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Design and formulation technique of a novel drug delivery system for azithromycin and its anti-bacterial activity

M Joyce Nirmala1, Amitava Mukherjee, N Chandrasekaran

  • 1Centre for Nanobiotechnology, VIT University, Vellore, 632-014, Tamil Nadu, India.

AAPS Pharmscitech
|June 27, 2013
PubMed

Insights

A novel cinnamon oil microemulsion enhances azithromycin (AZ) delivery, significantly boosting antibacterial activity against Staphylococcus aureus. This new system improves drug solubility and bioavailability for better oral administration.

Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Microbiology

Background:

  • Azithromycin, an azalide antibiotic, exhibits broad-spectrum activity but suffers from poor water solubility and low oral bioavailability (37%).
  • These limitations necessitate the development of advanced drug delivery systems to improve azithromycin's efficacy and therapeutic potential.

Purpose of the Study:

  • To develop and characterize a novel cinnamon oil-based microemulsion for enhanced azithromycin solubilization and delivery.
  • To evaluate the antibacterial activity and mechanism of action of the azithromycin-loaded microemulsion against Staphylococcus aureus.

Main Methods:

  • Formulation of a cinnamon oil microemulsion using Tween 20 as a non-ionic surfactant.
  • Characterization of the microemulsion system including droplet size, thermodynamic stability, and viscosity.
  • Assessment of antibacterial activity via minimum inhibitory concentration (MIC) determination and scanning electron microscopy (SEM).
  • Investigation of bacterial membrane permeability using fluorescence microscopy with acridine orange/ethidium bromide staining.

Main Results:

  • The optimized formulation (F4, oil:surfactant ratio 1:4) exhibited enhanced azithromycin solubilization, small droplet size (5-8 nm), and good thermodynamic stability.
  • The azithromycin-loaded microemulsion demonstrated significantly improved antibacterial activity, with an MIC of 4 μg/ml compared to 128 μg/ml for the conventional formulation.
  • SEM and fluorescence microscopy confirmed alterations in bacterial morphology and membrane permeability, indicating a synergistic effect between azithromycin and cinnamon oil.

Conclusions:

  • The developed cinnamon oil microemulsion represents a promising oral drug delivery system for azithromycin, enhancing its antibacterial efficacy and biocompatibility.
  • The combination of small droplet size, cinnamon oil's properties, and improved drug solubilization contributes to the enhanced performance of the novel formulation.
  • This approach offers a potential strategy to overcome azithromycin's bioavailability challenges and improve treatment outcomes for bacterial infections.

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