Atorvastatin calcium

Xia J, et al. International Immunopharmacology, 2023, 121, 110465.

In this study, Atorvastatin calcium (Ator) was evaluated for its capacity to alleviate intestinal damage induced by 5-fluorouracil (5-Fu) and enhance antitumor activity in colorectal cancer (CRC) models. Human intestinal epithelial cells (HIECs) and BALB/c mice were exposed to 5-Fu to induce oxidative stress and cellular senescence, monitored via SA-β-Gal staining, p16/p53/p21 expression, and SASP markers (IL-1β, IL-6, TNF-α). Ator treatment reversed these senescence indicators in vitro and in vivo. HCT116 cells were subjected to combination therapy with Ator and 5-Fu, showing significantly reduced cell viability. In CRC xenograft nude mice, co-administration of Ator and 5-Fu synergistically inhibited tumor growth, demonstrating Ator's experimental application as both a protective agent against drug-induced intestinal injury and as a chemosensitizer enhancing 5-Fu efficacy.

Lestari PM, et al. Journal of Pharmaceutical Sciences, 2025, 114(4), 103695.

In this study, atorvastatin calcium was formulated into transethosomes to develop a transdermal patch with enhanced systemic delivery. Six formulations were prepared and characterized for particle size (≤130.59 nm), polydispersity index (≤0.24), zeta potential (≥-51.87 mV), and deformability index. The optimal formulation exhibited a particle size of 114.62 ± 0.92 nm and a deformability index of 15.41 ± 1.56, with spherical vesicle morphology confirmed via microscopy. Transethosome patches were evaluated for pH, viscosity, and in vitro skin penetration, revealing a flux of 72.19 ± 1.53 µg/cm²/h. Pharmacokinetic studies demonstrated a 3.67-fold increase in bioavailability compared to oral suspension. Skin irritation assays confirmed the patch's safety. These results underscore the experimental application of transethosome-based patches as an effective strategy for enhancing atorvastatin calcium delivery.

Gaber DM, et al. International Journal of Pharmaceutics: X, 2024, 7, 100249.

Atorvastatin calcium (ATR Ca) was repurposed for antiproliferative activity against breast cancer using gelucire-based solid lipid nanoparticles (SLNs) with lactoferrin (Lf) as a targeting ligand. ATR Ca-SLNs, both Lf-decorated and undecorated, were prepared by melting lipids at 80 °C, dissolving ATR Ca in the molten lipid phase, and emulsifying with Milli-Q water at the same temperature. For in vitro cellular uptake studies, fluorescently labeled SLNs substituted ATR Ca with coumarin 6 (0.001% w/v) to enable confocal laser scanning microscopy visualization. The formulations were systematically characterized for particle size, encapsulation efficiency, and targeting efficacy, demonstrating enhanced tumor-specific delivery of ATR Ca. This method highlights a precise experimental approach to improve anticancer drug delivery using lipid-based nanocarriers with ligand-mediated targeting.