺炎链球菌菌株保持了 AZM 的抗菌效果,光晕超过 18 毫米。此外,对人类细胞株 BEAS-2B(肺上皮细胞)、HUVEC(内皮细胞)和 HFF1(成纤维细胞)也未观察到与制剂有关的细胞毒性。总之,本文所描述的方法可将 AZM-PCL 纳米粒子制成可吸入微粒,从而实现更有效的肺部感染治疗。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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CiteScore
6.90
自引率
0.00%
发文量
29
审稿时长
6-12 weeks
期刊介绍: The Journal of Pharmacy and Pharmaceutical Sciences (JPPS) is the official journal of the Canadian Society for Pharmaceutical Sciences. JPPS is a broad-spectrum, peer-reviewed, international pharmaceutical journal circulated electronically via the World Wide Web. Subscription to JPPS is free of charge. Articles will appear individually as soon as they are accepted and are ready for circulation.
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