FORMULATION DESIGN AND EVALUATION OF SAXAGLIPTIN SUSTAINED RELEASE MICROSPHERES

Sustained release oral product namely microspheres for Saxagliptin prepared by Ionotropic gelation technique to overcome the drug-related adverse effects like gastric irritation, improve its bioavailability in different gastrointestinal pH conditions. Total nine formulation batches (F1-F6) were formulated using sodium alginate as drug release modifiers in various proportions and investigate for physicochemical properties and drug release potential. All investigated properties showed satisfactory results. While increase in the concentration of sodium alginate dispersions increased sphericity, size distribution, flow properties and mean diameter of the Microspheres. The drug entrapment efficiency obtained in the range 78.4% to 95.42%. Increase in the concentration of calcium chloride was significantly affects the mean diameter but no appreciable change in morphology and drug release behavior. In-vitro study proves that drug release slowly increases as the pH of the medium is increased. The drug release in batch F1, F2, F3 F4, F5 and F6 containing sodium alginate. The mechanism drug release from Microspheres was found to be following Higuchi model graph. From the study it was concluded that controlled release Saxagliptin Microspheres can be developed successfully by using ionotropic gelation technique. Key words: Microencapsulation; Ionotropic gelation, Microspheres, Sodium alginate, pH dependent