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Published on: April 6, 2017
Novel Inhalable Ciprofloxacin Dry Powders for Bronchiectasis Therapy: Mannitol-Silk Fibroin Binary Microparticles
Chunxia Liu1,2, Ling Lin3, Zhengwei Huang3
1Department of Pharmacy, Sun Yat-Sen Memorial Hospital, Sun Yat-sen University, No.132 Xingang West Road, Haizhu District, Guangzhou, 510120, People's Republic of China.
Abstract:
Non-cystic fibrosis bronchiectasis (NCFB) is a chronic respiratory disease associated with the high morbidity and mortality. Long-term intermittent therapy by inhalable antibiotics has recently emerged as an effective approach for NCFB treatment. However, the effective delivery of antibiotics to the lung requires administering a high dose to the site of infection. Herein, we investigated the novel inhalable silk-based microparticles as a promising approach to deliver high-payload ciprofloxacin (CIP) for NCFB therapy. Silk fibroin (SF) was applied to improve drug-payload and deposit efficiency of the dry powder particles. Mannitol was added as a mucokinetic agent. The dry powder inhaler (DPI) formulations of CIP microparticles were evaluated in vitro in terms of the aerodynamic performance, particle size distribution, drug loading, morphology, and their solid state. The optimal formulation (highest drug loading, 80%) exhibited superior aerosolization performance in terms of fine particle fraction (45.04 ± 0.84%), emitted dose (98.10 ± 1.27%), mass median aerodynamic diameter (3.75 ± 0.03 μm), and geometric standard deviation (1.66 ± 0.10). The improved drug loading was due to the electrostatic interactions between the SF and CIP by adsorption, and the superior aerosolization efficiency would be largely attributed to the fluffy and porous cotton-like property and low-density structure of SF. The presented results indicated the novel inhalable silk-based DPI microparticles of CIP could provide a promising strategy for the treatment of NCFB.
Insights
Novel inhalable silk-based microparticles effectively deliver high-payload ciprofloxacin for non-cystic fibrosis bronchiectasis (NCFB) treatment. These silk fibroin microparticles demonstrate superior aerosolization, offering a promising strategy for NCFB therapy.
Area of Science:
- Biomaterials Science
- Respiratory Medicine
- Pharmaceutical Technology
Background:
- Non-cystic fibrosis bronchiectasis (NCFB) presents significant morbidity and mortality.
- Inhalable antibiotics are an emerging effective therapy for NCFB.
- Efficient lung delivery necessitates high antibiotic doses at the infection site.
Purpose of the Study:
- To investigate novel inhalable silk-based microparticles for high-payload ciprofloxacin (CIP) delivery in NCFB.
- To enhance drug loading and deposition efficiency using silk fibroin (SF).
- To evaluate the aerodynamic performance of CIP-loaded dry powder inhaler (DPI) formulations.
Main Methods:
- Silk fibroin (SF) was used to create microparticles for high drug loading.
- Mannitol was incorporated as a mucokinetic agent.
- In vitro evaluation of DPI formulations included aerosolization performance, particle size, drug loading, morphology, and solid state.
Main Results:
- The optimal formulation achieved 80% drug loading.
- Superior aerosolization performance was observed: fine particle fraction (45.04%), emitted dose (98.10%), mass median aerodynamic diameter (3.75 μm), and geometric standard deviation (1.66).
- Improved drug loading resulted from electrostatic interactions between SF and CIP; enhanced aerosolization was attributed to the fluffy, porous, low-density structure of SF.
Conclusions:
- Inhalable silk-based DPI microparticles offer a promising strategy for NCFB treatment.
- The high drug payload and efficient aerosolization support their therapeutic potential.
- This approach addresses the challenge of effective antibiotic delivery to the lungs in NCFB.
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