FORMULATION DEVELOPMENT OF MUCOADHESIVE MICROSPHERES OF ANTIDIABETIC DRUG
Talat Farheen*, Azmat Shaikh and Dr. Sadhana Shahi
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 saxagliptin, 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, Saxagliptin has been successfully
achieved.
Keywords: Orifice ionotropic gellation, Sodium alginate, CaCl2, HPMC K4M.
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