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用于治疗细菌感染的载有阿奇霉素的无乳糖微粒的肺部给药

Lung Delivery of Lactose-Free Microparticles Loaded with Azithromycin for the Treatment of Bacterial Infections.

作者信息

Molina Gracia, Serrano Dolores R, Dea-Ayuela María Auxiliadora, Rodriguez Carmina, González-Burgos Elena, Anaya Brayan J

机构信息

Pharmaceutics and Food Technology Department, Faculty of Pharmacy, Universidad Complutense de Madrid, Plaza Ramón y Cajal s/n, 28040 Madrid, Spain.

Instituto Universitario de Farmacia Industrial, Faculty of Pharmacy, Universidad Complutense de Madrid, 28040 Madrid, Spain.

出版信息

Pharmaceutics. 2025 Jun 11;17(6):770. doi: 10.3390/pharmaceutics17060770.

DOI:10.3390/pharmaceutics17060770
PMID:40574082
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12196266/
Abstract

Respiratory bacterial infections remain a significant global health challenge, with effective drug delivery to the lungs being crucial for successful treatment. This study aimed to develop a lactose-free dry powder inhaler (DPI) formulation containing azithromycin (AZM) microparticles for enhanced pulmonary delivery. Using a quality-by-design approach, an optimized formulation (4% AZM, 20% leucine, and 76% mannitol) was achieved. The formulation demonstrated excellent aerodynamic properties with a mass median aerodynamic diameter (MMAD) of 2.72 μm ± 0.01 μm and fine particle fraction (FPF) (<5 μm) of 65.42% ± 5.12%. AZM-loaded microparticles exhibited enhanced efficacy against with a two-fold reduction in the minimum bactericidal concentration (7.81 μg/mL vs. 15.62 μg/mL) compared to unprocessed AZM, while maintaining activity against . AZM microparticles demonstrated good biocompatibility with red blood cells and bronchial epithelial cells at therapeutic concentrations. These findings establish a promising lactose-free antibiotic formulation for targeted pulmonary delivery with enhanced antimicrobial efficacy.

摘要

呼吸道细菌感染仍然是一项重大的全球健康挑战，将药物有效递送至肺部对于成功治疗至关重要。本研究旨在开发一种含阿奇霉素（AZM）微粒的无乳糖干粉吸入剂（DPI）制剂，以增强肺部给药效果。采用质量源于设计的方法，获得了一种优化制剂（4% AZM、20%亮氨酸和76%甘露醇）。该制剂表现出优异的空气动力学特性，质量中值空气动力学直径（MMAD）为2.72μm±0.01μm，细颗粒分数（FPF，<5μm）为65.42%±5.12%。与未处理的AZM相比，载AZM微粒对……表现出增强的疗效，最低杀菌浓度降低了两倍（7.81μg/mL对15.62μg/mL），同时保持了对……的活性。AZM微粒在治疗浓度下与红细胞和支气管上皮细胞表现出良好的生物相容性。这些发现确立了一种有前景的无乳糖抗生素制剂，用于靶向肺部给药并增强抗菌疗效。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/96df/12196266/ffe70f973ec9/pharmaceutics-17-00770-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/96df/12196266/cce3c6173143/pharmaceutics-17-00770-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/96df/12196266/3649ed6c7cb1/pharmaceutics-17-00770-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/96df/12196266/fb4fa1a9e6f2/pharmaceutics-17-00770-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/96df/12196266/955ba3f3f32b/pharmaceutics-17-00770-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/96df/12196266/de3525a9eaa4/pharmaceutics-17-00770-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/96df/12196266/87c46cb8c899/pharmaceutics-17-00770-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/96df/12196266/2ad7f7580b61/pharmaceutics-17-00770-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/96df/12196266/ffe70f973ec9/pharmaceutics-17-00770-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/96df/12196266/cce3c6173143/pharmaceutics-17-00770-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/96df/12196266/3649ed6c7cb1/pharmaceutics-17-00770-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/96df/12196266/fb4fa1a9e6f2/pharmaceutics-17-00770-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/96df/12196266/955ba3f3f32b/pharmaceutics-17-00770-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/96df/12196266/de3525a9eaa4/pharmaceutics-17-00770-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/96df/12196266/87c46cb8c899/pharmaceutics-17-00770-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/96df/12196266/2ad7f7580b61/pharmaceutics-17-00770-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/96df/12196266/ffe70f973ec9/pharmaceutics-17-00770-g008.jpg

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