Design and evaluation of microspheres loaded with nizatidine

Abstract

A  novel  ionotropic  gelation  technique  was  employed  to  design  and  develop  sustained  release  Nizatidine microspheres for oral administration. Calcium chlorid e was selected as cross linking agent and sodium alginate as polymer to control the release profile of the Nizatidine from microspheres. The S1 to S14 formulations were subjected to micromeritic properties, swelling index, % yield, encapsulation efficiency and in vitro drug release. Fourier transform infrared spectroscopy (FTIR) and scanning electron microscope (SEM) were characterized for the prepared microspheres. The optimal formulation used for fabrication of microspheres was dispersion with 2% (w/v) sodium alginate, 10% (w/v) calcium chloride, and the drug Nizatidine content was 450mg based on solid weight in the dispersion. It was indicated that Nizatidine had no interactions with excipient by the FTIR and DSC. The optimized formulation (S6) showed the particle size, bulk density, tapped density, angle of repose,  Carr’s  index  and  swelling  index  of  82.45±0.09  µm,  0.52g/ml,  0.59g/ml,  20˚.54,  7.95%,  97%, respectively. The % yield, %EE and Cumulative % drug release of  S6 was found to be 98.3%, 96.3% and 98.54%,  respectively. The  in  vitro  drug  release  was  showed  the  98.07±0.46% within  12h.  The  optimized formulation followed the Zero order and Higuchi kinetics indicated the diffusion controlled release mechanism. SEM studies showed the optimized formulation ha d particles of spherical in shape. The optimized formulation S6 was found to stable. All the results proved that the ionotropic gelation is a novel and promising technique for preparing  sustained-release microspheres, and  suitable  for  industrial  production  due  to  its  successive  and controllable step in preparation.