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.

AAPS Pharmscitech
|January 24, 2019
PubMed

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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