Production and characterization of a budesonide nanosuspension for pulmonary administration.
OBJECTIVE
This study describes the production of a budesonide nanosuspension by high-pressure homogenization for pulmonary delivery from 40 mL up to 300 mL. The aim was to obtain a nanosuspension that can be nebulized and is also long-term stable.


METHODS
The nanosuspension was produced by high-pressure homogenization. Particle size analysis was performed by laser diffraction and photon correlation spectroscopy. For further particle characterization, zeta potential was determined. To investigate the aerosolization properties, the nanosuspension was nebulized and afterward analyzed on particle size.


RESULTS
It was possible to obtain a long-term stable budesonide nanosuspension. Mean particle size of this nanosuspension was about 500-600 nm, analyzed by photon correlation spectroscopy. Analysis by laser diffraction showed that the diameters 95% and 99% were below 3 microm. Budesonide nanosuspension showed a long-term stability; no aggregates and particle growth occurred over the examined period of 1 year. The PCS diameter before and after aerosolization did not change, and the LD diameters increased negligibly, showing the suitability for pulmonary delivery. The scale-up from 40 mL up to 300 mL was performed successfully.


CONCLUSIONS
High-pressure homogenization is a production method to obtain nanosuspensions with budesonide for pulmonary applica-
Jacobs
Claudia
C
Department of Pharmaceutics, Biopharmaceutics and Biotechnology, Free University of Berlin, Germany.
Müller
Rainer Helmut
RH
D000280:Administration, Inhalation; D000336:Aerosols; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage* / Q000737:chemistry*; D019819:Budesonide / Q000008:administration & dosage* / Q000737:chemistry*; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004339:Drug Compounding; D004353:Drug Evaluation, Preclinical; D004355:Drug Stability; D005079:Excipients; D010316:Particle Size; D013535:Suspensions
D000336:Aerosols; D000893:Anti-Inflammatory Agents; D005079:Excipients; D013535:Suspensions; D019819:Budesonide