FORMULATION DEVELOPMENT OF SUSTAINED RELEASE MUCOADHESIVE MICROSPHERES OF ANTIBIOTIC

Dr. Talat Farheen*, P. Srikanth, Suddala Anusha, Dwivedi Kanchan and Dr. Nijhawan Monika

ABSTRACT

The present investigation concerns the development of a new oral drug delivery system utilizing the concepts of controlled release and mucoadhesion, which would remain in stomach and extend the drug release for longer period of time. Levofloxacin is used to treat a variety of bacterial infections. It belongs to a class of drugs known as quinolone antibiotics. It works by stopping the growth of bacteria. Levofloxacin mucoadhesive microspheres were prepared by solvent evaporation technique using carbopol 934P and hydroxypropyl methyl cellulose K4M (HPMC K4M). The prepared microspheres were subjected to evaluation of particle size, entrapment efficiency, drug content, in vitro wash off test and in vitro drug release studies. Absence of drug-polymers interaction was confirmed by fourier transform infrared spectrophotometry. The particle sizes of batches ranged between 304.5 μm to 456.6 μm. The drug entrapment of formulations was about 70 to 88.3%. The prepared microspheres showed a strong mucoadhesive property i.e., 79.3% to 91.1%. The polymer concentration influenced the in vitro drug release significantly in 0.1N HCl which suggested sustained drug release from formulations and was found to be in the range of 78.9 to 87.4%. The prepared factorial batches have shown a nearly spherical shape with rough surface. F7 factorial batch was selected as optimized batch because it has shown maximum mucoadhesion and sustained the release of drug from formulation up to 8 hours. Regression analysis revealed that the drug release from the optimized batch followed zero order kinetics. From the above results, it was concluded that the mucoadhesive microspheres of levofloxacin has feasibility for eradicating Helicobacter pylori from the stomach more effectively because of the prolonged gastrointestinal residence time and controlled release of drug from the formulation.

Keywords: Levofloxacin, carbopol 934P, hydroxypropyl methyl cellulose K4M, Helicobacter pylori, mucoadhesion.