In vitro toxicity evaluation of lomefloxacin-loaded MCM-41 mesoporous silica nanoparticles. (4th May 2021)

• Record Type: Journal Article
• Authors: Tzankova, Virginia; Aluani, Denitsa; Yordanov, Yordan; Valoti, Massimo; Frosini, Maria; Spassova, Ivanka; Kovacheva, Daniela; Tzankov, Borislav
• Is Part Of: Drug and chemical toxicology. Volume 44:Number 3(2021)
• Page Start: 238
• Page End: 249
• Publication Date: 2021-05-04
• Subjects: Mesoporous silica MCM-41 -- lomefloxacin -- oxidative stress -- drug safety -- cytotoxicity -- in vitro; Toxicology -- Periodicals; Drugs -- Toxicology -- Periodicals; Toxicology, Experimental -- Periodicals; 615.9005
• DOI: 10.1080/01480545.2019.1571503
• Languages: English
• ISSNs: 0148-0545

Abstract

Abstract: Lomefloxacin (LF) is interesting as a model molecule from a safety point of view because of its high potential for serious adverse drug effects (i.e. phototoxic reactions). In this study, MCM-41 mesoporous silica nanoparticles (MCM-41) were loaded with lomefloxacin, aiming to overcome the drug's intrinsic cytotoxicity. The good biocompatibility of the empty drug carrier (0.1–1.0 mg/ml) was established by the absence of red blood cell lysis (hemolysis assay). The cytotoxicity of empty MCM-41 and lomefloxacin-loaded MCM-41 (LF-MCM-41) was evaluated by using a battery of in vitro cytotoxicity assays: Alamar blue, lactate dehydrogenase release and reactive oxygen species formation by dichlorofluorescein assay. Three cell cultures models: hepatoma HepG2, fibroblasts L929 and endothelial EA.hy926 cells were used to compare the cytotoxicity and reactive oxygen species formation by free drug, empty MCM-41, and LF-MCM-41. The findings from the study indicated that empty MCM-41 (0.1–1.0 mg/ml) showed a low cytotoxic potential in HepG2, followed by L929 and EA.hy926 cells. Lomefloxacin loading in MCM-41 mesoporous silica nanocarrier reduced the cytotoxicity of the free lomefloxacin, especially in the high concentration (1.0 mg/ml MCM-41, containing 120 µg/ml LF). L929 and EA.hy926 cells were more sensitive to the protective effects of LF-MCM-41, compared to HepG2 cells. The results indicate that an improvement in lomefloxacin safety might be expected after incorporation in an appropriate drug delivery system.