FORMULATION AND EVALUATION OF VILDAGLIPTIN MICROPHERES

Junaid Ahmed Khan*, A. Siva Kumar, Avinash Dundigalla and A. Yasodha

ABSTRACT

Microspheres were found to be more efficient for controlled drug delivery systems, further the mucoadhesion provides feature of targeted drug delivery to the dosage form. Mucoadhesion ensures increased contact time of the dosage form with the absorption site while microspheres sustained the release of drug from the dosage form at the site of absorption and result into improved bioavailability of drug. The objective of the present research is to formulate mucoadhesive microspheres of vildagliptin, to achieve reduced dosing frequency, increased bioavailability, increased patient compliance and decreased drug related adverse effects. This objective is achieved by formulating the mucoadhesive microspheres of the drug using orifice ionotropic gelation technique. Sodium alginate is used as a polymer while calcium chloride as counterion and HPMC K4M as mucoadhesive polymer. The formulation batches were prepared by 32 factorial design and evaluated for particle size, flow properties, mucoadhesion, microencapsulation efficiency, drug release and stability. The formulation SF6 showed nearly spherical microcapsules, good flowability, microencapsulation efficiency, mucoadhesion, stability and extended drug release upto 12 hours. An approach to develop a stable mucoadhesive microspheres of oral hypoglycemic drug, Vildagliptin has been successfully achieved.

Keywords: Orifice ionotropic gellation, Sodium alginate, CaCl2, HPMC K4M