PULMONARY DRUG DLIVERY SYSTEMS OF POSACONAZOLE : DEVELOPMENT AND OPTIMIZATION THROUGH QUALITY BY DESIGN

Pulmonary delivery of posaconazole

Abstract

Objective:  The main objective of this work is formulation of nano-embedded microparticles of Posaconazole  for targeted delivery into lungs through pulmonary route. 

Methods: PNCs were developed through quality by design  approach. Influences of sonication time, sonication power, stabilizer type and its concentration on the solubility and time for 90% drug dissolution (T90%) of the PNC were studied through central composite design. NMPs were developed by nano-crystallization using surfactants to enhance the solubility of Posaconazole and then  the optimized PNCs were embedded into lactose matrix to enhance the size through lyophilization to obtain NMPs that were suitable for inhalational administration.

Results:The optimized formulation was found to exhibit a particle size of 159.2 nm, solubility of 0.29 mg/mL and T90% of 24.7 min. this optimized PNCs were embedded into lactose using lyophilization. the lyophilized product was sieved to obtain a size below 5 µm.

Conclusion: The optimized formulation  is highly suitable for delivering the drug to lungs through inhalation in which drug particles reach secondary bronchi where they can dissolve readily to yield PNCs. These PNCs can easily escape into alveolar fluids for immediate local action.