Search

Introduction: The critical and complex properties of Biopharmaceutics Classification System Class II quetiapine fumarate active pharmaceutical ingredient molecules that complicate effective oral delivery of these active pharmaceutical ingredients include low aqueous solubility and reduced bioavailability. Objective: The objective of this investigation is to develop a nanosuspension formulation of quetiapine fumarate using media milling techniques to effectively reduce particle size and enhance dissolution rate. Method: Quetiapine fumarate Nano suspensions were prepared by the media milling method. The milling process was optimized by studying the effects of critical process parameters on the size of nanosuspension using a factorial design approach. The prepared nanosuspension is subjected to various characterization techniques such as Particle size, Zeta Potential, differential scanning calorimetry, X-ray powder diffraction, scanning electron microscopy, and in vitro dissolution rate assessment. Results: The obtained results demonstrate that the average particle size of the prepared nanosuspensions is 225 nm with a Polydispersity index of 0.530, while the average Zeta potential is -38.2 mv. The crystalline structure of quetiapine fumarate nano-suspension is evident from differential scanning calorimetry and X-ray powder diffraction. Conclusion: The dissolution rate of the nanosuspension is significantly faster than that of pure Quetiapine Fumarate, and the Cumulative drug release (%) of nanosuspension is higher than that of pure Quetiapine Fumarate, indicating that the use of nanotechnology can considerably enhance the dissolution rate. [ABSTRACT FROM AUTHOR]

Background: Pyrazinamide is a Biopharmaceutical Classification System class III antibiotic indicated for active tuberculosis. Methods: In the present work, pyrazinamide-loaded biodegradable polymeric nanoparticles (PNPs) based dry powder inhaler were developed using the double emulsion solvent evaporation technique and optimized using design of experiments to provide direct pulmonary administration with minimal side effects. Batches were characterized for various physicochemical and aerosol performance properties. Results: Optimized batch exhibited particle size of 284.5 nm, % entrapment efficiency of 71.82%, polydispersibility index of 0.487, zeta potential of −17.23 mV, and in vitro drug release at 4 hours of 79.01%. Spray-dried PNPs were evaluated for drug content, in vitro drug release, and kinetics. The particle mass median aerodynamic diameter was within the alveolar region's range (2.910 μm). In the trachea and lung, there was a 2.5- and 1.2-fold increase in in vivo deposition with respect to pure drug deposition, respectively. In vitro drug uptake findings showed that alveolar macrophages with pyrazinamide PNPs had a considerably higher drug concentration. Furthermore, accelerated stability studies were carried out for the optimized batch. Results indicated no significant change in the evaluation parameters, which showed stability of the formulation for at least a 6-month period. Conclusion: PNPs prepared using biodegradable polymers exhibited efficient pulmonary drug delivery with decent stability. [ABSTRACT FROM AUTHOR]