(+)-Limonene 1,2-Epoxide-Loaded SLNs: Evaluation of Drug Release, Antioxidant Activity, and Cytotoxicity in an HaCaT Cell Line

• Autor(a) principal: Souto, Eliana B.
• Data de Publicação: 2020
• Outros Autores: Zielińska, Aleksandra, Souto, Selma B, Durazzo, Alessandra, Lucarini, Massimo, Santini, Antonello, Atanasov, Atanas G., Marques, Conrado, Andrade, Luciana N., Severino, Patrícia
• Tipo de documento: Artigo
• Idioma: eng
• Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
• Texto Completo: http://hdl.handle.net/10316/106193; https://doi.org/10.3390/ijms21041449
• topic: (+)-limonene 1; 2-epoxide; monoterpene; Imwitor 900K-SLN; lipid peroxidation; cytotoxicity; HaCaT cell line; Cell Line; Delayed-Action Preparations; Humans; Keratinocytes; Lipid Peroxidation; Nanoparticles; Antioxidants; Cyclohexane Monoterpenes; Monoglycerides; Poloxamer

In this work, we developed a solid lipid nanoparticle (SLN) formulation with (+)-limonene 1,2-epoxide and glycerol monostearate (Lim-SLNs), stabilized with Poloxamer® 188 in aqueous dispersion to modify the release profile of the loaded monoterpene derivative. We also evaluated the role of SLNs in lipid peroxidation and cytotoxicity in a spontaneously transformed aneuploid immortal keratinocyte cell line from adult human skin (the HaCaT cell line). For the cell viability assay, the colorimetric 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay was used. Lim-SLNs with a loading capacity and encapsulation efficiency of 0.39% and 63%, respectively, were produced by high pressure homogenization. A mean particle size of 194 ± 3.4 nm and polydispersity index of 0.244 were recorded for the loaded Lim-SLNs, as compared to 203 ± 1.5 nm (PI 0.213) for the non-loaded (blank) SLNs. The loading of the monoterpene derivative into glycerol monostearate SLNs fitted into the zero-order kinetics, and ameliorated both lipid peroxidation and cytotoxicity in a keratinocyte cell line. A promising formulation for antioxidant and anti-tumoral activities is here proposed.