In vitro Evaluation of Floating Microspheres of Gabapentin by Solvent Evaporation Method

Abstract

The present study involves the design and characterization of floating microspheres with gabapentin as model drug for prolongation of tonic clonic jerk time, microsphere of gabapentin, was developed to reduce the frequency of drug administration, ease of dose adjustment and improve patient compliance. In this study, the shape and surface morphology of microspheres were characterized by scanning electron microscopy. In vitro drug release studies were performed and drug release kinetics was evaluated using the linear regression method. Effects of polymer concentration, solvent composition, particle size, drug entrapment efficiency and drug release were also studied. The synthesized microspheres exhibited prolonged drug release (> 10 h) and remained buoyant for > 24 h. The drug entrapment efficiency was in the range 50-70 %. At higher polymer concentration, the average particle size was increased and the drug release rate decreased. In vitro studies revealed diffusion-controlled drug release from the microspheres. Among all the formulations (F1-F6), F3 is the optimized formulation of gabapentin was prepared by solvent evaporation techniques using Ethyl cellulose as polymer and particle size, microsphere efficiencies and in vitro release of the fabricated microsphere were evaluated. Particle sizes of the microspheres were influenced by the concentration of Ethyl cellulose and stirring speed. From the results of the in vitro study shows that the desired release rate is achieved by ethyl cellulose. The object of this study was to develop and evaluate stable microspheres of gabapentin drug an antiepileptic drug using combination of Eudragit and ethyl cellulose as polymer which delivers the drug at a controlled rate for a prolonged period of time. Ethyl cellulose used in this study and it is showing hard binding of microspheres.