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Ciprofloxacin surf-plexes in sub-micron emulsions: a novel approach to improve payload efficiency and antimicrobial

Vikas Jain1, Deepak Singodia, Girish K Gupta

  • 1Pharmaceutics Division, Central Drug Research Institute (CSIR), Lucknow, India.

International Journal of Pharmaceutics
|March 2, 2011
PubMed

Insights

This study developed a novel ciprofloxacin-loaded submicron emulsion using ion-pairing for enhanced drug delivery. The modified emulsion significantly improved antimicrobial efficacy and pharmacokinetic profiles for better treatment outcomes.

Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Antimicrobial Research

Background:

  • Ciprofloxacin (CFn) is an important antibiotic with poor water solubility, limiting its therapeutic applications.
  • Developing effective drug delivery systems is crucial for improving the efficacy and pharmacokinetics of poorly soluble drugs like CFn.

Purpose of the Study:

  • To investigate the antimicrobial efficacy and pharmacokinetic profile of ciprofloxacin-loaded oil-in-water submicron emulsion (SE-CFn).
  • To develop hydrophobic ion-pair complexes of CFn with sodium deoxycholate (SDC) for enhanced incorporation into submicron emulsions.
  • To evaluate the impact of chitosan modification on the efficacy and pharmacokinetics of the developed formulation.

Main Methods:

  • Formation and characterization of ciprofloxacin-sodium deoxycholate (CFn-SDC) ion-pair complexes.
  • Incorporation of CFn-SDC into oil-in-water submicron emulsion (SE-CFn-SDC) and characterization (globule size, zeta potential, viscosity, TEM, entrapment efficiency, in vitro release).
  • Cytotoxicity assessment on J774 macrophage cells.
  • Chitosan modification of SE-CFn-SDC (SE-CH-CFn-SDC) and in vitro antimicrobial testing against E. coli, S. aureus, and P. aeruginosa.
  • In vivo pharmacokinetic studies in male Balb/c mice.

Main Results:

  • Ion-pairing significantly improved ciprofloxacin entrapment efficiency (≥80%) compared to free CFn (27.2±3.1%).
  • Formulations exhibited good biocompatibility with over 90% cell viability at high concentrations.
  • SE-CH-CFn-SDC showed a two-fold and four-fold enhancement in antimicrobial efficacy against tested bacteria compared to SE-CFn-SDC and SE-CFn, respectively.
  • In vivo studies demonstrated a 1.7-fold and 5-fold increase in AUC(0-24h) for SE-CH-CFn-SDC compared to SE-CFn-SDC and CFn solution, respectively.

Conclusions:

  • Surfactant-based ionic complex formation is a promising strategy to enhance the payload efficiency of poorly water-soluble drugs.
  • Surface modification of submicron emulsions with chitosan can significantly improve antimicrobial efficacy.
  • The developed SE-CH-CFn-SDC formulation offers improved antimicrobial activity and pharmacokinetic profile, representing a promising approach for ciprofloxacin delivery.

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