Preparation and In Vitro Evaluation of Budesonide Spray Dried Microparticles for Pulmonary Delivery

Abstract

The present study describes development and in vitro evaluation of budesonide microparticles prepared by spray drying for delivering drug directly to lungs via dry powder inhaler. This paper introduces new formulations for pharmaceutical applications which includes conventional formulations and novel spray dried microparticles viz., pulmosols, microspheres and porous particles. Optimized spray drying parameters for generation of microparticles were: inlet temperature, 130 °C; outlet temperature, 80 °C; aspirator rate, 240 mWc (60%); solution feed rate, 2 ml/min; spraying air flow pressure, 2 bar. Microparticles appeared to be spherical, low-density particles characterized by smooth surface. MMAD and GSD ranged from 2.5-4.6 µm and 1.5-2.7 respectively. Effective index of microspheres (54.48) and porous particle formulations (64.22) was higher than the conventional formulation (49.21) indicating more effective deposition of microparticles to the lungs. Carr's Index (20-30%) and Hausner ratio (1.2-1.7) for all formulations indicated good powder flow properties. Formulations emitted a fine particle fraction of 25-47%. Microparticles showed extended in vitro drug release upto 4 hours with high respirable fractions, thus use of microparticles potentially offers sustained release profile along with improved delivery of drug to the pulmonary tract.

Particle formation of budesonide from alcohol-modified subcritical water solutions

“…PEG has been used as an excipient for the pulmonary delivery of budesonide into the lungs (Steckel and Wehle, 2004;Naikwade and Bajaj, 2009). The effect of PEG as a modifier for particle formation in the PC was investigated on the morphology of budesonide.…”

“…The materials were selected based on the common usage of both materials as pharmaceutical excipients. Both lactose and PEG400 were selected because they are commonly used carriers for naproxen and budesonide (Steckel and Wehle, 2004;Nilsson and Santesson, 2001;Nokhodchi et al, 2007;Naikwade and Bajaj, 2009;Kinnarinen et al, 2003). The excipients were added to PC in proportions similar to those found in common API formulations for lung delivery.…”

Hollow microspheres as a drug carrier: An overview of fabrication andin vivocharacterization techniques

“…The drug release modifier and mucoadhesive properties of chitosan exploited while preparing sustained release formulations for pulmonary drug delivery [73] Heparin Eudragit S 100…”

Preparation, characterization and pulmonary pharmacokinetics of xyloglucan microspheres as dry powder inhalation

“…Test conducted at flow rate of 60 L/min for 4 s. For each test formulation, amount particle was determined and analyzed for drug content by UV spectrophotometer (UV-170, Shimadzu, Japan) at 285.5 nm. Starting at the filter, a cumulative mass deposition (undersize in percentage) vs. cut-off diameter of respective stages was derived, the mean mass aerodynamic diameter (MMAD), geometric standard diameter (GSD), fine particle dose (FPD), % fine particle fraction (%FPF) and % mass balance was calculated (Kundawala, Vishnu, & Patel, 2011;Naikwade & Bajaj, 2009). FPF considered as directly proportional to the amount of drug able to reach the pulmonary tract in vivo: consequently, higher the percentage of FPF, deeper the estimated lung deposition will be.…”