Formulation and evaluation of polymeric microspheres of a poorly soluble drug celecoxib

Abstract

The aim of this present work was to formulate microspheres of BCS Class II drug Celecoxib. The drug was identified by melting point study and FT-IR spectroscopy. Therapeutic success of a drug is greatly depended on its bioavailability. Majority of the recently discovered drugs shows poor solubility (BCS Class II) which decreases the bioavailability upon oral administration. Microspheres are a novel technique to circumvent this obstacle, which can increase bioavailability of drugs significantly. Polymeric microspheres with Polyvinylpyrrolidone and Eudragit L-100, prepared by Emulsion Solvent Diffusion and Evaporation technique, showed a range of drug release profile at intestinal pH 6.8. Different batches of microspheres were prepared by varying the drug-polymer ratio. Microparticulate systems like microspheres improve absorption which increases the bioavailability, ultimately leading to more efficient drug therapy. The microsphere system also provides protection to the gastric mucosa from GIT-irritant drugs thus decreasing toxic effects and sustained releases allows lower dosage frequency. Prepared microspheres were evaluated on various parameters like entrapment efficiency, %yield, particle size, scanning electron microscope analysis, and in-vitro drug release profile. Solid spherical microspheres were produced which showed good entrapment efficiency (43%-91%) and released 70-90% of the drug content in 10hrs.