ArticleInternational journal of nanomedicine2026
Inhalable Nanocrystal-in-Microparticle of Linezolid in Pulmonary Tuberculosis.
Article in International journal of nanomedicine, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
Background: Tuberculosis (TB) remains a major global health challenge, necessitating the development of advanced pulmonary drug delivery systems to improve therapeutic efficacy. Linezolid (LZD), a second-line oxazolidinone antibiotic, is effective against multidrug-resistant Objective: This study aimed to engineer and optimise LZD nanocrystals (LZD-NCs) in microparticles for dry powder inhalation (DPI) using a Quality by Design (QbD)-based Central Composite Design (CCD) approach to enhance localised pulmonary delivery. Methods: LZD-NCs were initially prepared by high-pressure homogenization (HPH) and subsequently converted into respirable nanocrystals in microparticles (LZD-NIM) using spray drying. The LZD-NCs formulation was optimised using CCD. The developed formulation was evaluated for physicochemical characteristics, including solid-state characterisation, in vitro drug-release study, kinetic study, and aerosolisation behaviour and stability. Results: The optimised formulation exhibited an average particle size of 239.5 ± 16.30 nm, polydispersity index (PDI) of 0.285 ± 0.042, and surface charge of -34.5 ± 1.84 mV, indicating acceptable colloidal stability. Later, NIM effectively retained the physicochemical integrity of LZD-NCs. The developed NIM formulation exhibited improved drug release of 61.39% over 24 h, compared with pure LZD at 37.26%. An in vitro aerosolisation study demonstrated appropriateness for deep lung deposition of NIM with a mass median aerodynamic diameter (MMAD) of 2.9 ± 0.15 µm and high fine particle fractions (FPF) of 76.12 ± 1.3%. Conclusion: The engineered LZD-NIM successfully yielded a highly stable, aerodynamically efficient DPI platform with sustained drug release kinetics. The engineered platform demonstrates its potential as an effective pulmonary drug-delivery system for TB treatment.
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