DESIGN AND CHARACTERIZATION OF NATURAL POLYMERIC MICROSPHERES LOADED RANOLAZINE HYDROCHLORIDE

Abstract

The aim of the study was formulation and characterization of polymeric Ranolazine hydrochloride loaded microspheres (IH-MS) in a sustained manner, to inhibit the If pacemaker current. The drug selectively targets the heart rate and to beta-blockers, that does not reduce myocardial contractility. The drug with different concentration ratio of natural polymers Gelatin, Ethyl cellulose and Methocel K4M (1:1, 1:2, 1:3, 1:4 and 1:5) were used to develop microspheres by emulsion cross-linking and emulsion solvent evaporation method. These were evaluated for % production yield, %Entrapment efficiency (EE) and Arithmetic mean particle size. On the basis of the highest values of these parameters, formulations G-F4, EC-F9 and MC- F14 were in each kind of polymer. The In-vitro drug release kinetics study and morphology were performed on selected batches. It was results that % production yield was in the range of

61.5±0.84 to 78.3±0.48, %EE was 59.7±0.51 to 87.2±0.13 and mean particle size was observed

71.4±0.95 to 93.2±0.47 µm in all formulations. In comparison, the formulation EC-F9 has maximum % production yield 78.3±0.48; maximum %EE 87.2±0.13 and suitable arithmetic mean size of 82.3±0.53 µm. The % cumulative drug release rate was found maximum in EC-F9 formulation in 12 h, which was 1.52 times greater than drug alone. SEM study showed spherical

shape of microspheres. The sustained effect was shown and data were most fitted into the Korsemeyer-pappas kinetic model. The calculated n value showed anomalous transport release profile of drug from polymers. Stability studies at 30±2ºC/60%RH±5% condition as per ICH guideline suggested that prepared microspheres were most stable at refrigeration conditions. Thus, developed polymeric microspheres encapsulated IH could be chosen for different drug delivery systems in future.