Abstract The present invention discloses the formulation of a nanoparticulate drug delivery system composed of at least one statin (preferably simvastatin) loaded in hydrophilic natural polymer (chitosan nanoparticles) in which both exerts synergistic action on each other. The formed biocompatible formulation is in nanosize with a positive surface charge, and released the drug in a sustained manner. This formulation provides alterations in physicochemical properties of drug not limited to solubility and also in properties of polymer not limited to molecular weight. These altered physicochemical properties can render modified biological properties like decrease in lipid level, increase in bioavailability (due to increased solubility and reduced PG efflux mechanism), and minimized muscle toxicity with reduced dose level.