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Purpose <p>The aim of this study was to develop a ciprofloxacin pamoate (CIP-PAM)-loaded liposomal dry powder as an inhalable formulation using hydrophobic ion pairing (HIP) to improve liposomal entrapment efficiency, and to evaluate whether the ion-paired liposomal system could maintain its nanoparticle characteristics after dry powder processing.</p> Methods <p>CIP-PAM was prepared using HIP and incorporated into liposomes using the thin-film hydration method. The liposomal characteristics were compared with those of ciprofloxacin HCl-loaded liposomes. Cryoprotectants were screened to preserve the liposomal properties during lyophilization, and the selected formulation was further processed into an inhalable dry powder by jet milling with magnesium stearate. The physicochemical properties, in-vitro release, solid-state characteristics, and aerodynamic performance were evaluated.</p> Results <p>CIP-PAM-loaded liposomes showed significantly higher entrapment efficiency than ciprofloxacin HCl-loaded liposomes (95.8 ± 1.3% vs. 24.5 ± 0.8%, <i>p</i> &lt; 0.0001) while maintaining a nanosized particle distribution. Lactose at a lipid-to-cryoprotectant ratio of 1:5 optimally preserved the liposomal characteristics after lyophilization, with no significant change in particle size or entrapment efficiency compared to those of the original liposomes. Transmission electron microscopy and in-vitro release studies confirmed that the liposomal structure and sustained release behavior were maintained after lyophilization and reconstitution. The final jet-milled dry powder exhibited a favorable aerosol performance, with an emitted dose of 93.3 ± 1.6% and a fine particle fraction of 46.7 ± 1.0%.</p> Conclusion <p>HIP effectively improved ciprofloxacin loading into liposomes, and an appropriate formulation design enabled successful conversion into an inhalable liposomal dry powder while preserving liposomal characteristics after powder processing.</p>

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Preparation and characterization of hydrophobic ion paired ciprofloxacin-loaded inhalable liposomal dry powder

  • 期刊论文

  • 发表日期：

    2026年7月29日

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  • Yuim Jeon,
  • Jong-Ju Lee,
  • Minji Choi,
  • Solyi Yoo,
  • Jaesik Jang,
  • Suwon Jung,
  • Waiting Tai,
  • Patricia Tang,
  • Hak-Kim Chan,
  • Sung-Joo Hwang

摘要

Purpose

The aim of this study was to develop a ciprofloxacin pamoate (CIP-PAM)-loaded liposomal dry powder as an inhalable formulation using hydrophobic ion pairing (HIP) to improve liposomal entrapment efficiency, and to evaluate whether the ion-paired liposomal system could maintain its nanoparticle characteristics after dry powder processing.

Methods

CIP-PAM was prepared using HIP and incorporated into liposomes using the thin-film hydration method. The liposomal characteristics were compared with those of ciprofloxacin HCl-loaded liposomes. Cryoprotectants were screened to preserve the liposomal properties during lyophilization, and the selected formulation was further processed into an inhalable dry powder by jet milling with magnesium stearate. The physicochemical properties, in-vitro release, solid-state characteristics, and aerodynamic performance were evaluated.

Results

CIP-PAM-loaded liposomes showed significantly higher entrapment efficiency than ciprofloxacin HCl-loaded liposomes (95.8 ± 1.3% vs. 24.5 ± 0.8%, p < 0.0001) while maintaining a nanosized particle distribution. Lactose at a lipid-to-cryoprotectant ratio of 1:5 optimally preserved the liposomal characteristics after lyophilization, with no significant change in particle size or entrapment efficiency compared to those of the original liposomes. Transmission electron microscopy and in-vitro release studies confirmed that the liposomal structure and sustained release behavior were maintained after lyophilization and reconstitution. The final jet-milled dry powder exhibited a favorable aerosol performance, with an emitted dose of 93.3 ± 1.6% and a fine particle fraction of 46.7 ± 1.0%.

Conclusion

HIP effectively improved ciprofloxacin loading into liposomes, and an appropriate formulation design enabled successful conversion into an inhalable liposomal dry powder while preserving liposomal characteristics after powder processing.