Context: one of the major challenges to drug development today is poor solubility, as estimated 40% of all newly developed drugs are poorly soluble or insoluble in water.
Objective: The aim of this study was to prepare and characterize amorphous nanoparticles of cefixime to enhance water Solubility and oral bioavailability of this drug.
Method: Nanoparticles were prepared by the application ultrasonication method. The 32 factorial design was applied for the optimization of process variables. The factors involve solvent to antisolvent ratio, surfactant concentration and response selected were particle size and % release.
Results: The particle size and zeta potential of optimized batch of amorphous nanoparticles were found to be 206nm and 58.2 mV, respectively. In vitro dissolution rate of cefixime increased significantly by reducing particle size. In vivo test shows that relative bioavailability of amorphous nanoparticles was improved 3.91 and 7.55 fold as compared to marketed formulation and pure drug respectively. Antimicrobial efficacy studies reveal that there was increased zone of inhibition, indicating that solubility of cefixime was improved due to increased surface area.
Conclusion: Thus, from experimental study it can be concluded, cefixime bioavailability can be improved by amorphous nanoparticles which needs to be further proved in human beings.
Keywords: Cefixime, nanoparticles, Ultrasonication, Solvent Antisolvent, Bioavailability.
Introduction:
Nanoparticles are known to improve dissolution rate and bioavailability of poorly water-soluble drugs[1-5] owing to increased surface area available for dissolution, as described by the Noyes–Whitney equation [6]. Nanoparticles are generally obtained by ‘top–down’ process...
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...ctant concentration, solvent antisolvent ratio, the precipitation temperature, and the sonication time length of ultrasonication on the particle size were investigated systematically in preoptimization studies and the optimal values were selected. The 32 factorial design was applied for the selected factors and its responses. The factors involves solvent to antisolvent ratio and surfactant concentration and response selected were particle size and % release. The corresponding physical properties of the prepared freeze dried amorphous nanoparticles were characterized by scanning electronic microscopy (SEM), X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC). The dissolution rate and saturation solubility of nanoparticles were also determined. Finally, the dissolution rate and oral bioavailability of Nanoparticles was evaluated in Wistar rats.
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