Cefquinome-loaded microsphere formulations against Klebsiella pneumonia infection during experimental infections

Area of Science:

• Biomedical Engineering
• Pharmacology
• Veterinary Medicine

Background:

• Pneumonia, particularly lung infections caused by Klebsiella, poses a significant therapeutic challenge.
• Effective drug delivery systems are crucial for improving treatment outcomes and minimizing side effects.

Purpose of the Study:

• To develop and characterize cefquinome-loaded polylactic acid microspheres for pneumonia therapy.
• To evaluate the in vitro and in vivo performance of these microspheres in a rat model.

Main Methods:

• Microspheres were prepared using a one-step spray-drying method with a two-fluid nozzle.
• Characterization included size, encapsulation efficiency, and drug loading.
• In vitro drug release studies were conducted over 36 hours.
• In vivo efficacy was assessed in a rat model of Klebsiella pneumonia, monitoring bacterial load and inflammatory markers.

Main Results:

• Uniform, spherical microspheres (9.8 ± 3.6 μm) were successfully prepared with high encapsulation efficiency (91.6 ± 2.6%) and drug loading (18.7 ± 1.2%).
• Sustained in vitro release of cefquinome was observed for 36 hours.
• The microspheres demonstrated efficacy in clearing experimental Klebsiella pneumonia infections, reducing inflammatory cells and cytokines (TNF-α, IL-1β, IL-8).
• Rats treated with microspheres achieved microbiological cure (bacterial load < 100 CFU/g).

Conclusions:

• Cefquinome-loaded polylactic acid microspheres represent a successful drug delivery system for treating lung infections.
• The spray-drying method is a safe and straightforward approach for preparing these lung-targeting microspheres.
• This technology holds promise for effective animal lung-targeting therapy.