Formulation and evaluation of rosuvastatin calcium loaded solid nanodispersions to improve its solubility

Rosuvastatin calcium, a third-generation statin, and its a strong LDL-C lowering ability and excellent binding interactions with HMG-CoA reductase, making it a better first-line therapy for hypercholesterolemia. However, rosuvastatin calcium has limited oral bioavailability due to its first-pass metabolism and poor water solubility. This study aimed to develop rosuvastatin calcium-loaded solid nanodispersion (RcNDs) to improve its solubility to effectively treat HMG-CoA reductase inhibition.

RcNDs were prepared by the solvent evaporation technique using polyvinylpyrrolidine K30 and poloxamer 407 in different ratios (RcNDs-1 to RcNDs-4) and evaluated their in vitro behaviors and characterized.

The developed RcNDs-4 demonstrated improved results in terms of average particle size, zeta potential, drug content, and entrapment efficiency, with respective values of 193.27±6.35nm, -8.72±0.23mV, 9.14±0.18mg, and 90.894±3.50%. Additionally, the amount of rosuvastatin calcium in RcNDs-4 was determined by the HPLC (high-performance liquid chromatography) method to be 9.14±0.18, which agreed with the results of the ultraviolet-visible (UV-visible) spectrophotometer. In comparison to other formulations and pure Rc, RcNDs-4 exhibits the highest release profile at 93.49±1.52%. The morphological and thermal evaluation showed a broad endothermic peak, which suggested drug embedding in the RcNDs, and amorphous particles that did not aggregate, which improved solubility.

According to the study, the formulation of nanodispersions may improve the solubility and lessen the side effects associated with oral administration of BCS class II drugs that are poorly aqueously soluble.