OPTIMIZATION AND DEVELOPMENT OF MUCOADHESIVE MICROSPHERES OF CARBIMAZOLE FOR HYPERTHYROIDISM

Abstract

The objectives of present study is to reduce dosing frequencies and improve the patient compliance by designing and systematically evaluating mucoadhesive microspheres of Carbimazole. Frequency dosing(2 to 3 times) administration is required in conventional dosage forms of Carbimazole that problem are overcome by using mucoadhesive microspheres drug delivery system. They adhere to the mucosal surface of intestine and provide sustained release effect. Carbimazole microspheres were formulated by Ionotropic Gelation Method using polymers i.e. Sodium Alginate, Carbopol 934 and Calcium chloride. All the formulations (F1-F9) were subjected to Percentage yield, Entrapment efficiency, Particle size analysis, Micromeritics properties, Swelling index, Muco-adhesion test, In-vitro drug release studies and Scanning electron microscopy. FTIR data indicates that there was no drug interaction between drug and polymers used. Scanning electron microscopy indicated that microspheres were spherical in shape and drug remained dispersed in polymer matrix. Among all formulations, the formulation F1 displayed better result whose Percentage yield (91%), Entrapment efficiency (74.18%), Swelling index (90%) and In-vitro drug release was found to be 73.95% after 7 hours. The formulation F1 is following zero-order kinetics. Based on all the above evaluation parameters it was concluded that the formulation F1 was found to be the best formulation among all the formulations and can be used in the treatment of Hyperthyroidism.