The aim of this study was to develop controlled release mucoadhesive microspheres of clarithromycin for the treatment of peptic ulcer disease caused by Helicobacter pylori (H. pylori). Clarithromycin mucoadhesive microspheres were prepared by using carbopol 974P and Hydroxypropyl methyl cellulose K4M (HPMC K4M) and Eudragit RS 100. The prepared microspheres were subjected to evaluation for percentage yield, particle size, incorporation efficiency, in vitro mucoadhesion and in vitro drug release characteristics. Absence of drug-polymer interaction was confirmed by using differential scanning calorimetry analysis and fourier transform infrared spectrophotometry. X- Ray diffraction study was conducted to analyze physical nature of entrapped drug. The stability of the clarithromycin in 0.1N HCl was determined to correct the dissolution data and also the stability of entrapped clarithromycin was analyzed in 0.1N HCl. The prepared microspheres showed a strong mucoadhesive property. The polymer concentration influenced the in vitro drug release significantly in 0.1N HCl. The particle sizes of microspheres ranged between 118.5±6.51 μm to 493.23±11.23 μm. The percentage drug entrapment and percentage yield of formulations were about 52.62±0.72 to 87.97±0.83% and 37.53±1.43 to 89.33±1.46% respectively. In vitro release was conducted in 0.1N HCl using high-performance liquid chromatography. The results further substantiated that mucoadhesive microspheres of clarithromycin improved the gastric stability of clarithromycin (due to entrapment within the microsphere). The formulation FC6 selected as best formulation based on release profile, mucoadhesiveness and mucous turnover rate. From the above results, it was concluded that the mucoadhesive microspheres of clarithromycin has feasibility for eradicating H. pylori from the stomach more effectively because of the prolonged gastrointestinal residence time and controlled release of drug from the of the formulation.
