Open AccessCondensational growth of combination drug‐excipient submicrometer particles for targeted high‐efficiency pulmonary delivery: evaluation of formulation and delivery device
Author(s) -
Hindle Michael,
Longest P. Worth
Publication year - 2012
Publication title -
journal of pharmacy and pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.745
H-Index - 118
eISSN - 2042-7158
pISSN - 0022-3573
DOI - 10.1111/j.2042-7158.2012.01476.x
Subject(s) - excipient , aerosol , dry powder inhaler , drug delivery , inhaler , particle size , active ingredient , dosage form , materials science , chemistry , chromatography , nanotechnology , pharmacology , medicine , asthma , organic chemistry
Objectives The objective of this study was to investigate the in‐vitro particle‐size growth of combination drug and excipient submicrometer aerosols generated from a series of formulations and two aerosol delivery devices. Methods Submicrometer combination drug and excipient particles were generated experimentally using both the capillary aerosol generator and the Respimat inhaler. Budesonide and albuterol sulfate were used as model drugs and were formulated with sodium chloride, citric acid and mannitol as excipients in various ratios. Aerosol growth was evaluated in‐vitro in a coiled‐tube geometry designed to provide residence times and thermodynamic conditions consistent with the airways. Key findings Submicrometer combination drug : excipient aerosols when exposed to simulated respiratory conditions increased to micrometer size suitable for pulmonary deposition. It was possible to control the aerosol growth ratio by altering: (1) the hygroscopic excipient, (2) the drug : excipient ratio and (3) the drug. The applicability of this approach was demonstrated using the capillary aerosol generator and the Respimat inhaler. Conclusions The enhanced excipient growth approach may enable the delivery of submicrometer aerosol particles that increase in size within the airways and result in high percentages of pulmonary deposition.