FORMULATION AND CHARACTERIZATION OF MUCOADHESIVE MICROSPHERES OF ATORVASTATIN CALCIUM

ABSTRACT

Oral bioavailability of atorvastatin calcium (ATC) is very low (only 14%) due to instability and incomplete intestinal absorption or extensive gut wall extraction. Atorvastatin belongs to BCS class II. Atorvastatin, as a synthetic lipid-lowering agent (for hypercholesterolemia). The Mucoadheive microsphere of Atorvastatin calcium (ATC) were developed to expand the gastric residence time of the drug, as ATC has maximum rate of absorption in the upper GI tract. Mucoadhesive microspheres were prepared by emulsification technique followed by cross-linking in mucoadhsive polymers carbopol 934P and sodium alginate used. The microspheres were assessed for percentage yield, average particle size, zeta potential, micromeritic properties, swelling properties, FTIR spectroscopy of microspheres, percentage drug entrapment, mucoadhesion testing by in-vitro wash-off test, in-vitro drug release, drug release kinetic & pharmacokinetic studies. Pharmacokinetic study performed on albino rabbits illustrated that the bioavailability of atorvastatin microspheres significantly increased. This research indicated that mucoadhesive microspheres for delivery of ATC can improve its bioavailability.

Keywords: atorvastatin calcium, bio-availability, mucoadhesive microspheres, crosslinking,emulsificat ion.