Ciprofloxacin in Layered Double Hydroxides: Looking for the Best Synthesis Method

Area of Science:

• Materials Science
• Nanotechnology
• Pharmaceutical Sciences

Background:

• Optimizing drug release kinetics is crucial for effective antibiotic therapy, particularly for maintaining therapeutic plasmatic concentrations.
• Layered double hydroxides (LDH) are biocompatible inorganic materials with tunable drug intercalation and release properties, influenced by pH.
• LDH present a promising platform for developing sustained-release drug formulations.

Purpose of the Study:

• To synthesize and characterize layered double hydroxides (LDH) intercalated with ciprofloxacin (CIP) using three distinct methods.
• To evaluate the drug release kinetics and dissolution profiles of the synthesized LDH-CIP complexes under various pH conditions.
• To compare the release performance of the optimized LDH-CIP formulation with a commercial ciprofloxacin product.

Main Methods:

• Synthesis of LDH-CIP complexes via coprecipitation, reconstruction, and ion exchange methods.
• Characterization using X-ray Diffraction (XRD), Thermogravimetric Differential Scanning Calorimetry (TG-DSC), Transmission Electron Microscopy (TEM), Scanning Electron Microscopy (SEM), Fourier-Transform Infrared Spectroscopy (FTIR), and electrophoretic mobility.
• Assessment of drug release and dissolution kinetics in NaCl solutions and under physiological conditions.

Main Results:

• The ion exchange method resulted in superior intercalation of ciprofloxacin into the LDH structure compared to coprecipitation and reconstruction.
• Ciprofloxacin release was pH-dependent, primarily governed by dissolution at pH < 3 and desorption/ion exchange at higher pH.
• The LDH-CIP complex synthesized via ion exchange exhibited a significantly slower release profile than a commercial formulation.
• Fast dissolution at gastric pH necessitates protective coating strategies for LDH materials.

Conclusions:

• Ion exchange is the preferred method for synthesizing LDH-CIP complexes with optimal intercalation and controlled release properties.
• LDH-based formulations can achieve sustained release of ciprofloxacin, potentially improving pharmacokinetic profiles.
• Further development, including protective coatings, is required to mitigate rapid drug release in acidic environments like the stomach.