PREPARATION OF IRBESARTAN NANOPARTICLES FOR DISSOLUTION RATE ENHANCEMENT
Hatem Sarhan* and Usama F. Aly
ABSTRACT
Nanoparticle technique offers promising methods for the formulation
of poorly water soluble drugs. The objective of the present
investigation was to enhance dissolution and oral bioavailability of
poorly water-soluble irbesartan (IBS) by preparing stable
nanoparticles. IBS nanosuspensions were produced by antisolvent
precipitation under sonication. The physicochemical properties of the
prepared nanoparticles were characterized by differential scanning
calorimetry (DSC), Fourier transform infrared spectroscopy (FT-IR), powder X-ray
diffractometry (PXRD), transmission electron microscopy (TEM) and solubility studies, as
well as measuring the particle size and in-vitro drug dissolution.
The physicochemical results indicated that the antisolvent precipitation process led to the
amorphization of IBS without drug-polymer chemical interaction. IBS nanoparticles
increased the saturation solubility of drug almost sixteen fold. The in vitro studies showed a
marked increase in the drug dissolution rate After 60 min, nanoparticles were almost
dissolved completely but only 53 % of unprocessed IBS and 70 % of physical mixture (PM)
had dissolved owing to its crystalline nature and larger crystal size. The combining of the
methods was a promising method to produce uniform nanoparticles of IBS with remarkable
improvement in dissolution rate.
Keywords: Antisolvent, nanosuspensions, saturation solubility, Hydroxypropyl methyl cellulose, and sodium dodecyl sulfate.
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