Evaluation of the Cholesterol-Lowering Effect of Atorvastatin Loaded in Lipid Nanodispersions Based on Natural Materials

Abstract

This study developed and evaluated nanostructured lipid carriers (NLC) made from natural materials loaded with atorvastatin (ATV) to improve its therapeutic effect. ATV is widely used as an antihyperlipidemic drug to lower cholesterol and triglycerides, which are key risk factors for cardiovascular diseases. However, as per the Biopharmaceutical Classification System, ATV belongs to Class II, with low aqueous solubility and extensive hepatic metabolism, which limits its bioavailability and hinder clinical effectiveness. Methods The NLCs were formulated using high-speed homogenization emulsification. The formulation incorporated natural oils such as safflower, sunflower, rice, avocado, and wheat germ oil, recognized for their cholesterol-lowering properties. Lipid matrices included Precirol ® ATO 5 and Gelucire ® 50/13, which also functioning as a surfactant due to its amphiphilic properties. Pluronic ® F-68 was also employed as a surfactant. The formulation was evaluated based on parameters such as lipid and surfactant composition, particle size, polydispersity index (PDI), entrapment efficiency, and drug release profile. Results The NLCs had particle sizes ranging from 163.3 ± 5.8 nm to 235.4 ± 6.2 nm with PDI values between 0.311 ± 0.023 and 0.396 ± 0.031. Entrapment efficiency reached up to 95.31 ± 4.32%. In-vivo studies demonstrated superior therapeutic efficacy of NLCs, reducing cholesterol levels by 14–37%, outperforming atorvastatin suspension. Conclusions The resulting formulations exhibited particle sizes ranging from 163 to 236 nm, with encapsulation efficiencies exceeding 90%. In-vivo studies demonstrated that these lipid nanocarriers significantly enhanced the cholesterol-lowering effect of atorvastatin compared to its conventional suspension form, achieving reductions in cholesterol levels ranging from 14% to 37%. Graphical Abstract

Bibliographic Information