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Lipid Nanostructures Containing Atorvastatin Decrease Lipopolysaccharide-Induced Inflammation in Macrophages

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Atorvastatin, an inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase, is known to exert lipid-lowering, but also anti-inflammatory effects in extra-arterial locations. In order to avoid its toxicity associated with long-term oral treatment, in this study we have proposed novel lipid nanostructures containing atorvastatin to improve its efficiency and bioavailability after local application in periodontitis inflammation therapy. The physico-chemical characterization of the nanostructures was performed using dynamic light scattering technique and morphological observations were made by light microscopy. The encapsulation efficiency was determined by high performance liquid chromatography analysis of loaded atorvastatin. In vitro cytotoxicity and anti-inflammatory activity were evaluated in human premonocytic THP-1 cell line and a model of lipopolysaccharide-induced inflammation in macrophages, respectively. The results showed that the population of atorvastatin lipid nanostructures presented a mean diameter of 178 nm and a good homogeneity after sonication and extrusion treatments applying, as indicated by the low polydispersity index of 0.223. The efficiency of atorvastatin encapsulation was high (87.3%) and the nanostructures cytotoxicity was reduced for lipid concentrations ranging from 50 μM to 500 μM. Experiments in THP-1 cells differentiated to macrophages demonstrated that atorvastatin liposomal formulation led to a higher inhibition of lipopolysaccharide-induced proinflammatory cytokines (interleukin 6, tumor necrosis factor alpha and interleukin 8) release, compared to free drug. In conclusion, atorvastatin lipid nanostructures could be used to develop an efficient local treatment of periodontitis inflammation.

Keywords: Cytokine; Cytotoxicity; Encapsulation Efficiency; Inflammation; Liposome; Particle Size; Statin

Document Type: Research Article

Affiliations: 1: Institute of Biochemistry of the Romanian Academy, 296, Splaiul Independentei, Sector 6, 060031 Bucharest, Romania 2: National Institute of Research and Development for Biological Sciences, 296, Splaiul Independentei, Sector 6, 060031 Bucharest, Romania

Publication date: July 1, 2017

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  • Journal for Nanoscience and Nanotechnology (JNN) is an international and multidisciplinary peer-reviewed journal with a wide-ranging coverage, consolidating research activities in all areas of nanoscience and nanotechnology into a single and unique reference source. JNN is the first cross-disciplinary journal to publish original full research articles, rapid communications of important new scientific and technological findings, timely state-of-the-art reviews with author's photo and short biography, and current research news encompassing the fundamental and applied research in all disciplines of science, engineering and medicine.
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