Enhancing exemestane delivery: Solid lipid nanoparticles formulation and pharmacokinetic evaluation

Abstract

This research investigates the development of exemestane (EXM) solid lipid nanoparticles (SLNs) for the purpose of improving drug delivery. To prepare EXM SLNs, glycerol monostearate was used as the lipid and Tween 80 as the surfactant and solvent injection followed by high-pressure homogenization as a method of preparation. The formulation parameters were optimized, leading to the development of a promising formula. The formula has a particle size of 188.72 ± 5.62 nm, a polydispersity index (PDI) of 0.215 ± 0.023, and an %EE of 65.39 ± 2.54 %. The formulation's robustness was indicated by minimal changes in particle size and %EE over 30 days, as revealed by stability studies. The bioavailability of EXM SLNs was found to be significantly improved in Wistar rats compared to conventional EXM suspension, as shown by pharmacokinetic studies. The formula that was optimized showed a higher maximum plasma concentration (Cmax) of 168.92 ± 2.40 ng/mL, a delayed time to reach Cmax (Tmax) of 4 hours, and significantly higher area under the curve (AUC) values. These results highlight the effectiveness of the optimized formula in improving drug absorption and bioavailability. The findings indicate that EXM SLNs show potential for enhancing the delivery and effectiveness of EXM, specifically in the treatment of breast cancer.