RT Journal Article
T1 Solid dispersions of atorvastatin with Kolliphor RH40: enhanced supersaturation and improvement in a hyperlipidemic rat model
A1 Torrado Salmerón, Carlos Félix
A1 Guarnizo Herrero, Victor
A1 Torrado Durán, Guillermo
A1 Peña Fernández, M. Ángeles
A1 Torrado Durán, Santiago
A1 Torre Iglesias, Paloma Marina De La
AB Atorvastatin is a potent lipid-lowering drug with poor solubility and high presystemic clearance that limits its therapeutic efficacy. The aim of this study was to develop solid dispersions and micellar systems to obtain fastdissolving atorvastatin systems that enhances their anti hyperlipidemic effect. Solubility and wettability studies allow the development of solid dispersions with low proportions of croscarmellose sodium as hydrophilic carrier. Solid state characterization studies indicated that the addition of Kolliphor® RH40 surfactant to solid dispersions increases intermolecular hydrogen bonding between drug and polymer chains. Dissolution studies in biorelevant Fasted State Simulate Intestinal Fluid (FaSSIF pH 6.5) medium showed for atorvastatin solid dispersion a supersaturation peak of atorvastatin followed by an aggregation/precipitation process. Only the presence of a surfactant such as Kolliphor® RH40 in atorvastatin micellar system, promotes the presence of micelles that achieve delayed recrystallization. Efficacy studies were carried out using a hyperlipidemic model of rats fed with a high- fat diet. The atorvastatin micellar system at doses of 10 mg/kg, revealed a significant improvement in serum levels of total cholesterol, low-density lipoproteins, and triglycerides compared to atorvastatin raw material. This micellar system also exhibited more beneficial effects on liver steatosis, inflammation and ballooning injury.
PB Elsevier
SN 0378-5173
YR 2023
FD 2023-01-25
LK https://hdl.handle.net/20.500.14352/72833
UL https://hdl.handle.net/20.500.14352/72833
LA eng
NO Torrado Salmerón, C., Guarnizo Herrero, V., Torrado Durán, G. et al. «Solid Dispersions of Atorvastatin with Kolliphor RH40: Enhanced Supersaturation and Improvement in a Hyperlipidemic Rat Model». International Journal of Pharmaceutics, vol. 631, enero de 2023, p. 122520. DOI.org (Crossref), https://doi.org/10.1016/j.ijpharm.2022.122520.
NO Ministerio de Ciencia, Innovación y Universidades (España)
NO Universidad Complutense de Madrid
DS Docta Complutense
RD 15 jun 2026