DEVELOPMENT OF NOVEL LIPID BASED DRUG DELIVERY SYSTEM FOR RALOXIFENE HYDROCHLORIDE

Abstract

Lipid-based delivery systems are becoming increasingly popular as carriers of drugs due to their ability to overcome barriers to oral absorption. The objective of the present study was to prepare novel lipid-based formulation of a sparingly soluble drug, Raloxifene hydrochloride (RLX) to increase its saturation solubility and dissolution velocity for enhancing bioavailability while reducing systemic variability. Lipid-based formulations were prepared using melt solubilization technique. The liquid formulations were converted into a solid intermediate by adsorbing onto an inert carrier and blended with excipients for encapsulation. The solid state properties, surface morphology and in-vitro release characteristics of the lipid formulations were investigated and compared with commercial formulation. The characterization of lipid formulations using Differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD) and Scanning electron microscopy (SEM) indicated that the drug is completely enveloped in the lipid core. The dissolution characteristics of lipid based formulation filled in hard gelatin capsules showed faster rate of drug dissolution as compared to commercial tablet formulation (Fiona^®). The in-vitro release studies in fed state simulated intestinal fluid (FeSSIF) and fasted state simulated intestinal fluid (FaSSIF) media indicated that, the variability in fed and fasted conditions was significantly reduced with lipid based formulation. The results from this study suggest the potential use of lipid based formulation a means of improving solubility, dissolution and concomitantly the bioavailability of a sparingly soluble drug like RLX.