Preparation, physicochemical characterization, and anti-proliferative properties of Lawsone-loaded solid lipid nanoparticles

• Published in: Chemistry and physics of lipids 2021-09, Vol.239, p.105123-105123, Article 105123
• Main Authors: Rasouliyan, Forough, Eskandani, Masoud, Jaymand, Mehdi, Akbari Nakhjavani, Sattar, Farahzadi, Raheleh, Vandghanooni, Somayeh, Eskandani, Morteza
• Format: Article
• Language: English
• Subjects: A549 Cells; Antineoplastic Agents - chemistry; Antineoplastic Agents - metabolism; Antineoplastic Agents - pharmacology; Cell Cycle Checkpoints - drug effects; Cell Death - drug effects; Cell Survival - drug effects; Cytotoxicity; Drug Carriers - chemistry; Drug Liberation; Gene Expression Regulation, Neoplastic - drug effects; Genotoxicity; Humans; Kinetics; Lawsone; Liposomes - chemistry; Nanoparticles - chemistry; Naphthoquinones - chemistry; Naphthoquinones - metabolism; Naphthoquinones - pharmacology; Particle Size; SLN; Solid lipid nanoparticles
• ISSN: 0009-3084; 1873-2941
• DOI: 10.1016/j.chemphyslip.2021.105123

•Lawsone (LWS)-loaded SLNs (LWS-SLNs) were formulated by hot homogenization technique.•LWS was encapsulated into homogenous SLNs with high efficiency.•LWS-SLNs were nano-sized with sustained release properties.•LWS-SLNs were more geno-and cytotoxic than plain LWS on A549 cell line and induced apoptosis. Lawsone (LWS) is a naphthoquinone-type dye with potential antitumor activity. LWS is used in cosmetics for coloring hair, skin, and nails. In this study, solid lipid nanoparticles (SLNs) containing LWS were prepared using a hot homogenization technique. Physicochemical properties of LWS-SLNs including encapsulation efficiency (EE), drug loading (DL), size, zeta potential, homogeneity, in vitro release, and kinetics of release were determined. The potential cytotoxic properties of LWS-SLNs were investigated. Comet assay was done to assess the genotoxicity of LWS-SLNs. The scanning electron microscopy (SEM) images revealed that LWS-SLNs were spherical and homogeneously dispersed. The average diameter of free SLNs and LWS-SLNs were 97 ± 1.4 and 127 ± 3.1 nm, respectively with high EE% (95.88 ± 3.29) and a DL of 22.72 ± 1.39 mg/mL of LWS-SLNs. The plain LWS could induce growth inhibition of A549 cells with IC50 of 17.99 ± 1.11, 13.37 ± 1.22, and 9.21 ± 1.15 μg/mL after 24, 48, and 72 h, respectively, while LWS-SLNs had more cytotoxic effects after 48 h (9.81 ± 1.3 μg/mL). Comet assay represented clear fragmentation in the chromatin of the treated cells. Besides, LWS-SLNs (13.37 ± 1.22 μg/mL) induced ∼52 % apoptosis and even necrosis after 48 h. The qPCR results showed an enhanced downregulation of Bcl-2 and upregulation of Casp 9 due to the treatment of A549 cells with LSW-SLNs. In conclusion, a stable formulation of LWS-SLN was prepared with good physicochemical features and long-term biological effects that candidate it for in vivo trials.