Clarithromycin-loaded liposomes offering high drug loading and less irritation

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Nanotechnology

Background:

• Clarithromycin (CLA) is an antibiotic requiring improved delivery methods.
• Injectable formulations often face challenges with irritation and low drug loading.
• Liposomes offer a promising nanocarrier system for enhanced drug delivery.

Purpose of the Study:

• To develop an efficient method for preparing less irritant clarithromycin-loaded liposomes (CLA-Lip) for injection.
• To achieve high drug loading and evaluate physicochemical characteristics before and after lyophilization.
• To assess the reduced irritation potential of the developed CLA-Lip formulation.

Main Methods:

• Liposomes were prepared using the film-dispersion method with sodium cholesterol sulfate (SCS) and n-hexyl acid.
• Characterization included size, zeta potential, morphology (TEM), in vitro release, and haemolysis.
• Lyophilization was performed using sucrose as a protective agent, followed by DSC and Infrared spectroscopy analysis.
• Irritation testing involved mouse scratch and rat paw lick tests, and rabbit ear vein experiments.

Main Results:

• Multilamellar CLA-Lip with a regular size of approximately 100 nm were successfully prepared.
• H-bonding and salt-forming reactions ensured stable encapsulation of clarithromycin.
• A 30-fold increase in clarithromycin concentration was achieved compared to aqueous solutions.
• Lyophilized CLA-Lip demonstrated stability, and irritation was reduced by approximately 80% compared to clarithromycin phosphate solution.

Conclusions:

• The developed film-dispersion method efficiently prepares stable, less irritant clarithromycin-loaded liposomes (CLA-Lip).
• Lyophilization with sucrose enhances stability, making CLA-Lip suitable for injection.
• The significant reduction in irritation suggests improved clinical applicability for clarithromycin therapy.