Formulation and Characterisation of Isoniazid by Spray Drying for use by Dry Powder Inhalers to treat Tuberculosis

Damiana Gabrielli, South East Technological UniversityFollow
Seán Roche, South East Technological UniversityFollow

Author ORCID Identifier

0009-0003-0712-2924

Abstract

The targeted delivery of antibiotics by dry powder inhalers (DPIs) is an increasingly important area of research, driven by the growing global burden of respiratory infections and the advantages of localized drug delivery to the lungs. Over the past five years, respiratory infections have risen significantly, with recent epidemiological data indicating a global increase in incidence by over 30%, largely due to factors such as air pollution, antimicrobial resistance, and emerging respiratory pathogens. One major challenge in developing DPI formulations for antibiotics is the need to optimize the particle physicochemical properties for deep lung deposition while accommodating the high doses required for efficacy. Respiratory diseases remain a leading cause of mortality worldwide, with tuberculosis (TB) being a major contributor. Isoniazid, a first-line antibiotic for TB treatment, was the focus of this project, which aimed to develop spray-dried, carrier-free formulations using various excipients. The formulations included combinations with l-leucine, l-isoleucine, trileucine, DPPC, soy lecithin, and ammonium hydrogen carbonate. Among these, trileucine demonstrated superior formulation stability compared to l-leucine, with both amino acids acting as surface-active agents to prevent particle agglomeration. Isoniazid:trileucine and isoniazid:DPPC formulations produced small, uniform particles suitable for inhalation. Their aerosolization performance was evaluated using the Cyclohaler® device and Next Generation Impactor. The isoniazid:trileucine formulation achieved a fine particle fraction (FPF) of 43.809% and an emitted dose (ED) of 82.7%, making it suitable for deep lung and alveolar delivery. In contrast, the isoniazid:DPPC formulation, with an FPF of 30.674% and ED of 81.3%, appeared more appropriate for bronchial region targeting.

Recommended Citation

Gabrielli, Damiana and Roche, Seán (2025) "Formulation and Characterisation of Isoniazid by Spray Drying for use by Dry Powder Inhalers to treat Tuberculosis," SURE Journal: Science Undergraduate Research Experience Journal: Vol. 7: Iss. 2, Article 8.
Available at: https://arrow.tudublin.ie/sure_j/vol7/iss2/8