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Purpose <p>To develop and evaluate a novel chitosan-coated submicron emulsion (SubE) incorporating a ciprofloxacin-potassium sorbate (CIF-PoS) ionic complex for improved ocular drug delivery, addressing limitations of conventional eye drops such as poor corneal retention and bioavailability.</p> Methods <p>The CIF-PoS complex was prepared via ion-pairing at optimized molar ratios and pH, characterized by ¹H NMR. SubEs were formulated using high-energy emulsification with egg lecithin, Pluronic F-68<sup>®</sup>, and chitosan. Physicochemical properties (droplet size, zeta potential, viscosity, encapsulation efficiency) were assessed. In vitro release was studied via dialysis. Ex vivo antimicrobial efficacy against <i>Pseudomonas aeruginosa</i> biofilms was evaluated using MIC/MBC assays. In vivo corneal retention was examined in Wistar rats using fluorescence microscopy and HPLC-MS for pharmacokinetics. Stability was tested per ICH guidelines.</p> Results <p>The optimized SubE-CN-CIF-PoS exhibited a droplet size of 227.1 ± 5.6&#xa0;nm and a polydispersity index (PdI) of 0.24 ± 0.03, + 33.2 mV zeta potential, 91.43% encapsulation efficiency, and sustained release (78% over 24&#xa0;h). It showed comparable MIC (0.0051&#xa0;µg/mL) and MBC (0.0114&#xa0;µg/mL) compared to marketed CIF formulations (MF). In vivo, it maintained therapeutic corneal levels for 12&#xa0;h (20.9% higher than controls). Stability was robust over 6 months.</p> Conclusion <p>This biomimetic system enhances corneal adhesion, penetration, and antibacterial action, offering potential for reduced dosing frequency and improved outcomes in ocular infections. No trial registration required as this is preclinical research.</p>

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Chitosan-Modified Submicron Emulsions for Enhanced Ocular Delivery and Antibacterial Efficacy of Ciprofloxacin

  • 期刊论文

  • 发表日期：

    2026年1月13日

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  • Durga Pandey,
  • Preeti Singh,
  • Girijesh Kumar Pandey,
  • Alok Kumar Mahor,
  • Prashant Pandey

摘要

Purpose

To develop and evaluate a novel chitosan-coated submicron emulsion (SubE) incorporating a ciprofloxacin-potassium sorbate (CIF-PoS) ionic complex for improved ocular drug delivery, addressing limitations of conventional eye drops such as poor corneal retention and bioavailability.

Methods

The CIF-PoS complex was prepared via ion-pairing at optimized molar ratios and pH, characterized by ¹H NMR. SubEs were formulated using high-energy emulsification with egg lecithin, Pluronic F-68®, and chitosan. Physicochemical properties (droplet size, zeta potential, viscosity, encapsulation efficiency) were assessed. In vitro release was studied via dialysis. Ex vivo antimicrobial efficacy against Pseudomonas aeruginosa biofilms was evaluated using MIC/MBC assays. In vivo corneal retention was examined in Wistar rats using fluorescence microscopy and HPLC-MS for pharmacokinetics. Stability was tested per ICH guidelines.

Results

The optimized SubE-CN-CIF-PoS exhibited a droplet size of 227.1 ± 5.6 nm and a polydispersity index (PdI) of 0.24 ± 0.03, + 33.2 mV zeta potential, 91.43% encapsulation efficiency, and sustained release (78% over 24 h). It showed comparable MIC (0.0051 µg/mL) and MBC (0.0114 µg/mL) compared to marketed CIF formulations (MF). In vivo, it maintained therapeutic corneal levels for 12 h (20.9% higher than controls). Stability was robust over 6 months.

Conclusion

This biomimetic system enhances corneal adhesion, penetration, and antibacterial action, offering potential for reduced dosing frequency and improved outcomes in ocular infections. No trial registration required as this is preclinical research.