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Vol. 84, Issue 2, 717-725, February 1998
Departments of 1 Chemical Engineering, 2 Medicine, and 3 Pharmaceutics, University of Illinois at Chicago, Chicago, Illinois 60612
Pillai, Raviraj S., Donovan B. Yeates, Irving F. Miller, and
Anthony J. Hickey. Controlled dissolution from wax-coated aerosol
particles in canine lungs. J. Appl.
Physiol. 84(2): 717-725, 1998.
Treatment of
pulmonary and systemic diseases may be improved and toxicity reduced by
pulmonary deposition of drug-containing aerosols exhibiting delayed
dissolution. Aqueous disodium fluorescein and pentamidine aerosols were
dried, concentrated, and condensation coated with paraffin wax. The
apparent mass median aerodynamic diameters of the coated fluorescein
particles were 2.8-4.0 µm. Wax-to-fluorescein ratios were
0.38-1.05. The dissolution half times determined using a
single-pass flow system were 1.5 min for uncoated fluorescein and 0.8 min for uncoated pentamidine. These increased over threefold when the
aerosols were coated with paraffin wax to maxima of 5.3 and 2.6 min,
respectively. Wax-coated aerosols generated from fluorescein mixed with
99mTc-labeled iron oxide colloid
delivered to the canine lungs demonstrated a 3.4-fold increase in the
absorption half time of disodium fluorescein compared with uncoated
fluorescein (11.2 vs. 38.4 min). The absence of changes in pulmonary
function on inhalation of these wax-coated aerosols, together with a
high drug load and delayed release, establishes a foundation for future
therapeutic applications.
paraffin wax; particle dissolution; aerosol concentrator; pentamidine; disodium fluorescein
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