Enhancing solubility and therapeutic potential of rosuvastatin via β-cyclodextrin inclusion complex-loaded chitosan nanoparticles

Rosuvastatin is a BCS class II drug effective in the management of atherosclerosis. To enhance solubility and efficacy, Rosuvastatin-β-Cyclodextrin complex-loaded chitosan nanoparticles (R-CD-CNs) were developed. β-cyclodextrin was crosslinked with Citric acid to impart stability to the inclusion complex. Rosuvastatin was incorporated into lyophilized crosslinked β-cyclodextrin by kneading method. R-CD complex was loaded into chitosan-tripolyphosphate nanoparticles. The R-CD-CNs were optimized by 32 full factorial design with independent variables Chitosan, Sodium Tripolyphosphate as crosslinking agent and their effects were checked on dependent variables. Optimized R-CD-CNs showed Particle size 265 ± 17 nm, PDI 0.251 ± 0.02, EE 80 ± 7.5%, and Zeta potential +19.8 ± 3.8 mV. The results of DSC confirmed that drug gets incorporated into chitosan nanoparticles. XRD confirmed amorphous form of drug into chitosan nanoparticles. SEM study confirmed the sphericity of R-CD-CNs. The in vitro release profile was found to be 91 ± 2.5% at the end of 10 h, indicating sustained release characteristics. R-CD-CNs showed a more prominent effect compared to plain Rosuvastatin calcium and the disease control group. The synergistic effect of chitosan was confirmed by the in vivo antihyperlipidemic study. The results of stability study reveal good stability of R-CD-CNs. R-CD-CNs were developed successfully and will be helpful for the effective management of hyperlipidemia.