FORMULATION AND EVALUATION OF MUCOADHESIVE MICROSPHERES OF SERTRALINE FOR IMPROVING BIOAVAILABILITY

Abstract

The objective of the current investigation was to optimize and formulate mucoadhesive microspheres loaded with sertraline utilizing guar gum as the mucoadhesive polymer and stabilizing the particles with magnesium stearate so that the formulation could control the release of the drug thereby reducing its dosing frequency and improving the bioavailability. The microspheres were prepared using emulsion coacervation method and the micromeritic features were evaluated. The angle of repose was measured using the fixed funnel method and was found to be ranging from 21.57 ± 0.121 to 28.14 ± 0.620. This indicates that good flow property of powder blend. The bulk and tapped density of the formulations ranged from 0.379 ± 0.009 to 0.608 ± 0.002 g/cm3 and 0.408 ± 0.003 to 0.735 ± 0.006 g/cm3 respectively. The values of Hausner’s ratio ranged from 1.04 to 1.25 whereas the Carr’s Index ranged from 3.92 to 19.94. The yield of all the batches of microspheres was found to be reasonably good ranging from 50.69 % to 73.84 %. The drug loading was found to be 68.35 ± 0.221 to 72.63 ± 0.535 % while the size of microspheres ranged from 13.64 ± 0.055 μm to 17.90 ± 0.121 μm. Swelling study was performed on all the formulation for 24 h and swelling index ranged from 2.69 to 4.72. The optimization was done and the optimized formulation was studied for particle size, mucoadhesion time and in vitro release. The particles size of the optimized formulation was found to be 13.92 μm with polydispersity index of 0.301. The mucoadhesion time of the formulation was obtained to be 6 h 08 min. The in vitro release of sertraline was studied for 12 h and it was found that the microsphere formulation was able to sustain the release of the drug for more than 12 h with 73.5 % drug released at the end of the 12th hour.