Electrosprayed co-crystals of levofloxacin for inhalation: a strategy for excipient-free dry powder antibiotics

Pulmonary delivery of antibiotics provides a targeted means of treating lower respiratory tract infections, yet the development of dry powder inhaler (DPI) formulations is limited by the poor aqueous solubility and physical instability of many active pharmaceutical ingredients. Here, we report a dual-platform strategy that combines mechanochemical co-crystallisation and electrospraying to produce, for the first time, an excipient-free inhalable formulation of levofloxacin (LEV). Three GRAS-listed co-formers-fumaric acid, salicylic acid, and isonicotinic acid-were screened using liquid-assisted grinding. Co-crystals of LEV with salicylic acid (SA) and isonicotinic acid (IN) were identified as crystalline, thermally stable, and physically robust. These co-crystals were processed via cone-jet electrospraying, yielding uniform, spherical microparticles with aerodynamic diameters below 5 µm, suitable for deep-lung deposition. Powder X-ray diffraction and microscopy confirmed that co-crystal integrity and morphology were preserved throughout electrospraying. This work establishes a scalable, low-temperature manufacturing platform for producing high-performance, excipient-free inhalable antibiotics. Beyond levofloxacin, this approach provides a general framework for on-demand, personalised pulmonary drug delivery, bridging solid-state chemistry with advanced particle engineering.

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Publication Details

Journal
International Journal of Pharmaceutics
Published
2025-12-02
DOI
https://doi.org/10.1016/j.ijpharm.2025.126454
Citations
2
Primary Topic
Inhalation and Respiratory Drug Delivery
Type
article
Field-Weighted Citation Impact
3.04
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article

Electrosprayed co-crystals of levofloxacin for inhalation: a strategy for excipient-free dry powder antibiotics

Xiaojie Sun, Bernardo Castro‐Dominguez, Vrinda Raninga, Christina Hage
2 citations
International Journal of Pharmaceutics
Inhalation and Respiratory Drug Delivery
3.04
article

Electrosprayed co-crystals of levofloxacin for inhalation: a strategy for excipient-free dry powder antibiotics

Xiaojie Sun, Bernardo Castro‐Dominguez, Vrinda Raninga, Christina Hage
article en
2 citations

Abstract

Pulmonary delivery of antibiotics provides a targeted means of treating lower respiratory tract infections, yet the development of dry powder inhaler (DPI) formulations is limited by the poor aqueous solubility and physical instability of many active pharmaceutical ingredients. Here, we report a dual-platform strategy that combines mechanochemical co-crystallisation and electrospraying to produce, for the first time, an excipient-free inhalable formulation of levofloxacin (LEV). Three GRAS-listed co-formers-fumaric acid, salicylic acid, and isonicotinic acid-were screened using liquid-assisted grinding. Co-crystals of LEV with salicylic acid (SA) and isonicotinic acid (IN) were identified as crystalline, thermally stable, and physically robust. These co-crystals were processed via cone-jet electrospraying, yielding uniform, spherical microparticles with aerodynamic diameters below 5 µm, suitable for deep-lung deposition. Powder X-ray diffraction and microscopy confirmed that co-crystal integrity and morphology were preserved throughout electrospraying. This work establishes a scalable, low-temperature manufacturing platform for producing high-performance, excipient-free inhalable antibiotics. Beyond levofloxacin, this approach provides a general framework for on-demand, personalised pulmonary drug delivery, bridging solid-state chemistry with advanced particle engineering.

International Journal of PharmaceuticsVol. 688
University of Bath (GB)
Openalex Percentile: Top 7%
Inhalation and Respiratory Drug Delivery
3.04
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