Studies on rosuvastatin calcium incorporated chitosan salt nanoparticles

Abstract

Cardiovascular diseases are the leading causes of death worldwide and rosuvastatin calcium (RCa) is one of the most effective drugs used for the prevention of coronary heart diseases. Considering low aqueous solubility oral bioavailability of RCa was hardly reached to almost 20%. Therefore there is still a demand for novel drug delivery systems with outstanding drug absorption, distribution, and elimination rates as well as less side effects. In this study RCa was incorporated into chitosan acetate (CA), chitosan lactate (CL), chitosan aspartate (CAs) and chitosan glutamate (CG) nanoparticles (NPs) for the enhancement of its preferential use. Spray drying method was used for the formation of the RCa incorporated NPs. Physicochemical characteristic properties were evaluated in detail and analyses results demonstrated that particle sizes were ranged between 240.0 ± 10.7-446.9 ± 13.1 nm with homogenous size distributions (with PDI data range of 0.490 ± 0.032 to 0.790 ± 0.090) while the zeta potentials mostly valued in the cationic scale. Entrapment efficiencies (EE) of RCa-CA-NPs and RCa-CL-NPs were the highest with 80.8 ± 3.1% and 99.1 ± 1.9%, respectively. In vitro release study results demonstrated initial burst releases for the RCa-CA-NPs and RCa-CL-NPs with almost 58% just within 5 min while the release rate of pure RCa was reached up to 53% in phosphate buffer solution (pH 6.8) only after 1 h. As a result of the study enhanced in vitro release rates were achieved from RCa incorpotared NPs showing that the chitosan (Cs) originated NPs have the potentials as novel drug delivery systems for RCa