Formulation, characterization and evaluation of inhalable effervescent dry powder of Rifampicin nanoparticles

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Nanotechnology

Background:

• Dry powder inhalers (DPIs) are key for pulmonary tuberculosis treatment.
• Lactose nanoparticles offer deep lung deposition but poor dispersion.
• Rifampicin nanoparticles target alveolar macrophages, enhancing tuberculosis treatment efficiency and reducing side effects.

Purpose of the Study:

• To formulate and optimize rifampicin nanoparticles using nano-precipitation.
• To characterize an effervescent DPI for rifampicin nanoparticles using citric acid and sodium bicarbonate.
• To improve nanoparticle redispersibility and lung deposition for enhanced tuberculosis therapy.

Main Methods:

• Rifampicin nanosuspension formulated via nano-precipitation with lecithin stabilizer.
• Optimization of drug and stabilizer concentrations using a 3*2 factorial design.
• Preparation of spray-dried powder using an effervescent carrier (citric acid and sodium bicarbonate).

Main Results:

• The effervescent formulation achieved monodispersity with a particle size of 1.5 microns (PDI 0.289).
• Demonstrated superior redispersibility compared to traditional lactose nanoparticles.
• Spray-dried formulations exhibited suitable mass median aerodynamic diameter for deep lung deposition.

Conclusions:

• The effervescent technique effectively enhances the redispersibility of rifampicin nanoparticles.
• This approach holds promise for improved pulmonary drug delivery in tuberculosis treatment.
• The developed DPI formulation is suitable for deep lung deposition, potentially increasing therapeutic efficacy.