Formulation Development and Evaluation Studies of Linezolid Inhaler in the Treatment of Tuberculosis

Abstract

The primary objective of this study was to prepare and evaluate a linezolid inhaler. Dry powder inhaler liposomes were formulated to investigate the efficacy of pulmonary delivery of linezolid for tuberculosis. The liposomes were prepared using soya lecithin and cholesterol in different weight ratios, constant amounts of drugs, and two methods: physical dispersion and ethanol injection. The F9 formulation was characterized for physical and chemical properties such as vesicle size, shape, and zeta potential. The results of physical characterization, in-vitro testing, and stability studies indicate that liposomes containing linezolid can be used for the treatment of tuberculosis. The evaluated batch exhibited favorable physicochemical properties, with spherical liposomes having a mean size below 100 nm and high entrapment efficiency (98.8%). The prepared liposomal dry powder inhalers (DPIs) sustained drug release for up to 8 hours. Liposome stability was assessed 90 days after storage at room temperature, revealing its stability. The liposomal formulation had steady zeta potential, good entrapment efficiency, improved stability, and an extended drug release time. In conclusion, linezolid-loaded liposomal inhalers were successfully formulated.