Research and Development of a New Safe Form of Drugs - Aerosols: Measurement, Dosimetry, and Health Effects - page 263

100 µm
FIGURE 11.16 Cross section of the lung from a mouse treated with 100 nm ibuprofen nanoparticles showing
a pronounced venous and arterial hyperemia as well as dilatation of bronchioli and alveolar channels, alveolar
wall thinning, and partial capillary bed reduction.
during the substance evaporation). The x-ray diffraction analysis showed that the indomethacin
nanoparticles were amorphous and the ibuprofen nanoparticles have the crystalline structure identi-
cal to that of the maternal substance.
The lung-deposited dose versus nanoparticle diameter was measured using the NOE chambers.
The mice lung deposition eficiency was evaluated as a function of the particle diameter changing
from about unity at d = 10 nm to about 0.2 at d = 100 nm.
The dose-dependent effect of aerosolized indometacin and ibuprofen was studied in comparison
with the oral treatment. It was found that aerosol administration is much more effective than the oral
delivery; thus, the aerosol treatment needs the dose a 3-6 orders of magnitude less than the oral one
at the same analgesic or anti-inlammatory effect.
However, the lung histology analysis for the mice treated with the small particles ( d = 9 nm) at
dose as small as 10 −5 mg per kg bw has revealed emphysematous signs like the dilatation of bron-
chioles and alveolar channels, alveolar wall thinning and partial capillary bed reduction.
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