چکیده (انگلیسی):

The present study investigates the preparation of celecoxib-
loaded albumin microspheres and the biodistribution
of technetium-99m (99mTc)-labeled celecoxib as well as its
microspheres after intravenous administration. Microspheres
were prepared using a natural polymer BSA using
emulsification chemical cross-linking method. The prepared
microspheres were characterized for entrapment efficiency,
particle size, and in vitro drug release. Surface
morphology was studied by scanning electron microscopy.
Biodistribution studies were performed by radiolabeling
celecoxib (CS) and its microspheres (CMS) using 99mTc
and injecting arthritic rats intravenously. The geometric
mean diameter of the microspheres was found to be
5.46 mm. In vitro release studies indicated that the microspheres
sustained the release of the drug for 36 days.
Radioactivity measured in different organs after intravenous
administration of celecoxib solution showed a significant
amount of radioactivity in the liver and spleen. In case
of celecoxib-loaded microspheres, a significant amount of
radioactivity accumulated in the lungs. No significant difference
(P > .1) in the radioactivity was observed between
the inflamed joint and the noninflamed joint following
intravenous injection of 99mTc-CS. However, in case of the
microspheres (CMS), the radioactivity present in the
inflamed joint was 2.5-fold higher than in the noninflamed
joint. The blood kinetic studies revealed that celecoxibloaded
albumin microspheres exhibited prolonged circulation
than the celecoxib solution.