Effervescent dry powder for respiratory drug delivery - Spray Drying

Effervescent dry powder for respiratory drug delivery
Received 4 July 2006; revised 23 October 2006; accepted 24 October 2006. Available online 7 November 2006.
Leticia Elya, Wilson Roab, Warren H. Finlayc and Raimar L?benberga
European Journal of Pharmaceutics and Biopharmaceutics
Article in Press
ScienceDirect
Copyright ? 2006 Elsevier B.V. All rights reserved
Abstract
The objective of this work was to develop a new type of respiratory drug delivery carrier particle that incorporates an active release mechanism. Spray drying was used to manufacture inhalable powders containing polybutylcyanoacrylate nanoparticles and ciprofloxacin as model substances for pulmonary delivery. The carrier particles incorporated effervescent technology, thereby adding an active release mechanism to their pulmonary route of administration. Effervescent activity of the carrier particles was observed when the carrier particles were exposed to humidity. Gas bubbles caused by the effervescent reaction were visualized by confocal laser scanning microscopy. The images showed that nanoparticles were distributed throughout the gas bubble. For the effervescent formulation the average mass median aerodynamic diameter (MMAD) was 2.17 ?m ? 0.42, fine particle fraction (FPF<=5.6 ?m) was 46.47% ? 15 and the GSD was 2.00 ? 0.06. The results also showed that the effervescent carrier particles released 56 ? 8% ciprofloxacin into solution compared with 32 ? 3% when lactose carrier particles were used. The mean nanoparticle size did not significantly change upon release when the nanoparticles were incorporated into an effervescent formulation. However, the mean size significantly increased upon release when only lactose was used as carrier particle matrix. In conclusion, effervescent carrier particles can be synthesized with an adequate particle size for deep lung deposition. This opens the door for future research to explore this technology for delivery of a large range of substances to the lungs with possible improved release compared to conventional carrier particles.
Keywords: Effervescent; Inhalable dry powders; Nanoparticles; Pulmonary delivery; Aerosol; Drug delivery; Ciprofloxacin; Spray drying
Corresponding author. 3126 Dentistry/Pharmacy Centre, Faculty of Pharmacy, University of Alberta, Edmonton, AB, Canada T6G 2G8. Tel.: +1 780 492 1255; fax: +1 780 492 1217.
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