Authors: Md. Faiyazuddin^a,b,∗, Niyaz Ahmad^a, Roop K. Khar^a, Aseem Bhatnagar^c, Farhan J. Ahmad^a,∗∗

^a Nanomedicine Research Lab, Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, New Delhi 110062, India

^b Faculty of Pharmacy, Integral University, Lucknow 226026, Uttar Pradesh, India

^c Division of Nuclear Medicine, Institute of Nuclear Medicine & Allied Sciences (INMAS), Brig. S. K. Majumdar Road, Delhi 110054, India

International Journal of Pharmaceutics 434 (2012) 59– 69

Abstract:

Terbutaline submicron particles (SµTBS) were prepared by nanoprecipitation technique followed by spray drying for deep lungs deposition. Inhalable SµTBS particles were 645.16 nm of diameter with 0.11 µm of MMAD, suggested for better aerosol effects. Both submicron and micron-sized TBS particles were administered in rodents administered via major delivery routes, and their biological effects were compared by using UHPLC/ESI-q-TOF-MS method. TBS was found stable in all exposed conditions with 96.28–99.0% of recovery and <4.34% of accuracy (CV). An inhalation device was designed and validated to deliver medicines to lungs, which was found best at dose level of 25 mg for 30 min of fluidization. Both submicron and micron particles were compared for in vivo lung deposition and a 1.67 fold increase in concentration was observed for SµTBS exposed by inhalation. Optimized DPI formulation contained lesser fraction of ultrafine particle (<500 nm) with the major fraction of submicron particles (>500 nm), advocated for better targeting to lungs. UHPLC/ESI-q-TOF-MS confirmed that a designed submicron particle has been successfully delivered to the lungs. From tongue to lungs, the landing of pulmonary medicines can be improved by submicronization technology.

http://www.sciencedirect.com/science/article/pii/S0378517312004632