Abstract

SYNTHESIS, CHARACTERIZATION AND OPTIMIZATION OF COLON TARGETING CIPROFLOXACIN LOADED MICROSPHERES

Rohit* and Neha

.

Abstract

Our objective in this research is to develop an enteric-coated capsule device filled with microencapsulated drug formulation by the crosslinking of microbially degradable matrix loaded with Ciprofloxacin to investigate its release behaviour. Because the gelatin capsule was enteric coated with Eudragit L-100, it prevented the disintegration of the capsule in the gastric fluid of pH 1.2 (acidic) and thereby, released the drug in a controlled manner on reaching the small intestine at basic pH 7.4, the capsule lost its enteric coating, microspheres swelled slowly, and started to release Ciprofloxacin in the colonic region. The prepared microspheres were evaluated for Micromeritic properties, Particle size, Solubility studies, Entrapment efficiency, Drug polymer compatibility (IR and DSC study), Swelling Index, Scanning Electron Microscopy and In vitro drug release. The microspheres produced exhibited good encapsulation efficiencies and micromeritic properties. Encapsulation efficiency of microsphere is around 89%. The mean diameters of microspheres were found in required micrometer range. The results of optimized formulations showed a narrow size distribution and smooth surface. The DSC and the FTIR analysis showed the absence of any potent incompatibility between the drug and the polymer. In-vitro release showed 86.3% drug release after 12 hours. Results of present study suggest that Ciprofloxacin loaded microspheres for colon targeting can be successfully prepared by Ionotropic gelation method.

Keywords: Ciprofloxacin, Microencapsulation, Colon targeting, Entrapment efficiency, Particle size, In vitro release stability studies.