FABRICATION AND CHARACTERIZATION OF LERCANIDIPINE HYDROCHLORIDE LOADED HOLLOW MICROSPHERES

Abstract

The goal of this research is to treatment of hypertension by developing hollow microspheres that are loaded with Lercanidipine hydrochloride. The purpose of developing hollow microspheres loaded with Lercanidipine hydrochloride is to extend the drug's gastrointestinal retention time over currently available sustained release solutions, hence reducing the frequency of dose and improving bioavailability. The following polymers were used: cellulose acetate, Eudragit RS 100, polyethylene oxide, Hydroxypropyl cellulose K15M, ethyl cellulose, and Eudragit RL100. These microspheres were manufactured using solvents such as dichloromethane and ethanol. Hollow microspheres that contain Lercanidipine hydrochloride were produced by modifying quasi-emulsion diffusion techniques. Preformulation tests for hollow microspheres loaded with Lercanidipine hydrochloride showed that all formulations have acceptable flow characteristics. SEM analysis investigated that the surface of hollow microspheres was found to be slightly porous, smooth, and spherical in shape. FTIR spectra studies confirmed that there is compatibility between the drug and excipients. By using buoyancy tests and the maximum   amount of drug released within 12 hours, the formulation design was optimised. In vitro tests shown that Lercanidipine hydrochloride hollow microspheres composed of Eudragit RL 100 and Eudragit RS 100 at a ratio of 1:2 (F7) exhibited the most efficient sustained release of drug. Therefore, there is potential for a novel treatment of hypertension with the optimised formulation (F7) of hollow microspheres containing Lercanidipine hydrochloride.