The Hypolipidemic Effect of Liposomal Atorvastatin in Wistar Albino Rats with Dyslipidemia
Keywords:
Dyslipidemia , Statins, Atorvastatin, Quercetin, HMG-CoA reductase, lipid profileAbstract
Background: Atorvastatin is the cornerstone of hyperlipidemia therapy. It lowers lipids and shows cardioprotective effects. However, challenges like low bioavailability and side effects exist. Liposomal technology presents a solution by encapsulating the drug, enhancing its effectiveness, and decreasing side effects by providing more efficient delivery to the liver. The synergistic action of quercetin additionally improves this outcome.
Objective: The current study aimed to evaluate the hypolipidemic effect of liposomal atorvastatin (LA) compared to free atorvastatin in albino Wistar rats with hypercholesterolemia.
Patients and Methods: Liposomal atorvastatin was prepared using a modified thin-film hydration method. The hypolipidemic effect of LA was evaluated using adult, healthy male
Wistar albino rats, which were randomly divided into a negative control group (C-) and a high-cholesterol diet group containing 27 animals. The high-cholesterol diet was administered for four weeks to induce hypercholesterolemia. Following this induction period, the 27 hypercholesterolemic rats were further categorized into three groups for the treatment: Positive Control Group (C+), including hypercholesterolemic rats; Atorvastatin Group, which orally administered 20 mg/kg/day of atorvastatin for 4 weeks; and LA Group, which orally administered 10 mg/kg/day of LA for 4 weeks. The serum concentration of total cholesterol (TC), triglycerides (TG), low-density lipoprotein cholesterol (LDL-C), high-density lipoprotein cholesterol (HDL-C), very low-density lipoprotein (VLDL) and HMG-CoA reductase was determined in the current study.
Results: The study results indicate that the morphological shape of LA was A large unilamellar vesicle, a single-layered vesicle composed of a single lipid bilayer enclosing a single aqueous core. The average size was 13.78±2.38 µm, and the zeta potential reached approximately -74.45 mV. Furthermore, the results showed that TC, TG, LDL-C, HDL-C, VLDL, and HMG-CoA reductase enzyme levels were significantly elevated in the C+ group. These levels then significantly decreased after treatment with both atorvastatin and LA.
Conclusion: Our study concludes that the liposomal co-formulation of atorvastatin and quercetin is a stable and highly effective therapeutic strategy for hyperlipidemia. This novel delivery system enhances drug bioavailability and targets the liver, significantly reducing serum lipids and HMG-CoA reductase activity in dyslipidemic rats.
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