Design and Evaluation of Entecavir Sustained Release Microspheres

B. Venkateswara Reddy*, G. Shankar, K. Navaneetha
Department of Industrial Pharmacy, St.Paul’s College of Pharmacy, Hayathnagar, Hyderabad, R.R.Dist-501510, India

A B S T R A C T
The present research work is aimed to design oral twice a daily sustained release microspheres of Entecavir, used for the treating or preventing Hepatitis B which can release the drug for 10 to 12 hours. The microspheres were prepared by the Quasi emulsion solvent diffusion method using varying concentrations of sustained release polymers Eudragit S 100, Eudragit RS 100 and Eudragit RLPO. The compatibility of the polymers was ruled out by FT-IR studies and found to be compatible. Total nine formulations were prepared. The Entecavir were evaluated for their micromeritic properties and found to have good flow property. The prepared microspheres were evaluated for particle size analysis, determination of drug entrapments efficiency, percentage yield and in vitro drug release. The dissolution medium used was pH 7.4 phosphate buffer. All formulations showed acceptable pharmaco-technical properties and complied with in-house specifications for tested parameters. The results of dissolution studies indicated all formulations released up to 12hours and F7 was the most successful formulation with 99.43 % drug release at the end of 12 hours.
Keywords: Quasi emulsion solvent diffusion method, Entecavir, Sustained release, Microspheres.