Use of Black Gram Polysaccharide Mucilage as Release Retardant in the Development of Sustained Release Matrix Pellets of Ciprofloxacin Hydrochloride

Abstract:

Ciprofloxacin HCl is a BCS class III drug with high solubility and low permeability. It is a second generation fluoroquinolone antibiotic used in the treatment of mild to moderate urinary and respiratory tract infections. It has half-life of 4-5 h and bioavailability about 70%. The main objective of this research work was to develop sustained release matrix pellets of ciprofloxacin HCl to obtained better delivery of ciprofloxacin HCl to the stomach and the proximal parts of the small intestine by increasing the mean residence time (MRT) in the stomach using novel natural excipient that is black gram polysaccharide as release retarding polymer. The pellets were prepared by an extruder spheronizer. The characterization of pellets was done using X-ray powder diffraction (XRPD), Scanning electron microscopy (SEM), flow properties, percent friability, drug content, percent production yield, swelling ability of pellets, mucoadhesive strength, and in-vitro drug release and stability studies. The optimized pellets were found to be free flowing and had yield 30.4% and drug content 97.79±0.60%. The optimized formulation NF1 showed sustained drug release of 96.08% up to 12 h. The optimized formulation (NF1) showed good flow properties which were within the official limits. The optimized formulation showed percent mucoadhesion of 72% in 0.1N HCL (pH 1.2). It can be concluded that black gram polysaccharide mucilage can be effectively used as release retarding excipient in sustained release formulations.

Key words: Sustained release drug delivery system, Ethyl cellulose, Black gram polysaccharide, Pelletization, in vitro drug release study.