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Open AccessArticle

Self-Micellizing Technology Improves the Properties of Ezetimibe and Increases Its Effect on Hyperlipidemic Rats

1
Department of Pharmaceutics and Food Technology, Faculty of Pharmacy, Complutense University, Plaza Ramón y Cajal s/n, Madrid 28040, Spain
2
Department of Biomedical Sciences, Faculty of Pharmacy, University of Alcalá de Henares, Ctra Madrid-Barcelona Km 33,600 28805 Madrid, Spain
3
Instituto Universitario de Farmacia Industrial, Complutense University, Plaza Ramón y Cajal s/n, Madrid 28040, Spain
*
Author to whom correspondence should be addressed.
Pharmaceutics 2019, 11(12), 647; https://doi.org/10.3390/pharmaceutics11120647
Received: 22 October 2019 / Revised: 22 November 2019 / Accepted: 29 November 2019 / Published: 3 December 2019
(This article belongs to the Special Issue Surfactant-Based Drug Delivery)
The aim of this work was to develop ezetimibe self-micellizing solid dispersions using Kolliphor® RH40 (MS-K) as a surfactant incorporating ezetimibe (EZ) into the croscarmellose hydrophilic carrier. Different ezetimibe:Kolliphor® ratios were studied to select micellar systems that improve the dissolution properties of ezetimibe. The different formulations were characterized by means of solid state analysis by SEM, powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), and dissolution studies. These physicochemical studies showed a decrease from the crystalline structure of ezetimibe (EZ) to its amorphous state in the micellar systems (MS-K). A rapid dissolution profile was observed in these micellar systems compared to the drug raw material and physical mixture. Efficacy studies were conducted using a high-fat diet that induced hyperlipidemic rats. The micellar system selected (MS-K 1:0.75) revealed a significant improvement in serum levels of total cholesterol (TC), low-density lipoproteins (LDL), and triglycerides (TG) compared to ezetimibe raw material. The histopathological examination of liver tissue also showed that this micellar system exhibited more beneficial effects on liver steatosis compared to ezetimibe raw material (EZ-RM) and the high-fat diet group (HFD). This study suggests that EZ micellar systems using Kolliphor® RH40 could enhance the antihyperlipidemic effect of ezetimibe and reduce liver steatosis.
Keywords: Ezetimibe; solid dispersion; micellar systems; antihyperlipidemic activity; liver steatosis Ezetimibe; solid dispersion; micellar systems; antihyperlipidemic activity; liver steatosis
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MDPI and ACS Style

Torrado-Salmerón, C.; Guarnizo-Herrero, V.; Cerezo-Garreta, J.; Torrado Durán, G.; Torrado-Santiago, S. Self-Micellizing Technology Improves the Properties of Ezetimibe and Increases Its Effect on Hyperlipidemic Rats. Pharmaceutics 2019, 11, 647.

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