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Improved Encapsulation and Potential of Liposomal Tosufloxacin via Inclusion in Cyclodextrin
Hemat Mostafa1, Hamid Alghurabi2, Koki Ogawa1
1Drug Delivery and Nano Pharmaceutics, Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-Dori, Mizuho-Ku, Nagoya, 467-8603, Japan.
AAPS Pharmscitech
|November 20, 2025
Summary
Hydroxypropyl-β-cyclodextrin (HP-β-CD) complexation significantly boosted tosufloxacin (TFLX) solubility and liposomal encapsulation efficiency. This dual-delivery system enhanced TFLX
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Antimicrobial Agents
Background:
- Liposomal formulations and intratracheal delivery are advanced strategies for enhancing antimicrobial agent efficacy.
- Tosufloxacin (TFLX), a potent fluoroquinolone, exhibits poor aqueous solubility and low encapsulation efficiency (EE) in liposomes using conventional methods.
- Addressing these limitations is crucial for optimizing TFLX therapeutic potential.
Purpose of the Study:
- To improve the solubility and liposomal loading of tosufloxacin (TFLX) by utilizing hydroxypropyl-β-cyclodextrin (HP-β-CD).
- To develop and characterize a novel TFLX/HP-β-CD liposomal formulation for enhanced antimicrobial delivery.
- To evaluate the physicochemical properties, drug release kinetics, and intracellular antibacterial efficacy of the developed formulation.
Main Methods:
- Preparation of a TFLX/HP-β-CD inclusion complex optimized via phase solubility analysis.
- Incorporation of the TFLX/HP-β-CD complex into liposomes using the thin-film hydration method.
- Characterization using Fourier-transform infrared spectroscopy (FTIR) and X-ray diffraction (XRD), alongside evaluation of encapsulation efficiency, in vitro drug release, and intracellular antibacterial activity against Staphylococcus aureus.
Main Results:
- HP-β-CD complexation increased TFLX solubility approximately 25-fold.
- TFLX/HP-β-CD-liposomes exhibited significantly higher EE (69.7%) compared to conventional TFLX-liposomes (17.9%).
- The formulation demonstrated sustained drug release over 48 hours and superior intracellular antibacterial efficacy against Staphylococcus aureus.
Conclusions:
- The combination of HP-β-CD complexation and liposomal encapsulation effectively enhances TFLX solubility, loading efficiency, and intracellular antimicrobial activity.
- FTIR and XRD analyses confirmed the formation of the TFLX/HP-β-CD inclusion complex.
- This dual-delivery strategy presents a promising platform for formulating poorly water-soluble antimicrobial agents, particularly for lung delivery.
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