Lung Delivery of Lactose-Free Microparticles Loaded with Azithromycin for the Treatment of Bacterial Infections
<b>Background/Objectives:</b> 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 azithr...
Saved in:
| Main Authors: | , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2025-06-01
|
| Series: | Pharmaceutics |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1999-4923/17/6/770 |
| Tags: |
Add Tag
No Tags, Be the first to tag this record!
|
| _version_ | 1849744459665768448 |
|---|---|
| author | Gracia Molina Dolores R. Serrano María Auxiliadora Dea-Ayuela Carmina Rodriguez Elena González-Burgos Brayan J. Anaya |
| author_facet | Gracia Molina Dolores R. Serrano María Auxiliadora Dea-Ayuela Carmina Rodriguez Elena González-Burgos Brayan J. Anaya |
| author_sort | Gracia Molina |
| collection | DOAJ |
| description | <b>Background/Objectives:</b> 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. <b>Methods:</b> Using a quality-by-design approach, an optimized formulation (4% AZM, 20% leucine, and 76% mannitol) was achieved. <b>Results:</b> 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 <i>Pseudomonas aeruginosa</i> 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 <i>Streptococcus pneumoniae</i>. AZM microparticles demonstrated good biocompatibility with red blood cells and bronchial epithelial cells at therapeutic concentrations. <b>Conclusions:</b> These findings establish a promising lactose-free antibiotic formulation for targeted pulmonary delivery with enhanced antimicrobial efficacy. |
| format | Article |
| id | doaj-art-a057266d46ff42758bb4e7241b312c9d |
| institution | DOAJ |
| issn | 1999-4923 |
| language | English |
| publishDate | 2025-06-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj-art-a057266d46ff42758bb4e7241b312c9d2025-08-20T03:16:25ZengMDPI AGPharmaceutics1999-49232025-06-0117677010.3390/pharmaceutics17060770Lung Delivery of Lactose-Free Microparticles Loaded with Azithromycin for the Treatment of Bacterial InfectionsGracia Molina0Dolores R. Serrano1María Auxiliadora Dea-Ayuela2Carmina Rodriguez3Elena González-Burgos4Brayan J. Anaya5Pharmaceutics and Food Technology Department, Faculty of Pharmacy, Universidad Complutense de Madrid, Plaza Ramón y Cajal s/n, 28040 Madrid, SpainPharmaceutics and Food Technology Department, Faculty of Pharmacy, Universidad Complutense de Madrid, Plaza Ramón y Cajal s/n, 28040 Madrid, SpainDepartment of Pharmacy, Universidad Cardenal Herrera-CEU, CEU University, 46115 Valencia, SpainDepartment of Microbiology and Parasitology, Faculty of Pharmacy, Universidad Complutense de Madrid (UCM), 28040 Madrid, SpainDepartment of Pharmacology, Pharmacognosy and Botany, Faculty of Pharmacy, Universidad Complutense de Madrid (UCM), 28040 Madrid, SpainPharmaceutics and Food Technology Department, Faculty of Pharmacy, Universidad Complutense de Madrid, Plaza Ramón y Cajal s/n, 28040 Madrid, Spain<b>Background/Objectives:</b> 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. <b>Methods:</b> Using a quality-by-design approach, an optimized formulation (4% AZM, 20% leucine, and 76% mannitol) was achieved. <b>Results:</b> 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 <i>Pseudomonas aeruginosa</i> 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 <i>Streptococcus pneumoniae</i>. AZM microparticles demonstrated good biocompatibility with red blood cells and bronchial epithelial cells at therapeutic concentrations. <b>Conclusions:</b> These findings establish a promising lactose-free antibiotic formulation for targeted pulmonary delivery with enhanced antimicrobial efficacy.https://www.mdpi.com/1999-4923/17/6/770azithromycindry powder inhalerlactose-freemicroparticlespulmonary drug delivery |
| spellingShingle | Gracia Molina Dolores R. Serrano María Auxiliadora Dea-Ayuela Carmina Rodriguez Elena González-Burgos Brayan J. Anaya Lung Delivery of Lactose-Free Microparticles Loaded with Azithromycin for the Treatment of Bacterial Infections Pharmaceutics azithromycin dry powder inhaler lactose-free microparticles pulmonary drug delivery |
| title | Lung Delivery of Lactose-Free Microparticles Loaded with Azithromycin for the Treatment of Bacterial Infections |
| title_full | Lung Delivery of Lactose-Free Microparticles Loaded with Azithromycin for the Treatment of Bacterial Infections |
| title_fullStr | Lung Delivery of Lactose-Free Microparticles Loaded with Azithromycin for the Treatment of Bacterial Infections |
| title_full_unstemmed | Lung Delivery of Lactose-Free Microparticles Loaded with Azithromycin for the Treatment of Bacterial Infections |
| title_short | Lung Delivery of Lactose-Free Microparticles Loaded with Azithromycin for the Treatment of Bacterial Infections |
| title_sort | lung delivery of lactose free microparticles loaded with azithromycin for the treatment of bacterial infections |
| topic | azithromycin dry powder inhaler lactose-free microparticles pulmonary drug delivery |
| url | https://www.mdpi.com/1999-4923/17/6/770 |
| work_keys_str_mv | AT graciamolina lungdeliveryoflactosefreemicroparticlesloadedwithazithromycinforthetreatmentofbacterialinfections AT doloresrserrano lungdeliveryoflactosefreemicroparticlesloadedwithazithromycinforthetreatmentofbacterialinfections AT mariaauxiliadoradeaayuela lungdeliveryoflactosefreemicroparticlesloadedwithazithromycinforthetreatmentofbacterialinfections AT carminarodriguez lungdeliveryoflactosefreemicroparticlesloadedwithazithromycinforthetreatmentofbacterialinfections AT elenagonzalezburgos lungdeliveryoflactosefreemicroparticlesloadedwithazithromycinforthetreatmentofbacterialinfections AT brayanjanaya lungdeliveryoflactosefreemicroparticlesloadedwithazithromycinforthetreatmentofbacterialinfections |