Azithromycin-loaded respirable microparticles for targeted pulmonary delivery for the treatment of pneumonia
| Autor: | Qiyue Wang, Jiasheng Tu, Daniel J. Hickey, Thomas J. Webster, Yan Shen, Yanan Li, Gujie Mi |
|---|---|
| Rok vydání: | 2018 |
| Předmět: |
Surface Properties
medicine.drug_class Antibiotics Biophysics Bioengineering Diketopiperazines 02 engineering and technology Azithromycin Pharmacology 030226 pharmacology & pharmacy Biomaterials 03 medical and health sciences 0302 clinical medicine Oral administration Pneumonia Bacterial medicine Animals Humans Tissue Distribution Particle Size Lung Drug Carriers Mice Inbred BALB C business.industry Bacterial pneumonia 021001 nanoscience & nanotechnology Antimicrobial medicine.disease Microspheres Anti-Bacterial Agents Bioavailability Pneumonia Streptococcus pneumoniae medicine.anatomical_structure Solubility Mechanics of Materials Biofilms Delayed-Action Preparations Ceramics and Composites Female 0210 nano-technology business medicine.drug |
| Zdroj: | Biomaterials. 160:107-123 |
| ISSN: | 0142-9612 |
| DOI: | 10.1016/j.biomaterials.2018.01.022 |
| Popis: | Pneumonia is a major contributor to infection-based hospitalizations and deaths in the United States. Antibiotics such as azithromycin (AZM), although effective at managing pneumonia, often suffer from off-target diffusion and poor bioavailability when administered orally or via intravenous injection. The formation of biofilms at the disease sites makes the treatment more complicated by protecting bacteria from antimicrobial agents and thus necessitating a much higher dosage of antibiotics to eradicate the biofilms. As such, targeted pulmonary delivery of antibiotics has emerged as a promising alternative by providing direct access to the lung while also allowing higher local therapeutic concentrations but minimal systemic exposure. In this study, AZM was encapsulated in N-fumaroylated diketopiperazine (FDKP) microparticles for efficient pulmonary delivery. Both in vitro and in vivo results demonstrated that AZM@FDKP-MPs administered via intratracheal insufflation achieved at least a 3.4 times higher local concentration and prolonged retention times compared to intravenous injection and oral administration, suggesting their potential to better manage bacterial pneumonia. |
| Databáze: | OpenAIRE |
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