Optimization of Ethyl Cellulose Microspheres Containing Satranidazole Using 32 Factorial Design

Abstract

Intestinal amoebiasis is an infection of the large intestine caused by microscopic one-celled parasites, Entamoeba histolytica. Intestinal amoebiasis has a worldwide distribution and many drugs are available for the same. For better management of intestinal amoebiasis, satranidazole is a potent drug. For its successful delivery to colon, satranidazole must be protected in gastrointestinal tract and then released later in colon. This delayed drug delivery can be achieved using microspheres of satranidazole. Thus the aim of the study is to prepare a multi-particulate system for colonic delivery of satranidazole for better management of intestinal amoebiasis. It is proposed to formulate satranidazole microspheres using emulsion-solvent evaporation technique with ethyl cellulose as a polymer. Since particle size plays an important role in drug release from microspheres, it was optimized using 32 full factorial design in 2 stage. Prepared microspheres were evaluated for particle size, yield, drug loading, encapsulation efficiency, cumulative percentage release in 10 hrs and 24 hrs. The best batch was selected and further evaluated. The release of drug from best batch was compared with dissolution of pure drug. These results suggest that multi-particulate system of ethyl cellulose microspheres could successfully be utilized for colon delivery of satranidazole for better management of intestinal amoebiasis.    &nbsp